Pharmaceutics

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21 pages, 2272 KiB

Open AccessArticle

The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems

by Katarina Rede, Mirjana Gašperlin, Marija Bogataj and Katarina Bolko Seljak

Pharmaceutics 2025, 17(5), 545; https://doi.org/10.3390/pharmaceutics17050545 - 23 Apr 2025

Abstract

Objectives: A novel two-step flow-through in vitro lipolysis model was developed for the evaluation of drug release from a self-microemulsifying drug delivery system (SMEDDS). Methods: Firstly, the SMEDDS was dispersed in an acidic medium. Subsequently, the pH was increased, and a [...] Read more.

Objectives: A novel two-step flow-through in vitro lipolysis model was developed for the evaluation of drug release from a self-microemulsifying drug delivery system (SMEDDS). Methods: Firstly, the SMEDDS was dispersed in an acidic medium. Subsequently, the pH was increased, and a lipolytic reaction was immediately initiated, accompanied by medium flow onset. The latter enabled increase of the initial low pH of the medium, improving the physiological relevance of the method by simulating dosage form retainment in the stomach and transfer to the duodenum, which is very important for a weakly basic active pharmaceutical ingredient (API) incorporated in an SMEDDS. Results: Conversely to the traditional pH-stat in vitro lipolysis, the developed method is not established on titration, as the reaction vessel pH is regulated by a medium flow and buffer capacity. Individual parameters, such as pancreatin activity, buffer capacity, and medium shift, were researched using traditional pH-stat in vitro lipolysis prior to their implementation in the flow-through setup. Conclusions: The concentration of the solubilized model API, carvedilol, was increased as pancreatin activity decreased and as buffer capacity increased. The ratios between release profiles obtained under different conditions utilizing the pH-stat and novel two-step flow-through in vitro lipolysis were comparable; however, the differences were more pronounced in the flow-through method. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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18 pages, 2091 KiB

Open AccessArticle

N-(9-Acridinyl) Amino Acid Derivatives: Synthesis and In Vitro Evaluation of Anti-Toxoplasma gondii Activity

by Đorđe Zlatković, Vladimir Dobričić, Jelena Srbljanović, Olivera Lijeskić, Neda Bauman, Vladimir Ćirković and Tijana Štajner

Pharmaceutics 2025, 17(3), 374; https://doi.org/10.3390/pharmaceutics17030374 - 15 Mar 2025

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Abstract

Background/Objectives: Acridine, an aromatic heterocyclic compound, serves as a basis for the synthesis of potent bioactive derivatives, displaying a broad spectrum of biological activity, such as antibacterial, antitumor, and antiparasitic activity. With the ability to undergo various types of electrophilic substitutions, introducing [...] Read more.

Background/Objectives: Acridine, an aromatic heterocyclic compound, serves as a basis for the synthesis of potent bioactive derivatives, displaying a broad spectrum of biological activity, such as antibacterial, antitumor, and antiparasitic activity. With the ability to undergo various types of electrophilic substitutions, introducing different side chains could lead to compounds being active towards various and potentially multiple biotargets. Toxoplasma gondii, a ubiquitous protozoan parasite with worldwide distribution, poses a major health threat, particularly in immunocompromised patients and fetuses. Current treatment options for toxoplasmosis are scarce, with notable limitations, especially regarding side myelotoxicity and inactivity towards T. gondii cysts, causing a need for novel drug candidates. The aim of this study was to evaluate selected N-(9-acrydinil) amino acid derivatives as potential anti-T. gondii agents. Methods: Synthesis of new derivatives was performed using a two-step method, with the initial mixing of 9-chloroacridine with methanol and sodium alkoxide solution and subsequent adding of appropriate amino acids. Cytotoxicity of the tested compounds was evaluated on the Vero cell line using a MTT assay, while their anti-T. gondii activity was investigated using T. gondii RH strain tachyzoites. Results: CC₅₀ values of the derivatives ranged from 41.72 to 154.10 µM. Anti-T. gondii activity, displayed as a reduction in the number of viable tachyzoites compared to the untreated control, ranged from 0 to 33.3%. One of the derivatives displayed activity comparable to the standard treatment option while retaining acceptable cytotoxicity. Esterification, presence of aromatic substituents and the length of the amino acid side chain were identified as key factors that affect both toxicity and activity of these derivatives. Conclusions: Promising results obtained throughout this study provide guidelines for further structural modifications of N-(9-acrydinil) amino acid derivatives in order to synthesize drug candidates competitive to standard treatment options for toxoplasmosis. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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13 pages, 2153 KiB

Open AccessArticle

Intranasal Administration of Acetaminophen-Loaded Poly(lactic-co-glycolic acid) Nanoparticles Increases Pain Threshold in Mice Rapidly Entering High Altitudes

by Qingqing Huang, Xingyue Han, Jin Li, Xilin Li, Xin Chen, Jianwen Hou, Sixun Yu, Shaobing Zhou, Gu Gong and Haifeng Shu

Pharmaceutics 2025, 17(3), 341; https://doi.org/10.3390/pharmaceutics17030341 - 6 Mar 2025

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Abstract

Background/Objectives: Orally or intravenously administered acetaminophen experiences considerable liver first-pass elimination and may cause liver/kidney damage. This work examined the pharmacological effects of acetaminophen-loaded poly(lactic-co-glycolic acid) nanoparticles (AAP PLGA NPs) intranasally administered to mice rapidly entering high altitudes. Methods: AAP PLGA [...] Read more.

