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Journal Description
Pharmaceutics
Pharmaceutics
is a peer-reviewed, open access journal on the science and technology of pharmaceutics and biopharmaceutics, and is published monthly online by MDPI. The Spanish Society of Pharmaceutics and Pharmaceutical Technology (SEFIG), Pharmaceutical Solid State Research Cluster (PSSRC), Academy of Pharmaceutical Sciences (APS) and Korean Society of Pharmaceutical Sciences and Technology (KSPST) are affiliated with Pharmaceutics and their members receive a discount on the article processing charges.
- Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
- High Visibility: indexed within Scopus, SCIE (Web of Science), PubMed, PMC, Embase, CAPlus / SciFinder, and other databases.
- Journal Rank: JCR - Q1 (Pharmacology and Pharmacy) / CiteScore - Q1 (Pharmaceutical Science)
- Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 14.9 days after submission; acceptance to publication is undertaken in 3.4 days (median values for papers published in this journal in the first half of 2024).
- Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
- Companion journals for Pharmaceutics include: Future Pharmacology and Journal of Pharmaceutical and BioTech Industry.
Impact Factor:
4.9 (2023);
5-Year Impact Factor:
5.5 (2023)
Latest Articles
The Role of Pharmacogenetic-Based Pharmacokinetic Analysis in Precise Breast Cancer Treatment
Pharmaceutics 2024, 16(11), 1407; https://doi.org/10.3390/pharmaceutics16111407 (registering DOI) - 31 Oct 2024
Abstract
Given the high prevalence of breast cancer and the diverse genetic backgrounds of patients, a growing body of research emphasizes the importance of pharmacogenetic-based pharmacokinetic analysis in optimizing treatment outcomes. The treatment of breast cancer involves multiple drugs whose metabolism and efficacy are
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Given the high prevalence of breast cancer and the diverse genetic backgrounds of patients, a growing body of research emphasizes the importance of pharmacogenetic-based pharmacokinetic analysis in optimizing treatment outcomes. The treatment of breast cancer involves multiple drugs whose metabolism and efficacy are influenced by individual genetic variations. Genetic polymorphisms in drug-metabolizing enzymes and transport proteins are crucial in the regulation of pharmacokinetics. Our review aims to investigate the opportunities and challenges of pharmacogenomic-based pharmacokinetic analysis as a precision medicine tool in breast cancer management.
Full article
(This article belongs to the Special Issue Role of Pharmacokinetics in Drug Development and Evaluation)
Open AccessArticle
Treatment of Inflammatory Bowel Disease by Using Curcumin-Containing Self-Microemulsifying Delivery System: Macroscopic and Microscopic Analysis
by
Nabeela Ameer, Muhammad Hanif, Ghulam Abbas, Muhammad Azeem, Khalid Mahmood, Dure Shahwar, Ahmed Khames, Essam Mohamed Eissa and Baher Daihom
Pharmaceutics 2024, 16(11), 1406; https://doi.org/10.3390/pharmaceutics16111406 - 31 Oct 2024
Abstract
Background: The lack of local availability for drugs in the colon can be addressed by preparing a self-microemulsifying drug delivery system (SMEDDS) of curcumin (Cur) which is ultimately used for the treatment of inflammatory bowel disease (IBD). Methods: From preformulation studies, Lauroglycol FCC
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Background: The lack of local availability for drugs in the colon can be addressed by preparing a self-microemulsifying drug delivery system (SMEDDS) of curcumin (Cur) which is ultimately used for the treatment of inflammatory bowel disease (IBD). Methods: From preformulation studies, Lauroglycol FCC (oil), Tween 80 (surfactant), Transcutol HP (co-surfactant), and Avicel (solid carrier) were selected for the preparation of blank liquid and solid Cur-loaded SMEDDSs (S-Cur-SMEDDSs). Results: Z-average size (12.36 ± 0.04 nm), zeta potential (−14.7 ± 0.08 mV), and polydispersity index (PDI) (0.155 ± 0.036) showed a comparative droplet surface area and charge of both SMEDDSs. The physicochemical stability of Cur in S-Cur-SMEDDSs was confirmed via FTIR, DSC, TGA, and XRD analyses, while morphological analysis through SEM and atomic force microscopy (AFM) confirmed Cur loading into SMEDDSs with an increased surface roughness root mean square (RMS) of 11.433 ± 0.91 nm, greater than the blank SMEDDS. Acute toxicity studies with an organ weight ratio and % hemolysis of 15.65 ± 1.32% at a high concentration of 600 mM showed that S-Cur-SMEDDSs are safe at a medium dose (0.2–0.8 g/kg/day). The excellent in vitro antioxidant (68.54 ± 1.42%) and anti-inflammatory properties (56.47 ± 1.17%) of S-Cur-SMEDDS proved its therapeutic efficacy for IBD. Finally, S-Cur-SMEDDS significantly improved acetic acid-induced IBD in albino rats through a reduction in the disease activity index (DAI) and macroscopic ulcer score (MUS) from 4.15 ± 0.21 to 1.62 ± 0.12 at 15 mg/kg/day dose, as confirmed via histopathological assay. Conclusions: Based on the above findings, S-Cur-SMEDDS appears to be a stable, less toxic, and more efficacious alternative for Cur delivery with strong competence in treating IBD.
Full article
(This article belongs to the Special Issue Development of New Nanotechnological Systems Loaded with Drugs for Infectious Disease Application)
Open AccessArticle
New Chalcone-Derived Molecule for the Topical Regulation of Hyperpigmentation and Skin Aging
by
Alfredo Martínez-Gutiérrez, Alexandra Bertran, Teresa Noya, Eloy Pena-Rodríguez, Susana Gómez-Escalante, Sergio Pascual, Luis Shotze Luis and Mari Carmen González
Pharmaceutics 2024, 16(11), 1405; https://doi.org/10.3390/pharmaceutics16111405 - 31 Oct 2024
Abstract
Background/Objectives: Skin hyperpigmentation is a biological process that results in an excessive production of melanin and is highly regulated by several mechanisms, tyrosinase being one of the key enzymes involved. Current reported inhibitors lack clinical efficacy, show toxic side effects, have poor
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Background/Objectives: Skin hyperpigmentation is a biological process that results in an excessive production of melanin and is highly regulated by several mechanisms, tyrosinase being one of the key enzymes involved. Current reported inhibitors lack clinical efficacy, show toxic side effects, have poor bioavailability, or low formulation compatibility. The aim of this study was to design a new effective tyrosinase inhibitor for topical hyperpigmentation and anti-aging treatments. Methods: Homology modeling was used to build the tridimensional structure of human tyrosinase, and virtual docking was used to predict molecule–enzyme binding modes. The tyrosinase activity of the designed and synthesized compounds was assessed and water solubility was determined by HPLC. Cell assays were performed to determine melanin content, cytotoxicity, wound healing, anti-glycation, antioxidation, and autophagy efficacy. Gene expression and miRNA levels were quantified by qPCR and chromatin accessibility by ATAC-Seq. Human reconstructed epidermis was used to test the depigmenting efficacy as well as the skin irritation potential. Results: The 3D structure of human tyrosinase was designed and validated. The new molecule could effectively inhibit human tyrosinase and melanin synthesis in 2D monocultures and a 3D epidermis model. Two melanogenesis-related miRNAs were increased in treated cells. Anti-glycation, antioxidant, mitochondria protection, autophagy activation, and wound healing properties were also observed, with special emphasis on epigenetics. Conclusions: The designed molecule is a potential candidate to be used as a depigmenting and anti-aging agent, with suitable properties to be introduced in final product formulations for dermatology or cosmetics treatments.
Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds in Pharmaceutical Formulations and Drug Delivery Systems)
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Open AccessArticle
Chemical Characterization and In Vitro Evaluation of Glucans from Fermentation-Produced Nutraceutical Bionutri-AR1®: Antioxidant and Immunomodulatory Properties
by
Elaine R. Carbonero, Tammara S. M. Novikov, Yagly G. S. Gomes, Dayane R. Brito, Luisa C. Coelho, Marcia F. Mendes, Maria Carolina B. Di Medeiros Leal, Anamélia L. Bocca and Luciano M. Lião
Pharmaceutics 2024, 16(11), 1404; https://doi.org/10.3390/pharmaceutics16111404 - 31 Oct 2024
Abstract
Background: The consumption of nutraceuticals or food supplements has increased crucially, aiming to address nutrient deficits and enhance immune system function. To develop safe food products with unique nutritional and functional benefits, new production methods of these nutraceuticals such as the fermentative process
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Background: The consumption of nutraceuticals or food supplements has increased crucially, aiming to address nutrient deficits and enhance immune system function. To develop safe food products with unique nutritional and functional benefits, new production methods of these nutraceuticals such as the fermentative process have been gaining prominence for industrial applications. Bionutri-AR1® is a nutraceutical produced via this bioprocess, featuring a complex composition, that has been used to improve the immune systems of debilitated people. Objectives: Considering the various biological properties attributed to glucans, one of its main components, this study aims to structurally characterize and evaluate, in vitro, the antioxidant and immunomodulatory potential of the polymers from this nutraceutical to assess whether these polymers contribute to the product’s reported biological effects. Methods/Results: Unlike previous reports, this study characterized by NMR, GC-MS, and Congo Red assay techniques two main glucans: a water-insoluble linear α-D-glucan with glycosidic bonds (1→4) and a soluble branched (1→3)- and (1→6)-linked β-glucan with a triple helix. Both glucans showed significant antioxidant activity, measured by their capacity to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. They were also capable of inducing the secretion of cytokines such as tumoral necrosis factor-alpha (TNF-α), interleukin 10 (IL-10), and interleukin 6 (IL-6), determined through capture enzyme-linked immunosorbent assay (ELISA), especially when co-stimulated with lipopolysaccharide (LPS). Conclusions: This suggests a dual action of these glucans in both proinflammatory and regulatory pathways. Future studies will describe the mechanisms by which these glucans, especially the insoluble ones, enhance immune system function, highlighting their potential use in immunotherapy.