Background/Objectives: Orally or intravenously administered acetaminophen experiences considerable liver first-pass elimination and may cause liver/kidney damage. This work examined the pharmacological effects of acetaminophen-loaded poly(lactic-co-glycolic acid) nanoparticles (AAP PLGA NPs) intranasally administered to mice rapidly entering high altitudes. Methods: AAP PLGA NPs were prepared using ultrasonication-assisted emulsification and solvent evaporation and characterized in terms of drug encapsulation efficiency and loading, in vitro and in vivo release behaviors, and toxicity to hippocampal neurons. In vivo fluorescence imaging was used to monitor the concentrations of AAP PLGA NPs (labeled with indocyanine green) in the brain and blood of the mice after intranasal administration. The effects of these NPs on the pain threshold in mice rapidly entering high altitudes were evaluated through hot plate and tail flick experiments. Results: The AAP PLGA NPs were found to be noncytotoxic, highly biocompatible and stable, with a drug encapsulation efficiency and loading capacity of 42.53% and 3.87%, respectively. The in vitro release of acetaminophen lasted for up to 72 h, and the release rate was ~82%. After intranasal administration in vivo, the drug release occurred slowly, and the drug was mainly concentrated in the brain. Compared with nonencapsulated acetaminophen, the intranasal administration of AAP PLGA NPs resulted in higher brain levels of the drug and delayed its elimination, thus increasing the pain threshold in mice rapidly entering high altitudes. Conclusions: The proposed strategy addresses the common problems of intranasal drug administration (low retention time and bioavailability) and paves the way for effective pain management in high-altitude environments. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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20 pages, 3591 KiB

Open AccessArticle

Novel HSA-PMEMA Nanomicelles Prepared via Site-Specific In Situ Polymerization-Induced Self-Assembly for Improved Intracellular Delivery of Paclitaxel

by Yang Chen, Shuang Liang, Binglin Chen, Fei Jiao, Xuliang Deng and Xinyu Liu

Pharmaceutics 2025, 17(3), 316; https://doi.org/10.3390/pharmaceutics17030316 - 1 Mar 2025

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Abstract

Background/Objectives: Paclitaxel (PTX) is a potent anticancer drug that is poorly soluble in water. To enhance its delivery efficiency in aqueous environments, amphiphilic polymer micelles are often used as nanocarriers for PTX in clinical settings. However, the hydrophilic polymer segments on the [...] Read more.

Background/Objectives: Paclitaxel (PTX) is a potent anticancer drug that is poorly soluble in water. To enhance its delivery efficiency in aqueous environments, amphiphilic polymer micelles are often used as nanocarriers for PTX in clinical settings. However, the hydrophilic polymer segments on the surface of these micelles may possess potential immunogenicity, posing risks in clinical applications. To address this issue, nanomicelles based on human serum albumin (HSA)–hydrophobic polymer conjugates constructed via site-specific in situ polymerization-induced self-assembly (SI-PISA) are considered a promising alternative. The HSA shell not only ensures good biocompatibility but also enhances cellular uptake because of endogenous albumin trafficking pathways. Moreover, compared to traditional methods of creating protein–hydrophobic polymer conjugates, SI-PISA demonstrates higher reaction efficiency and better preservation of protein functionality. Methods: We synthesized HSA-PMEMA nanomicelles via SI-PISA using HSA and methoxyethyl methacrylate (MEMA)—a novel hydrophobic monomer with a well-defined and stable chemical structure. The protein activity and the PTX intracellular delivery efficiency of HSA-PMEMA nanomicelles were evaluated. Results: The CD spectra of HSA and HSA-PMEMA exhibited similar shapes, and the relative esterase-like activity of HSA-PMEMA was 94% that of unmodified HSA. Flow cytometry results showed that Cy7 fluorescence intensity in cells treated with HSA-PMEMA-Cy7 was approximately 1.35 times that in cells treated with HSA-Cy7; meanwhile, HPLC results indicated that, under the same conditions, the PTX loading per unit protein mass on HSA-PMEMA was approximately 1.43 times that of HSA. These collectively contributed to a 1.78-fold overall PTX intracellular delivery efficiency of HSA-PMEMA compared to that of HSA. Conclusions: In comparison with HSA, HSA-PMEMA nanomicelles exhibit improved cellular uptake and higher loading efficiency for PTX, effectively promoting the intracellular delivery of PTX. Tremendous potential lies in these micelles for developing safer and more efficient next-generation PTX formulations for tumor treatment. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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20 pages, 1477 KiB

Open AccessArticle

Evaluating the Impact of Minimized GnRH and PGF_2α Analogues-Loaded Chitosan Nanoparticles on Ovarian Activity and Fertility of Heat-Stressed Dairy Cows

by Mohammed E. A. Omar, Eman M. Hassanein, Ahmed M. Shehabeldin, Ottó Szenci and Abdelghany A. El-Shereif

Pharmaceutics 2025, 17(2), 274; https://doi.org/10.3390/pharmaceutics17020274 - 18 Feb 2025

Cited by 1 | Viewed by 610

Abstract

Objectives: This study aimed to evaluate the effectiveness of gonadotropin-releasing hormone-loaded chitosan–TPP nanoparticles (GnRH-CNPs) and prostaglandin F_2α-loaded chitosan–TPP nanoparticles (PGF_2α-CNPs) within the Ovsynch protocol for enhancing reproductive performance in heat-stressed dairy cows. Methods: Thirty-six cyclic purebred Friesian [...] Read more.

Objectives: This study aimed to evaluate the effectiveness of gonadotropin-releasing hormone-loaded chitosan–TPP nanoparticles (GnRH-CNPs) and prostaglandin F_2α-loaded chitosan–TPP nanoparticles (PGF_2α-CNPs) within the Ovsynch protocol for enhancing reproductive performance in heat-stressed dairy cows. Methods: Thirty-six cyclic purebred Friesian cows not detected in standing heat for more than 90 days postpartum were randomly allocated to three treatment groups. The control group (OVS, n = 12) followed the standard Ovsynch protocol with conventional doses. The ½ OVS group (n = 12) received 5 µg GnRH-CNPs on days 0 and 9, along with 250 µg PGF_2α-CNPs on day 7. While the ¼ OVS group (n = 12) was administered 2.5 µg GnRH-CNPs on days 0 and 9, with 125 µg PGF_2α-CNPs on day 7. Ovarian follicular dynamics and corpus luteum (CL) development were monitored on days 0, 4, 7, and 9 of the protocol. Serum progesterone (P₄) concentrations were measured throughout the synchronization period and on days 15 and 30 post-AI. Pregnancy was diagnosed on day 30 post-AI. Results: The ¼ OVS protocol achieved a significantly greater follicular response (p < 0.05) than other protocols. On day 4, following the first GnRH administration, the OVS group exhibited a higher number of subordinate follicles (p < 0.05) and a greater diameter of the dominant follicles (DFs), whereas the ¼ OVS group showed a greater subordinate follicle diameter (p < 0.05) and a higher number of DFs. On day 9, after PGF_2α administration, the ¼ OVS group maintained an elevated number of subordinate follicles, while larger subordinate follicle diameters were observed in the ½ OVS and OVS groups. No significant differences in DF numbers and diameters were observed among groups. P₄ concentrations remained similar across groups during treatments. Compared to control, a significantly higher value of P₄ concentration (p < 0.05) was recorded on day 15 post-AI in the ½ OVS group and on day 30 post-AI in the ¼ OVS group. These findings correlated with a higher pregnancy rate in the ¼ OVS group (65%) compared to the ½ OVS and OVS groups (40% in each). Conclusions: Nanofabrication reduced GnRH and PGF_2α dosage by 50% and 75% without impairing ovarian response and pregnancy rates. The ¼ OVS protocol notably enhanced the ovarian activity and fertility, highlighting the use of GnRH-CNPs and PGF_2α-CNPs as promising and practical approaches to enhance the fertility in dairy cattle under heat stress (HS). Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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20 pages, 26605 KiB

Open AccessArticle

Sulforaphane Wrapped in Self-Assembled Nanomicelle Enhances the Effect of Sonodynamic Therapy on Glioma

by Yihong Li, Xuejie Yang, Zhen Wei, Heng Niu, Liyang Wu, Caijing Chen, Huina Liu, Ting Cai and Huadong Fan

Pharmaceutics 2025, 17(1), 34; https://doi.org/10.3390/pharmaceutics17010034 - 30 Dec 2024

Cited by 1 | Viewed by 981

Abstract

Background/Objectives: The two obstacles for treating glioma are the skull and the blood brain–barrier (BBB), the first of which forms a physical shield that increases the difficulties of traditional surgery or radiotherapy, while the latter prevents antitumor drugs reaching tumor sites. To conquer [...] Read more.

Background/Objectives: The two obstacles for treating glioma are the skull and the blood brain–barrier (BBB), the first of which forms a physical shield that increases the difficulties of traditional surgery or radiotherapy, while the latter prevents antitumor drugs reaching tumor sites. To conquer these issues, we take advantage of the high penetrating ability of sonodynamic therapy (SDT), combined with a novel nanocomplex that can easily pass the BBB. Methods: Through ultrasonic polymerization, the amphiphilic peptides (C₁₈GR₇RGDS) were self-assembled as a spherical shell encapsulating a sonosensitizer Rose Bengal (RB) and a plant-derived compound, sulforaphane (SFN), to form the nanocomplex SFN@RB@SPM. Results/Conclusions: SFN@RB@SPM can be internalized by the glioma cells through the tumor-targeting motif RGDS (abbreviated for the peptide sequence composed of arginine, glycine, aspartic acid, and serine), and further executes antitumor function during SDT. Also, SFN@RB@SPM could be easily taken up by U87-MG cells and cross the BBB in glioma-bearing mice during SDT. The mechanism investigation revealed that, compared with the SFN-free nanocomplex (RB@SPM), SFN@RB@SPM induced much more apoptosis of U87-MG cells in an ROS-dependent manner through the depletion of glutathione by SFN and the cavitation effect by SDT. In animal experiments, besides a significant reduction in tumor volume and a delay in losing body weight, H&E staining showed a massive infiltration of neutrophils adjacent to the tumor sites, indicating this novel nanocomplex SFN@RB@SPM can synergistically augment SDT efficacy, partially by enhancing the antitumor function of innate immunity. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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11 pages, 5136 KiB

Open AccessArticle

A Human Feedback Strategy for Photoresponsive Molecules in Drug Delivery: Utilizing GPT-2 and Time-Dependent Density Functional Theory Calculations

by Junjie Hu, Peng Wu, Shiyi Wang, Binju Wang and Guang Yang

Pharmaceutics 2024, 16(8), 1014; https://doi.org/10.3390/pharmaceutics16081014 - 31 Jul 2024

Cited by 1 | Viewed by 1388

Abstract

Photoresponsive drug delivery stands as a pivotal frontier in smart drug administration, leveraging the non-invasive, stable, and finely tunable nature of light-triggered methodologies. The generative pre-trained transformer (GPT) has been employed to generate molecular structures. In our study, we harnessed GPT-2 on the [...] Read more.