Full article
(This article belongs to the Section Biopharmaceutics)
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Open AccessReview
Skin Structure, Physiology, and Pathology in Topical and Transdermal Drug Delivery
by
Sofia Brito, Moonki Baek and Bum-Ho Bin
Pharmaceutics 2024, 16(11), 1403; https://doi.org/10.3390/pharmaceutics16111403 - 31 Oct 2024
Abstract
Several industries are increasingly focused on enhancing the delivery of active ingredients through the skin to optimize therapeutic outcomes. By facilitating the penetration of active ingredients through the skin barrier, these enhancers can significantly improve the efficacy of various formulations, ranging from skincare
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Several industries are increasingly focused on enhancing the delivery of active ingredients through the skin to optimize therapeutic outcomes. By facilitating the penetration of active ingredients through the skin barrier, these enhancers can significantly improve the efficacy of various formulations, ranging from skincare products to therapeutic agents targeting systemic circulation. As the understanding of skin physiology and the mechanisms of drug absorption deepen, these industries are adopting permeation enhancers more widely, ultimately leading to better patient outcomes and expanded treatment options. However, the structure and physiological function of the skin can vary according to different factors, such as the area of the body and between individuals. These variations, along with external environmental exposures, aging and pathological conditions, introduce complexities that must be carefully considered when designing effective delivery systems. Considering the intricacies of skin structure and physiology, tailoring systems to account for regional differences, individual variability, and changes induced by environmental factors or disease is critical to optimizing therapeutic outcomes. This review discusses the features of skin structure, physiology, and pathologies, as well as the application of permeation enhancers in these contexts. Furthermore, it addresses the use of animal skin models in transdermal delivery and dermatological studies, along with the latest developments in this field.
Full article
(This article belongs to the Special Issue Transdermal Delivery: Challenges and Opportunities)
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Open AccessArticle
The Combination of Buparvaquone and ELQ316 Exhibit a Stronger Effect than ELQ316 and Imidocarb Against Babesia bovis In Vitro
by
Natalia M. Cardillo, Nicolas F. Villarino, Paul A. Lacy, Michael K. Riscoe, Joseph Stone Doggett, Massaro W. Ueti, Chungwon J. Chung and Carlos E. Suarez
Pharmaceutics 2024, 16(11), 1402; https://doi.org/10.3390/pharmaceutics16111402 - 31 Oct 2024
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Background/Objectives: Bovine babesiosis is a vector-borne disease transmitted by ticks that causes important losses in livestock worldwide. Recent research performed on the drugs currently used to control bovine babesiosis reported several issues including drug resistance, toxicity impact, and residues in edible tissue, suggesting
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Background/Objectives: Bovine babesiosis is a vector-borne disease transmitted by ticks that causes important losses in livestock worldwide. Recent research performed on the drugs currently used to control bovine babesiosis reported several issues including drug resistance, toxicity impact, and residues in edible tissue, suggesting the need for developing novel effective therapies. The endochin-like quinolones ELQ-316 and buparvaquone (BPQ) act as cytochrome bc1 inhibitors and have been proven to be safe and efficacious against related apicomplexans, such as Plasmodium spp. and Babesia microti, without showing toxicity in mammals. The objectives of this study are investigating whether ELQ-316, BPQ, and their combination treatment could be effective against Babesia bovis in an in vitro culture model and comparing with imidocarb (ID), the routinely used drug. Methods: In vitro cultured parasites starting at 2% percentage of parasitemia (PPE) were treated with BPQ, ELQ-316, ID, and the combinations of BPQ + ELQ-316 and ID + ELQ-316 at drug concentrations that ranged from 25 to 1200 nM, during four consecutive days. The IC50% and IC99% were reported. Parasitemia levels were evaluated daily using microscopic examination. Data were compared using the non-parametrical Mann–Whitney and Kruskall–Wallis test. Results: All drugs tested, whether used alone or in combination, significantly decreased the survival (p < 0.05) of B. bovis in in vitro cultures. The combination of BPQ + ELQ-316 had the lowest calculated inhibitory concentration 50% (IC50%) values, 31.21 nM (IC95%: 15.06–68.48); followed by BPQ, 77.06 nM (IC95%: 70.16–86.01); ID + ELQ316, 197 nM (IC95%:129.0–311.2); ID, 635.1 nM (IC95%: 280.9–2119); and ELQ316, 654.9 nM (IC95%: 362.3–1411). Conclusions: The results reinforce the higher efficacy of BPQ at affecting B. bovis survival and the potential synergistic effects of its combination with ELQ-316, providing a promising treatment option against B. bovis.
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Open AccessReview
Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective
by
Ivana Z. Kuzminac, Andrea R. Nikolić, Marina P. Savić and Jovana J. Ajduković
Pharmaceutics 2024, 16(11), 1401; https://doi.org/10.3390/pharmaceutics16111401 - 30 Oct 2024
Abstract
Due to the high prostate cancer incidence worldwide, the development of different methods of treatment continues to be a hot research topic. Since its first clinical application at the beginning of the 2010s, abiraterone in the form of prodrug abiraterone acetate continues to
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Due to the high prostate cancer incidence worldwide, the development of different methods of treatment continues to be a hot research topic. Since its first clinical application at the beginning of the 2010s, abiraterone in the form of prodrug abiraterone acetate continues to be the most used hormone derivative in the treatment of castration-resistant prostate cancer. This is the reason behind the publication of many scientific results regarding its synthesis, biological activity, metabolism, novel designed steroid derivatives based on its structure, etc. A similar steroid compound with a heterocycle in the C17 position, called galeterone, also designed to treat prostate cancer, continues to be in clinical studies, which provides further proof of the importance of these steroid derivatives. Besides prostate cancer treatment, abiraterone showed indications for possible clinical application in the treatment of breast, ovarian, lung, kidney, salivary gland, and adrenocortical cancer, congenital adrenal hyperplasia, Cushing’s syndrome, and COVID-19, while galeterone is investigated for its use against prostate, pancreatic, and breast cancer. Herein, we report a review comprising methods of synthesis, possible clinical applications, and mechanisms of action, as well as structures and bioactivities of derivatives of these two important steroids.