Photoresponsive drug delivery stands as a pivotal frontier in smart drug administration, leveraging the non-invasive, stable, and finely tunable nature of light-triggered methodologies. The generative pre-trained transformer (GPT) has been employed to generate molecular structures. In our study, we harnessed GPT-2 on the QM7b dataset to refine a UV-GPT model with adapters, enabling the generation of molecules responsive to UV light excitation. Utilizing the Coulomb matrix as a molecular descriptor, we predicted the excitation wavelengths of these molecules. Furthermore, we validated the excited state properties through quantum chemical simulations. Based on the results of these calculations, we summarized some tips for chemical structures and integrated them into the alignment of large-scale language models within the reinforcement learning from human feedback (RLHF) framework. The synergy of these findings underscores the successful application of GPT technology in this critical domain. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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20 pages, 7014 KiB

Open AccessEditor’s ChoiceArticle

Amorphous Polymer–Phospholipid Solid Dispersions for the Co-Delivery of Curcumin and Piperine Prepared via Hot-Melt Extrusion

by Kamil Wdowiak, Andrzej Miklaszewski and Judyta Cielecka-Piontek

Pharmaceutics 2024, 16(8), 999; https://doi.org/10.3390/pharmaceutics16080999 - 28 Jul 2024

Viewed by 2034

Abstract

Curcumin and piperine are plant compounds known for their health-promoting properties, but their use in the prevention or treatment of various diseases is limited by their poor solubility. To overcome this drawback, the curcumin–piperine amorphous polymer–phospholipid dispersions were prepared by hot melt extrusion [...] Read more.

Curcumin and piperine are plant compounds known for their health-promoting properties, but their use in the prevention or treatment of various diseases is limited by their poor solubility. To overcome this drawback, the curcumin–piperine amorphous polymer–phospholipid dispersions were prepared by hot melt extrusion technology. X-ray powder diffraction indicated the formation of amorphous systems. Differential scanning calorimetry confirmed amorphization and provided information on the good miscibility of the active compound–polymer–phospholipid dispersions. Owing to Fourier-transform infrared spectroscopy, the intermolecular interactions in systems were investigated. In the biopharmaceutical properties assessment, the improvement in solubility as well as the maintenance of the supersaturation state were confirmed. Moreover, PAMPA models simulating the gastrointestinal tract and blood-brain barrier showed enhanced permeability of active compounds presented in dispersions compared to the crystalline form of individual compounds. The presented paper suggests that polymer–phospholipid dispersions advantageously impact the bioaccessibility of poorly soluble active compounds. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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16 pages, 1319 KiB

Open AccessArticle

Prediction of Protein Targets in Ovarian Cancer Using a Ru-Complex and Carbon Dot Drug Delivery Therapeutic Nanosystems: A Bioinformatics and µ-FTIR Spectroscopy Approach

by Maja D. Nešić, Tanja Dučić, Branislava Gemović, Milan Senćanski, Manuel Algarra, Mara Gonçalves, Milutin Stepić, Iva A. Popović, Đorđe Kapuran and Marijana Petković

Pharmaceutics 2024, 16(8), 997; https://doi.org/10.3390/pharmaceutics16080997 - 27 Jul 2024

Cited by 1 | Viewed by 1553

Abstract

We predicted the protein therapeutic targets specific to a Ru-based potential drug and its combination with pristine and N-doped carbon dot drug delivery systems, denoted as RuCN/CDs and RuCN/N-CDs. Synchrotron-based FTIR microspectroscopy (µFTIR) in addition to bioinformatics data on drug structures and protein [...] Read more.

We predicted the protein therapeutic targets specific to a Ru-based potential drug and its combination with pristine and N-doped carbon dot drug delivery systems, denoted as RuCN/CDs and RuCN/N-CDs. Synchrotron-based FTIR microspectroscopy (µFTIR) in addition to bioinformatics data on drug structures and protein sequences were applied to assess changes in the protein secondary structure of A2780 cancer cells. µFTIR revealed the moieties of the target proteins’ secondary structure changes only after the treatment with RuCN and RuCN/N-CDs. A higher content of α-helices and a lower content of β-sheets appeared in A2780 cells after RuCN treatment. Treatment with RuCN/N-CDs caused a substantial increase in parallel β-sheet numbers, random coil content, and tyrosine residue numbers. The results obtained suggest that the mitochondrion-related proteins NDUFA1 and NDUFB5 are affected by RuCN either via overexpression or stabilisation of helical structures. RuCN/N-CDs either induce overexpression of the β-sheet-rich protein NDUFS1 and affect its random coil structure or interact and stabilise its structure via hydrogen bonding between -NH2 groups from N-CDs with protein C=O groups and –OH groups of serine, threonine, and tyrosine residues. The N-CD nanocarrier tunes this drug’s action by directing it toward a specific protein target, changing this drug’s coordination ability and inducing changes in the protein’s secondary structures and function. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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Review