Full article
(This article belongs to the Special Issue Steroid Derivatives: Design and Pharmaceutical Application)
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Open AccessArticle
Assessing Drug Product Shelf Life Using the Accelerated Stability Assessment Program: A Case Study of a GLPG4399 Capsule Formulation
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Dattatray Modhave, Sara Vrielynck and Kevin Roeleveld
Pharmaceutics 2024, 16(11), 1400; https://doi.org/10.3390/pharmaceutics16111400 - 30 Oct 2024
Abstract
Objective: To evaluate and project the shelf life of GLPG4399, an early-phase clinical drug formulation by applying the Accelerated Stability Assessment Program (ASAP) approach. Methods: Forced degradation conditions were implemented to identify the stability-limiting degradation product. The drug and its degradation products were
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Objective: To evaluate and project the shelf life of GLPG4399, an early-phase clinical drug formulation by applying the Accelerated Stability Assessment Program (ASAP) approach. Methods: Forced degradation conditions were implemented to identify the stability-limiting degradation product. The drug and its degradation products were separated using a validated liquid chromatography method. Then, the selected clinical capsule formulation was placed in a glass vial and exposed to accelerated short-term conditions of combinations of high- and low-level heat and humidity in an open state for 5 weeks. The liquid chromatography results were evaluated using the ASAP, which is based on the moisture-modified Arrhenius principle. The resulting data were fitted using a suitable diffusion kinetics method. Results: The developed model was applied to predict the shelf life of the drug product when using clinically appropriate primary packaging (high-density polyethylene container). The derived stability parameters of the moisture-modified Arrhenius equation were the Arrhenius collision frequency, activation energy, and humidity sensitivity constant. The goodness of fit parameters R2 (>0.95) and goodness of prediction Q2 (>0.80) parameters for the selected model were acceptable. The results of the accelerated, short-term stability study were verified against real-time, long-term 12-month data. Conclusions: We demonstrated the application of the ASAP approach to evaluate the shelf life of a GLPG4399 solid capsule formulation. The studied ASAP approach can be extended to evaluate the stability and shelf-life estimations of other early-phase clinical formulations.
Full article
(This article belongs to the Special Issue Stability of Medicines and Novel Approaches for Predicting Drug Stability)
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Open AccessArticle
Afro-Latin American Pharmacogenetics of CYP2D6, CYP2C9, and CYP2C19 in Dominicans: A Study from the RIBEF-CEIBA Consortium
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Mariela Guevara, Fernanda Rodrigues-Soares, Carla González de la Cruz, Fernando de Andrés, Ernesto Rodríguez, Eva Peñas-Lledó, Adrián LLerena and CEIBA Consortium of the Ibero-American Network of Pharmacogenetics and Pharmacogenomics RIBEF
Pharmaceutics 2024, 16(11), 1399; https://doi.org/10.3390/pharmaceutics16111399 - 30 Oct 2024
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Background/Objectives: Research on pharmacogenetic variability in response to prescribed drugs and across ethnic groups is essential for personalized medicine, particularly in admixed and unstudied populations. For the first time, this study examines CYP2D6, CYP2C9, and CYP2C19 alleles and genotypes in
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Background/Objectives: Research on pharmacogenetic variability in response to prescribed drugs and across ethnic groups is essential for personalized medicine, particularly in admixed and unstudied populations. For the first time, this study examines CYP2D6, CYP2C9, and CYP2C19 alleles and genotypes in 197 healthy volunteers from the Dominican Republic, as part of the RIBEF-CEIBA collaborative network. Methods: The analysis focuses on the participants’ tri-hybrid genomic ancestry, with CYP alleles determined by real-time PCR and molecular ancestry inferred using 90 AIMs. Linear regression was used to associate ancestry components with CYP frequencies. Results: The average ancestry was 23.8% European, 42.6% Native American, and 33.6% African, the latter being higher than in most Latin American populations. Native American ancestry was also higher than expected. Predicted phenotype frequencies based on genotypes were 4.2% poor metabolizers (gPMs) and 3.6% ultrarapid metabolizers (gUMs) for CYP2D6, as well as 3% gPMs, 22.8% rapid metabolizers (gRMs), and 1.5% gUMs for CYP2C19. No gPM individuals were observed for CYP2C9. Certain alleles associated with decreased CYP2D6 activity (*17 and *29) and increased CYP2C19 activity (*17 and gUMs) were positively linked with African ancestry and negatively with Native American ancestry. Rare CYP2C9 alleles (*5 and *6) with clinical relevance were additionally found. Conclusions: These findings build on previous results from the RIBEF-CEIBA collaborative network, demonstrating differences in allele frequencies of CYP2D6, CYP2C9, and CYP2C19 in relation to genomic ancestry. In summary, ethnicity must be considered in the development of pharmacogenetic guidelines for clinical application, research, and regulation to avoid widening the biotechnology gap and to allow Personalized Medicine to reach the entire world population.
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Open AccessReview
Revolutionizing Eye Care: Exploring the Potential of Microneedle Drug Delivery
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Satish Rojekar, Swapnali Parit, Amol D. Gholap, Ajit Manchare, Sopan N. Nangare, Navnath Hatvate, Vrashabh V. Sugandhi, Keshav Raj Paudel and Rahul G. Ingle
Pharmaceutics 2024, 16(11), 1398; https://doi.org/10.3390/pharmaceutics16111398 - 30 Oct 2024
Abstract
Microneedle technology revolutionizes ocular drug delivery by addressing challenges in treating ocular diseases. This review explores its potential impact, recent advancements, and clinical uses. This minimally invasive technique offers precise control of drug delivery to the eye, with various microneedle types showing the
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Microneedle technology revolutionizes ocular drug delivery by addressing challenges in treating ocular diseases. This review explores its potential impact, recent advancements, and clinical uses. This minimally invasive technique offers precise control of drug delivery to the eye, with various microneedle types showing the potential to penetrate barriers in the cornea and sclera, ensuring effective drug delivery. Recent advancements have improved safety and efficacy, offering sustained and controlled drug delivery for conditions like age-related macular degeneration and glaucoma. While promising, challenges such as regulatory barriers and long-term biocompatibility persist. Overcoming these through interdisciplinary research is crucial. Ultimately, microneedle drug delivery presents a revolutionary method with the potential to significantly enhance ocular disease treatment, marking a new era in eye care.
Full article
(This article belongs to the Special Issue Microarray Patches for Transdermal Drug Delivery)
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Open AccessReview
Challenges and Opportunities in Managing Geriatric Depression: The Role of Personalized Medicine and Age-Appropriate Therapeutic Approaches
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Agnieszka Jaros, Filip Rybakowski, Judyta Cielecka-Piontek, Magdalena Paczkowska-Walendowska, Bogusław Czerny, Adam Kamińki, Rasha Wafaie Mahmoud Elsorady and Agnieszka Bienert
Pharmaceutics 2024, 16(11), 1397; https://doi.org/10.3390/pharmaceutics16111397 - 30 Oct 2024
Abstract
The global aging population has experienced rapid growth in recent decades, leading to an increased prevalence of psychiatric disorders, particularly depression, among older adults. Depression in the geriatric population is often compounded by chronic physical conditions and various psychosocial factors, significantly impacting their
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The global aging population has experienced rapid growth in recent decades, leading to an increased prevalence of psychiatric disorders, particularly depression, among older adults. Depression in the geriatric population is often compounded by chronic physical conditions and various psychosocial factors, significantly impacting their quality of life. The main question raised in this review is as follows: how can personalized medicine and age-appropriate therapeutic approaches improve the management of geriatric depression? This paper explores the epidemiology of geriatric depression, highlighting the influence of gender, race, and socioeconomic status on its prevalence. The classification and diagnosis of geriatric depressive disorders, based on ICD-11 and DSM-5 criteria, reveal the complexity of managing these conditions in older adults. Personalized medicine (PM) emerges as a promising approach, focusing on tailoring treatments to the individual’s genetic, clinical, and environmental characteristics. However, the application of PM in this demographic faces challenges, particularly in the context of pharmaceutical forms. The need for age-appropriate drug delivery systems is critical, given the prevalence of polypharmacy and issues such as dysphagia among the older patients. This study emphasizes the importance of developing patient-centric formulations to enhance the effectiveness of personalized therapy in geriatric patients.
Full article
(This article belongs to the Special Issue Pharmacokinetics and Drug–Drug Interactions of Novel Psychotropic Drugs)
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The Ability of Vaping Technology to Deliver an Equivalent Respirable Dose of Beclomethasone Dipropionate Compared to Nebulization
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Cyrille Bruneau, Clément Mercier, Lara Leclerc and Jérémie Pourchez
Pharmaceutics 2024, 16(11), 1396; https://doi.org/10.3390/pharmaceutics16111396 - 30 Oct 2024
Abstract
Background/Objectives: This study focuses on the ability of vaping technology to deliver beclomethasone dipropionate compared to nebulization. Methods: An in vitro comparison of aerosol properties in terms of respirable dose with the Glass Twin Impinger and the mass median aerodynamic diameter
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Background/Objectives: This study focuses on the ability of vaping technology to deliver beclomethasone dipropionate compared to nebulization. Methods: An in vitro comparison of aerosol properties in terms of respirable dose with the Glass Twin Impinger and the mass median aerodynamic diameter using the Next Generation Impactor was performed. The respirable dose delivered in a vaping drug delivery system (VDDS) puff as a function of concentration was quantified by high-pressure liquid chromatography coupled with an ultraviolet detector. Results: The mass of drug contained in a single puff of 55 mL of aerosol varied between 0.94 and 1.95 µg for a refill liquid concentration range of 400 to 1600 µg/mL. The analysis of the particle size distribution shows an advantage for a VDDS in producing smaller particles compared to nebulization (1.56 ± 0.05 µm vs. 2.30 ± 0.19 µm). In total, 81 puffs are needed to reach the dose equivalent to nebulized beclomethasone dipropionate under these specific experimental conditions, which corresponds to an aerosol duration of about 4 min (i.e., four times lower than the jet nebulizer) and a patient administration time of about 45 min (i.e., three times higher than the jet nebulizer). Conclusions: The results show the potential of vaping devices as an alternative to nebulizers for the administration of beclomethasone dipropionate in an equivalent respirable dose.