Jump to: Research

32 pages, 3475 KiB

Open AccessReview

Revolutionizing Drug Delivery: The Impact of Advanced Materials Science and Technology on Precision Medicine

by Mohamed El-Tanani, Shakta Mani Satyam, Syed Arman Rabbani, Yahia El-Tanani, Alaa A. A. Aljabali, Ibrahim Al Faouri and Abdul Rehman

Pharmaceutics 2025, 17(3), 375; https://doi.org/10.3390/pharmaceutics17030375 - 15 Mar 2025

Cited by 1 | Viewed by 1163

Abstract

Recent progress in material science has led to the development of new drug delivery systems that go beyond the conventional approaches and offer greater accuracy and convenience in the application of therapeutic agents. This review discusses the evolutionary role of nanocarriers, hydrogels, and [...] Read more.

Recent progress in material science has led to the development of new drug delivery systems that go beyond the conventional approaches and offer greater accuracy and convenience in the application of therapeutic agents. This review discusses the evolutionary role of nanocarriers, hydrogels, and bioresponsive polymers that offer enhanced drug release, target accuracy, and bioavailability. Oncology, chronic disease management, and vaccine delivery are some of the applications explored in this paper to show how these materials improve the therapeutic results, counteract multidrug resistance, and allow for sustained and localized treatments. The review also discusses the translational barriers of bringing advanced materials into the clinical setting, which include issues of biocompatibility, scalability, and regulatory approval. Methods to overcome these challenges include surface modifications to reduce immunogenicity, scalable production methods such as microfluidics, and the harmonization of regulatory systems. In addition, the convergence of artificial intelligence (AI) and machine learning (ML) is opening new frontiers in material science and personalized medicine. These technologies allow for predictive modeling and real-time adjustments to optimize drug delivery to the needs of individual patients. The use of advanced materials can also be applied to rare and underserved diseases; thus, new strategies in gene therapy, orphan drugs development, and global vaccine distribution may offer new hopes for millions of patients. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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27 pages, 3136 KiB

Open AccessReview

An Overview on the Role of Ionic Liquids and Deep Eutectic Solvents in Oral Pharmaceuticals

by Stefano Sangiorgi, Beatrice Albertini, Serena Bertoni and Nadia Passerini

Pharmaceutics 2025, 17(3), 300; https://doi.org/10.3390/pharmaceutics17030300 - 25 Feb 2025

Viewed by 565

Abstract

Over the past twenty years, ionic liquids (ILs) and deep eutectic solvents (DESs) have gained recognition across various fields, including catalysis, extraction and purification, materials science, and biotechnology. Notably, the use of ILs and DESs in pharmaceutical research, especially in drug delivery, has [...] Read more.

Over the past twenty years, ionic liquids (ILs) and deep eutectic solvents (DESs) have gained recognition across various fields, including catalysis, extraction and purification, materials science, and biotechnology. Notably, the use of ILs and DESs in pharmaceutical research, especially in drug delivery, has seen remarkable expansion over the past decade. This review offers a comprehensive analysis of ILs and DESs specifically designed for the oral administration of drugs having unfavorable biopharmaceutical properties. The classification and characteristics of ILs and DESs, along with their newer natural (Bio-ILs and NaDESs) and therapeutic subcategories (API-ILs and TheDESs) are outlined. Additionally, a further subgroup of ILs, known as surface active ionic liquids (SAILs), is described. Then, a detailed examination of the available manufacturing methods in a sustainable, time-consuming, and scalable perspective, and toxicity concerns in relation to their subdivision are evaluated. Finally, their specific applications in oral drug delivery, whether used as neat solvents or converted into administrable dosage forms, are analyzed and discussed. Despite the significant advancements in recent years regarding the use of these solvents in oral drug delivery, there are still many aspects that need further investigation. These include their interaction with biological systems (gastrointestinal fluids and mucosa), their long-term stability, and the development of effective drug delivery systems. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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28 pages, 1342 KiB

Open AccessReview

Advances in Materials Science for Precision Melanoma Therapy: Nanotechnology-Enhanced Drug Delivery Systems

by Sivakumar S. Moni, Jobran M. Moshi, Sabine Matou-Nasri, Shmoukh Alotaibi, Yousef M. Hawsawi, Mohamed Eltaib Elmobark, Ahlam Mohammed S. Hakami, Mohammed A. Jeraiby, Ahmed A. Sulayli and Hassan N. Moafa

Pharmaceutics 2025, 17(3), 296; https://doi.org/10.3390/pharmaceutics17030296 - 24 Feb 2025

Viewed by 759

Abstract

Melanoma, a highly aggressive form of skin cancer, poses a major therapeutic challenge due to its metastatic potential, resistance to conventional therapies, and the complexity of the tumor microenvironment (TME). Materials science and nanotechnology advances have led to using nanocarriers such as liposomes, [...] Read more.