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(This article belongs to the Special Issue Drug Delivery Systems for Respiratory Diseases)
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Open AccessArticle
Targeted Magnetic Nanoparticles for Beta-Amyloid Detection
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Nelly S. Chmelyuk, Aleksey A. Nikitin, Veronika V. Vadekhina, Vladimir A. Mitkevich and Maxim A. Abakumov
Pharmaceutics 2024, 16(11), 1395; https://doi.org/10.3390/pharmaceutics16111395 - 29 Oct 2024
Abstract
Background/Objectivities: The presence of beta-amyloid plaques is a part of the pathogenesis of Alzheimer’s disease, but there is currently no universally accepted method for magnetic resonance (MR) imaging of the disease. However, it is known that magnetic nanoparticles (MNPs) can improve the T2
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Background/Objectivities: The presence of beta-amyloid plaques is a part of the pathogenesis of Alzheimer’s disease, but there is currently no universally accepted method for magnetic resonance (MR) imaging of the disease. However, it is known that magnetic nanoparticles (MNPs) can improve the T2 contrast in MR images of various targets. Methods: We used cubic MNPs, which were produced by thermal decomposition and then it was covalently bonded to a modified fluorescently labeled tetrapeptide, HAEE-Cy5, for visualizing beta-amyloid plaques. The interaction of MNPs-HAEE-Cy5 and beta-amyloid was determinate by confocal microscopy using SH-SY5Y cell line. Results: MNPs exhibit relatively high relaxivity (approximately 200 mM−1s−1), which is crucial for enhancing target visibility in MR imaging. HAEE provides targeted delivery of MNPs by specifically interacting with beta-amyloid, while the fluorescent label Cy5 enables monitoring the efficacy of the interaction through confocal microscopy. Conclusions: The MNPs modified with HAEE-Cy5 demonstrated excellent binding to beta-amyloid plaques in vitro, as shown by experiments on the SH-SY5Y cell line. These results suggest that the proposed method has potential for use in future MR imaging studies of Alzheimer’s disease.
Full article
(This article belongs to the Special Issue Metal-Based Nanoparticles for Pharmaceutical Applications)
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Open AccessReview
Minimal Information for Studies of Extracellular Vesicles (MISEV): Ten-Year Evolution (2014–2023)
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Yuan Zhang, Mengyi Lan and Yong Chen
Pharmaceutics 2024, 16(11), 1394; https://doi.org/10.3390/pharmaceutics16111394 - 29 Oct 2024
Abstract
In the tenth year since the first edition of MISEV was released in 2014, MISEV2023 has been reported in 2024 with the aim of refining the standard and improving the rigor, reproducibility, and transparency of extracellular vesicle (EV) research to clarify the requirements
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In the tenth year since the first edition of MISEV was released in 2014, MISEV2023 has been reported in 2024 with the aim of refining the standard and improving the rigor, reproducibility, and transparency of extracellular vesicle (EV) research to clarify the requirements for experimental design of EVs, emphasize the importance of reproducible experimental results as well as encouraging openness of experimental information. The release of MISEV has significantly contributed to the quality of research in the field of EVs, which creates a more reliable research environment. However, despite the important role of MISEV, there is still a need for the EV researchers to continue to push for the widespread implementation of the guidelines to meet the evolving nature and challenges of EV research. The evolution of EV research and the attention it receives have grown exponentially over time, as has the number of people involved in the writing of MISEV. Here, this review briefly summarizes the evolution of the three editions of MISEV, aiming to recall MISEV2014 and MISEV2018 while learning about the latest release, MISEV2023, to gain a deeper understanding of the content, and to provide a quick note for beginners who want to learn about MISEV and explore the EV world.
Full article
(This article belongs to the Special Issue Advances of Membrane Vesicles in Drug Delivery Systems, 2nd Edition)
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Open AccessArticle
Antimycobacterial Activity of Essential Oils from Bulgarian Rosa Species Against Phylogenomically Different Mycobacterium tuberculosis Strains
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Violeta Valcheva, Milka Mileva, Marine Dogonadze, Ana Dobreva and Igor Mokrousov
Pharmaceutics 2024, 16(11), 1393; https://doi.org/10.3390/pharmaceutics16111393 - 29 Oct 2024
Abstract
In this study, we aimed to assess the activity of the essential oils from four Bulgarian oil-bearing roses Rosa damascena Mill., R. alba L., R. centifolia L., and R. gallica L., on the reference strain Mycobacterium tuberculosis H37Rv and clinical M. tuberculosis strains
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In this study, we aimed to assess the activity of the essential oils from four Bulgarian oil-bearing roses Rosa damascena Mill., R. alba L., R. centifolia L., and R. gallica L., on the reference strain Mycobacterium tuberculosis H37Rv and clinical M. tuberculosis strains of the Beijing and Latin-American Mediterraneum genotypes. The chemical composition of the essential oils was determined by gas chromatography (GC-FID/MS). Minimal inhibitory concentrations (MIC) were determined using the resazurin method. R. alba oil showed the highest inhibitory activity when tested on all strains of different phylogenetic origins with MIC in the range of 0.16–0.31 mg/mL, while R. gallica oil was the least active (MIC 0.62–1.25 mg/mL). The obtained results show heterogeneity of rose oil action on different mycobacterial strains and we hypothesize that the combined level of geraniol and nerol is a key factor that underlies the antimycobacterial action of the rose oils. Strain Beijing 396 was relatively more susceptible to the rose oils probably due to multiple and likely deleterious mutations in its efflux pump genes. Two clinical MDR strains have likely developed during their previous adaptation to anti-TB drugs certain drug tolerance mechanisms that also permitted them to demonstrate intrinsic tolerance to the essential oils. Further research should investigate a possible synergistic action of the new-generation anti-TB drugs and the most promising rose oil extracts on the large panel of different strains.
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(This article belongs to the Special Issue Antimicrobial Resistance and Antimicrobial Activity of Bioactive Compounds in Drug Formulations)
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Open AccessArticle
Stability Studies of a Tetraethyl Orthosilicate-Based Thixotropic Drug Delivery System
by
Emma Barrett-Catton, Elizabeth M. Arrigali, Bogdan A. Serban, Kolton C. Sandau and Monica A. Serban
Pharmaceutics 2024, 16(11), 1392; https://doi.org/10.3390/pharmaceutics16111392 - 29 Oct 2024
Abstract
Background/Objectives: This study assessed the effects of formulation components on the long-term stability of a previously described tetraethyl orthosilicate-based drug delivery system. Early stability studies of a product concept are crucial not only to provide information on the overall system stability and individual
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Background/Objectives: This study assessed the effects of formulation components on the long-term stability of a previously described tetraethyl orthosilicate-based drug delivery system. Early stability studies of a product concept are crucial not only to provide information on the overall system stability and individual components’ contributions to it, but also to identify opportunities for dosage form optimization and to define its use case. Methods: We assessed the time-dependent thixogel properties—specifically, mechanical strength, thixotropy, release of model drug, and dry substance—in both real-time and accelerated shelf-life determination set-ups. Results: Our findings indicate that the concentration and molecular weight of hyaluronic acid, one of the main constituents of the investigated thixotropic systems, are key determinants of formulation stability. We further showed that changes in both of these parameters reflect on the drug release properties and stiffness of the formulation and could inform subsequent product development based on several use cases. Conclusions: Overall, this study provides an understanding of some key factors that would need to be considered prior to and in the final product development process of thixogels in preparation for commercialization.
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(This article belongs to the Special Issue Biodegradable Hydrogels with Potential Biomedical Applications as Drug Delivery Systems)
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Open AccessReview
Pharmacological Treatment of Interstitial Lung Diseases: A Novel Landscape for Inhaled Agents
by
Vito D’Agnano, Fabio Perrotta, Ramona Fomez, Valerio Maria Carrozzo, Angela Schiattarella, Stefano Sanduzzi Zamparelli, Raffaella Pagliaro, Andrea Bianco and Domenica Francesca Mariniello
Pharmaceutics 2024, 16(11), 1391; https://doi.org/10.3390/pharmaceutics16111391 - 29 Oct 2024
Abstract
Interstitial lung diseases (ILDs) encompass a heterogeneous group of over 200 disorders that require individualized treatment. Antifibrotic agents, such as nintedanib and pirfenidone, have remarkably revolutionized the treatment landscape of patients with idiopathic pulmonary fibrosis (IPF). Moreover, the approval of nintedanib has also
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Interstitial lung diseases (ILDs) encompass a heterogeneous group of over 200 disorders that require individualized treatment. Antifibrotic agents, such as nintedanib and pirfenidone, have remarkably revolutionized the treatment landscape of patients with idiopathic pulmonary fibrosis (IPF). Moreover, the approval of nintedanib has also expanded the therapeutic options for patients with progressive pulmonary fibrosis other than IPF. However, despite recent advances, current therapeutic strategies based on antifibrotic agents and/or immunomodulation are associated with non-negligible side effects. Therefore, several studies have explored the inhalation route aiming to spread higher local concentrations while limiting systemic toxicity. In this review, we examined the currently available literature about preclinical and clinical studies testing the efficacy and safety of inhalation-based antifibrotics, immunomodulatory agents, antioxidants, mucolytics, bronchodilators, and vasodilator agents in ILDs.
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(This article belongs to the Special Issue Inhalable Drugs for the Treatment of Chronic Respiratory Diseases)
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Enhanced Ocular Drug Delivery of Dexamethasone Using a Chitosan-Coated Soluplus®-Based Mixed Micellar System
by
Samer Adwan, Faisal Al-Akayleh, Madeiha Qasmieh and Teiba Obeidi
Pharmaceutics 2024, 16(11), 1390; https://doi.org/10.3390/pharmaceutics16111390 - 29 Oct 2024
Abstract
Background: This study introduces a novel dexamethasone (DEX) mixed micellar system (DEX-MM) using Soluplus® and Pluronic F-127 (PF127) to enhance ocular drug delivery. The enhancement of ocular application properties was achieved by creating a chitosan-coated DEX-MM (DEX-CMM), which promotes better adherence to
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Background: This study introduces a novel dexamethasone (DEX) mixed micellar system (DEX-MM) using Soluplus® and Pluronic F-127 (PF127) to enhance ocular drug delivery. The enhancement of ocular application properties was achieved by creating a chitosan-coated DEX-MM (DEX-CMM), which promotes better adherence to the ocular surface, thereby improving drug absorption. Methods: Using the solvent evaporation method, a formulation was developed with a Soluplus®-to-drug ratio of 1:10, enhanced with 0.25% PF127. After dispersing in water, 1% chitosan (CS) was added. The stability and integrity of DEX within the micelles were verified using attenuated total reflection–Fourier transform infrared spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC). Additionally, in vitro and ex vivo drug release studies were conducted. Results: DEX-CMM (F6) demonstrated a particle size of 151.9 ± 1 nm and a polydispersity index (PDI) of 0.168 ± 0.003, suggesting uniformity and high electrostatic stability with a zeta potential of +35.96 ± 2.13 mV. The non-Fickian drug release mechanism indicated prolonged drug retention. Comparative analyses showed DEX-CMM outperforming a standard DEX suspension in drug release and ocular tissue permeation, with flux measurements significantly higher than the DEX suspension. Conclusion: The study confirmed the efficacy of DEX-CMM in enhancing drug delivery to ocular tissues, evidenced by improved permeability. Safety evaluations using the HET-CAM test demonstrated that DEX-CMM was non-irritant, supporting its potential for effective ocular drug delivery.