Melanoma, a highly aggressive form of skin cancer, poses a major therapeutic challenge due to its metastatic potential, resistance to conventional therapies, and the complexity of the tumor microenvironment (TME). Materials science and nanotechnology advances have led to using nanocarriers such as liposomes, dendrimers, polymeric nanoparticles, and metallic nanoparticles as transformative solutions for precision melanoma therapy. This review summarizes findings from Web of Science, PubMed, EMBASE, Scopus, and Google Scholar and highlights the role of nanotechnology in overcoming melanoma treatment barriers. Nanoparticles facilitate passive and active targeting through mechanisms such as the enhanced permeability and retention (EPR) effect and functionalization with tumor-specific ligands, thereby improving the accuracy of drug delivery and reducing systemic toxicity. Stimuli-responsive systems and multi-stage targeting further improve therapeutic precision and overcome challenges such as poor tumor penetration and drug resistance. Emerging therapeutic platforms combine diagnostic imaging with therapeutic delivery, paving the way for personalized medicine. However, there are still issues with scalability, biocompatibility, and regulatory compliance. This comprehensive review highlights the potential of integrating nanotechnology with advances in genetics and proteomics, scalable, and patient-specific therapies. These interdisciplinary innovations promise to redefine the treatment of melanoma and provide safer, more effective, and more accessible treatments. Continued research is essential to bridge the gap between evidence-based scientific advances and clinical applications. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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51 pages, 3047 KiB

Open AccessEditor’s ChoiceReview

The Impact of COVID-19 on RNA Therapeutics: A Surge in Lipid Nanoparticles and Alternative Delivery Systems

by Nargish Parvin, Tapas K. Mandal and Sang-Woo Joo

Pharmaceutics 2024, 16(11), 1366; https://doi.org/10.3390/pharmaceutics16111366 - 25 Oct 2024

Cited by 1 | Viewed by 2359

Abstract

The COVID-19 pandemic has significantly accelerated progress in RNA-based therapeutics, particularly through the successful development and global rollout of mRNA vaccines. This review delves into the transformative impact of the pandemic on RNA therapeutics, with a strong focus on lipid nanoparticles (LNPs) as [...] Read more.

The COVID-19 pandemic has significantly accelerated progress in RNA-based therapeutics, particularly through the successful development and global rollout of mRNA vaccines. This review delves into the transformative impact of the pandemic on RNA therapeutics, with a strong focus on lipid nanoparticles (LNPs) as a pivotal delivery platform. LNPs have proven to be critical in enhancing the stability, bioavailability, and targeted delivery of mRNA, facilitating the unprecedented success of vaccines like those developed by Pfizer-BioNTech and Moderna. Beyond vaccines, LNP technology is being explored for broader therapeutic applications, including treatments for cancer, rare genetic disorders, and infectious diseases. This review also discusses emerging RNA delivery systems, such as polymeric nanoparticles and viral vectors, which offer alternative strategies to overcome existing challenges related to stability, immune responses, and tissue-specific targeting. Additionally, we examine the pandemic’s influence on regulatory processes, including the fast-tracked approvals for RNA therapies, and the surge in research funding that has spurred further innovation in the field. Public acceptance of RNA-based treatments has also grown, laying the groundwork for future developments in personalized medicine. By providing an in-depth analysis of these advancements, this review highlights the long-term impact of COVID-19 on the evolution of RNA therapeutics and the future of precision drug delivery technologies. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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22 pages, 6892 KiB

Open AccessEditor’s ChoiceReview

Review on Photoacoustic Monitoring after Drug Delivery: From Label-Free Biomarkers to Pharmacokinetics Agents

by Jiwoong Kim, Seongwook Choi, Chulhong Kim, Jeesu Kim and Byullee Park

Pharmaceutics 2024, 16(10), 1240; https://doi.org/10.3390/pharmaceutics16101240 - 24 Sep 2024

Cited by 2 | Viewed by 1353

Abstract

Photoacoustic imaging (PAI) is an emerging noninvasive and label-free method for capturing the vasculature, hemodynamics, and physiological responses following drug delivery. PAI combines the advantages of optical and acoustic imaging to provide high-resolution images with multiparametric information. In recent decades, PAI’s abilities have [...] Read more.

Photoacoustic imaging (PAI) is an emerging noninvasive and label-free method for capturing the vasculature, hemodynamics, and physiological responses following drug delivery. PAI combines the advantages of optical and acoustic imaging to provide high-resolution images with multiparametric information. In recent decades, PAI’s abilities have been used to determine reactivity after the administration of various drugs. This study investigates photoacoustic imaging as a label-free method of monitoring drug delivery responses by observing changes in the vascular system and oxygen saturation levels across various biological tissues. In addition, we discuss photoacoustic studies that monitor the biodistribution and pharmacokinetics of exogenous contrast agents, offering contrast-enhanced imaging of diseased regions. Finally, we demonstrate the crucial role of photoacoustic imaging in understanding drug delivery mechanisms and treatment processes. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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37 pages, 6387 KiB

Open AccessReview

Drug-Loaded Bioscaffolds for Osteochondral Regeneration

by Yifan Tong, Jiaqi Yuan, Zhenguang Li, Cuijun Deng and Yu Cheng

Pharmaceutics 2024, 16(8), 1095; https://doi.org/10.3390/pharmaceutics16081095 - 21 Aug 2024

Cited by 1 | Viewed by 2211

Abstract

Osteochondral defect is a complex tissue loss disease caused by arthritis, high-energy trauma, and many other reasons. Due to the unique structural characteristics of osteochondral tissue, the repair process is sophisticated and involves the regeneration of both hyaline cartilage and subchondral bone. However, [...] Read more.

Osteochondral defect is a complex tissue loss disease caused by arthritis, high-energy trauma, and many other reasons. Due to the unique structural characteristics of osteochondral tissue, the repair process is sophisticated and involves the regeneration of both hyaline cartilage and subchondral bone. However, the current clinical treatments often fall short of achieving the desired outcomes. Tissue engineering bioscaffolds, especially those created via three-dimensional (3D) printing, offer promising solutions for osteochondral defects due to their precisely controllable 3D structures. The microstructure of 3D-printed bioscaffolds provides an excellent physical environment for cell adhesion and proliferation, as well as nutrient transport. Traditional 3D-printed bioscaffolds offer mere physical stimulation, while drug-loaded 3D bioscaffolds accelerate the tissue repair process by synergistically combining drug therapy with physical stimulation. In this review, the physiological characteristics of osteochondral tissue and current treatments of osteochondral defect were reviewed. Subsequently, the latest progress in drug-loaded bioscaffolds was discussed and highlighted in terms of classification, characteristics, and applications. The perspectives of scaffold design, drug control release, and biosafety were also discussed. We hope this article will serve as a valuable reference for the design and development of osteochondral regenerative bioscaffolds and pave the way for the use of drug-loaded bioscaffolds in clinical therapy. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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42 pages, 4178 KiB

Open AccessReview

Recent Review on Biological Barriers and Host–Material Interfaces in Precision Drug Delivery: Advancement in Biomaterial Engineering for Better Treatment Therapies

by Rohitas Deshmukh, Pranshul Sethi, Bhupendra Singh, Jailani Shiekmydeen, Sagar Salave, Ravish J. Patel, Nemat Ali, Summya Rashid, Gehan M. Elossaily and Arun Kumar

Pharmaceutics 2024, 16(8), 1076; https://doi.org/10.3390/pharmaceutics16081076 - 16 Aug 2024

Cited by 12 | Viewed by 2597

Abstract

Preclinical and clinical studies have demonstrated that precision therapy has a broad variety of treatment applications, making it an interesting research topic with exciting potential in numerous sectors. However, major obstacles, such as inefficient and unsafe delivery systems and severe side effects, have [...] Read more.

Preclinical and clinical studies have demonstrated that precision therapy has a broad variety of treatment applications, making it an interesting research topic with exciting potential in numerous sectors. However, major obstacles, such as inefficient and unsafe delivery systems and severe side effects, have impeded the widespread use of precision medicine. The purpose of drug delivery systems (DDSs) is to regulate the time and place of drug release and action. They aid in enhancing the equilibrium between medicinal efficacy on target and hazardous side effects off target. One promising approach is biomaterial-assisted biotherapy, which takes advantage of biomaterials’ special capabilities, such as high biocompatibility and bioactive characteristics. When administered via different routes, drug molecules deal with biological barriers; DDSs help them overcome these hurdles. With their adaptable features and ample packing capacity, biomaterial-based delivery systems allow for the targeted, localised, and prolonged release of medications. Additionally, they are being investigated more and more for the purpose of controlling the interface between the host tissue and implanted biomedical materials. This review discusses innovative nanoparticle designs for precision and non-personalised applications to improve precision therapies. We prioritised nanoparticle design trends that address heterogeneous delivery barriers, because we believe intelligent nanoparticle design can improve patient outcomes by enabling precision designs and improving general delivery efficacy. We additionally reviewed the most recent literature on biomaterials used in biotherapy and vaccine development, covering drug delivery, stem cell therapy, gene therapy, and other similar fields; we have also addressed the difficulties and future potential of biomaterial-assisted biotherapies. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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16 pages, 3690 KiB

Open AccessReview

Revitalizing Bacillus Calmette–Guérin Immunotherapy for Bladder Cancer: Nanotechnology and Bioengineering Approaches

by Maoxin Lv, Shihao Shang, Kepu Liu, Yuliang Wang, Peng Xu, Hao Song, Jie Zhang, Zelong Sun, Yuhao Yan, Zheng Zhu, Hao Wu and Hao Li

Pharmaceutics 2024, 16(8), 1067; https://doi.org/10.3390/pharmaceutics16081067 - 15 Aug 2024

Cited by 1 | Viewed by 2246

Abstract

Bacillus Calmette–Guérin (BCG) immunotherapy has been a cornerstone treatment for non-muscle-invasive bladder cancer for decades and still faces challenges, such as severe immune adverse reactions, which reduce its use as a first-line treatment. This review examines BCG therapy’s history, mechanisms, and current status, [...] Read more.