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(This article belongs to the Special Issue Ophthalmic Drug Delivery, 3rd Edition)
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Open AccessArticle
Design of Experiments to Tailor the Potential of BSA-Coated Peptide Nanocomplexes for Temozolomide/p53 Gene Co-Delivery
by
Inês Afonso, Ana R. Neves, Dalinda Eusébio, Tânia Albuquerque, Eric Vivès, Prisca Boisguérin, Adriana O. Santos, Ângela Sousa and Diana Costa
Pharmaceutics 2024, 16(11), 1389; https://doi.org/10.3390/pharmaceutics16111389 - 29 Oct 2024
Abstract
Background: Gene therapy can be viewed as a promising/valuable therapeutic approach directed to cancer treatment, including glioblastoma. Concretely, the combination of gene therapy with chemotherapy could increase its therapeutic index due to a synergistic effect. In this context, bovine serum albumin (BSA)-coated temozolomide
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Background: Gene therapy can be viewed as a promising/valuable therapeutic approach directed to cancer treatment, including glioblastoma. Concretely, the combination of gene therapy with chemotherapy could increase its therapeutic index due to a synergistic effect. In this context, bovine serum albumin (BSA)-coated temozolomide (TMZ)-peptide (WRAP5)/p53 gene-based plasmid DNA complexes were developed to promote payload co-delivery. Methods: Design of experiments (DoE) was employed to unravel the BSA-coated TMZ-WRAP5/p53 nanocomplexes with the highest potential by considering the nitrogen to phosphate groups ratio (N/P), and the BSA concentration as inputs and the size, polydispersity index, surface charge and p53-based plasmid complexation capacity (CC) as DoE outputs. Results: The obtained quadratic models were statistically significant (p-value < 0.05) with an adequate coefficient of determination, and the correspondent optimal points were successfully validated. The optimal complex formulation had N/P of 1.03, a BSA concentration of 0.08%, a size of approximately 182 nm, a zeta potential of +9.8 mV, and a pDNA CC of 96.5%. The optimal nanocomplexes are approximately spherical. A cytotoxicity assay showed that these BSA-coated TMZ-WRAP5/p53 complexes did not elicit toxicity in normal brain cells, and a hemolysis study demonstrated the hemocompatibility of the complexes. The complexes were stable in cell culture medium and fetal bovine serum and assured pDNA protection and release. Moreover, the optimal BSA-coated complexes were able of gene transcription and promoted a significant inhibition of glioblastoma cell viability. Conclusions: The reported findings instigate the development of future research to evaluate their potential utility to TMZ/p53 co-delivery. The DoE tool proved to be a powerful approach to explore and tailor the composition of BSA-coated TMZ-WRAP5/p53 complexes, which are expected to contribute to the progress toward a more efficient therapy against cancer and, more specifically, against glioblastoma.
Full article
(This article belongs to the Special Issue Smart Nanocarriers for Drug Delivery in Cancer Therapy)
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Physically Cross-Linked PVA Hydrogels as Potential Wound Dressings: How Freezing Conditions and Formulation Composition Define Cryogel Structure and Performance
by
Anna Górska, Ewelina Baran, Justyna Knapik-Kowalczuk, Joanna Szafraniec-Szczęsny, Marian Paluch, Piotr Kulinowski and Aleksander Mendyk
Pharmaceutics 2024, 16(11), 1388; https://doi.org/10.3390/pharmaceutics16111388 - 28 Oct 2024
Abstract
Objectives: Hydrogels produced using the freeze–thaw method have demonstrated significant potential for wound management applications. However, their production requires precise control over critical factors including freezing temperature and the choice of matrix-forming excipients, for which no consensus on the optimal conditions currently
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Objectives: Hydrogels produced using the freeze–thaw method have demonstrated significant potential for wound management applications. However, their production requires precise control over critical factors including freezing temperature and the choice of matrix-forming excipients, for which no consensus on the optimal conditions currently exists. This study aimed to address this gap by evaluating the effects of the above-mentioned variables on cryogel performance. Methods: Mechanical properties, absorption capacity, and microstructure were assessed alongside advanced analyses using differential scanning calorimetry (DSC) and low-field nuclear magnetic resonance relaxometry (LF TD NMR). Results: The results demonstrated that fully hydrolyzed polyvinyl alcohol (PVA) with a molecular weight above 61,000 g/mol is essential for producing high-performance cryogels. Among the tested formulations, an 8% (w/w) PVA56–98 solution (Mw~195,000; DH = 98.0–98.8%) with 10% (w/w) propylene glycol (PG) provided the best balance of stretchability, durability, and low adhesion. Notably, while −25 °C is often used for cryogel preparation, freezing the gel precursor at −80 °C yielded superior results, producing materials with more open, interconnected structures and enhanced mechanical strength and elasticity—deviating from conventional practices. Conclusions: The designed cryogel prototypes exhibited functional properties comparable to or even surpassing commercial wound dressings, except for absorption capacity, which remained lower. Despite this, the cryogel prototypes demonstrated potential as wound dressings, particularly for use in dry or minimally exuding wounds. All in all, this study provides a comprehensive analysis of the physicochemical and functional properties of PVA cryogels, establishing a strong foundation for the development of advanced wound dressing systems.
Full article
(This article belongs to the Special Issue Prospects of Hydrogels in Wound Healing)
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