Bacillus Calmette–Guérin (BCG) immunotherapy has been a cornerstone treatment for non-muscle-invasive bladder cancer for decades and still faces challenges, such as severe immune adverse reactions, which reduce its use as a first-line treatment. This review examines BCG therapy’s history, mechanisms, and current status, highlighting how nanotechnology and bioengineering are revitalizing its application. We discuss novel nanocarrier systems aimed at enhancing BCG’s efficacy while mitigating specific side effects. These approaches promise improved tumor targeting, better drug loading, and an enhanced stimulation of anti-tumor immune responses. Key strategies involve using materials such as liposomes, polymers, and magnetic particles to encapsulate BCG or functional BCG cell wall components. Additionally, co-delivering BCG with chemotherapeutics enhances drug targeting and tumor-killing effects while reducing drug toxicity, with some studies even achieving synergistic effects. While most studies remain experimental, this research direction offers hope for overcoming BCG’s limitations and advancing bladder cancer immunotherapy. Further elucidation of BCG’s mechanisms and rigorous safety evaluations of new delivery systems will be crucial for translating these innovations into clinical practice. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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15 pages, 1621 KiB

Open AccessReview

Application of Scaffold-Based Drug Delivery in Oral Cancer Treatment: A Novel Approach

by Elham Saberian, Andrej Jenča, Adriána Petrášová, Hadi Zare-Zardini and Meysam Ebrahimifar

Pharmaceutics 2024, 16(6), 802; https://doi.org/10.3390/pharmaceutics16060802 - 14 Jun 2024

Cited by 10 | Viewed by 2884

Abstract

This comprehensive review consolidates insights from two sources to emphasize the transformative impact of scaffold-based drug delivery systems in revolutionizing oral cancer therapy. By focusing on their core abilities to facilitate targeted and localized drug administration, these systems enhance therapeutic outcomes significantly. Scaffolds, [...] Read more.

This comprehensive review consolidates insights from two sources to emphasize the transformative impact of scaffold-based drug delivery systems in revolutionizing oral cancer therapy. By focusing on their core abilities to facilitate targeted and localized drug administration, these systems enhance therapeutic outcomes significantly. Scaffolds, notably those coated with anti-cancer agents such as cisplatin and paclitaxel, have proven effective in inhibiting oral cancer cell proliferation, establishing a promising avenue for site-specific drug delivery. The application of synthetic scaffolds, including Poly Ethylene Glycol (PEG) and poly(lactic-co-glycolic acid) (PLGA), and natural materials, like collagen or silk, in 3D systems has been pivotal for controlled release of therapeutic agents, executing diverse anti-cancer strategies. A key advancement in this field is the advent of smart scaffolds designed for sequential cancer therapy, which strive to refine drug delivery systems, minimizing surgical interventions, accentuating the significance of 3D scaffolds in oral cancer management. These systems, encompassing local drug-coated scaffolds and other scaffold-based platforms, hold the potential to transform oral cancer treatment through precise interventions, yielding improved patient outcomes. Local drug delivery via scaffolds can mitigate systemic side effects typically associated with chemotherapy, such as nausea, alopecia, infections, and gastrointestinal issues. Post-drug release, scaffolds foster a conducive environment for non-cancerous cell growth, adhering and proliferation, demonstrating restorative potential. Strategies for controlled and targeted drug delivery in oral cancer therapy span injectable self-assembling peptide hydrogels, nanocarriers, and dual drug-loaded nanofibrous scaffolds. These systems ensure prolonged release, synergistic effects, and tunable targeting, enhancing drug delivery efficiency while reducing systemic exposure. Smart scaffolds, capable of sequential drug release, transitioning to cell-friendly surfaces, and enabling combinatorial therapy, hold the promise to revolutionize treatment by delivering precise interventions and optimized outcomes. In essence, scaffold-based drug delivery systems, through their varied forms and functionalities, are reshaping oral cancer therapy. They target drug delivery efficiency, diminish side effects, and present avenues for personalization. Challenges like fabrication intricacy, biocompatibility, and scalability call for additional research. Nonetheless, the perspective on scaffold-based systems in oral cancer treatment is optimistic, as ongoing advancements aim to surmount current limitations and fully leverage their potential in cancer therapy. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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18 pages, 809 KiB

Open AccessEditor’s ChoiceReview

The Integration of Advanced Drug Delivery Systems into Conventional Adjuvant Therapies for Peri-Implantitis Treatment

by Iria Seoane-Viaño, Mariola Seoane-Gigirey, Carlos Bendicho-Lavilla, Luz M. Gigirey, Francisco J. Otero-Espinar and Santiago Seoane-Trigo

Pharmaceutics 2024, 16(6), 769; https://doi.org/10.3390/pharmaceutics16060769 - 5 Jun 2024

Viewed by 2331

Abstract

Despite the high success rates of dental implants, peri-implantitis is currently the most common complication in dental implantology. Peri-implantitis has an inflammatory nature, it is associated with the accumulation of plaque in the peri-implant tissues, and its evolution can be progressive depending on [...] Read more.

Despite the high success rates of dental implants, peri-implantitis is currently the most common complication in dental implantology. Peri-implantitis has an inflammatory nature, it is associated with the accumulation of plaque in the peri-implant tissues, and its evolution can be progressive depending on various factors, comorbidities, and poor oral health. Prophylaxis and different treatment methods have been widely discussed in recent decades, and surgical and non-surgical techniques present both advantages and disadvantages. In this work, a literature review of different studies on the application of adjuvant treatments, such as local and systemic antibiotics and antiseptic treatments, was conducted. Positive outcomes have been found in the short (up to one year after treatment) and long term (up to ten years after treatment) with combined therapies. However, there is still a need to explore new therapies based on the use of advanced drug delivery systems for the effective treatment of peri-implantitis in the long term and without relapses. Hence, micro- and nanoparticles, implants, and injectable hydrogels, among others, should be considered in future peri-implantitis treatment with the aim of enhancing overall therapy outcomes. Full article

(This article belongs to the Special Issue Advanced Materials Science and Technology in Drug Delivery)

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