Nanoparticles for Local Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: 31 December 2024 | Viewed by 11194

Special Issue Editors


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Guest Editor
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia
Interests: nanoplatforms for brain and skin delivery; innovative biocompatible excipients; poorly water-soluble drugs; physicochemical/in vitro/in silico characterization methods; in vivo pharmacokinetics in rats
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Guest Editor
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia
Interests: lipid nanosystems for localized drug delivery (brain, skin); formulation development; physicochemical characterization methods; in vitro drug permeation through biological barriers (blood–brain barrier, skin); in vivo (dermo) pharmacokinetics

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Guest Editor
Faculty of Technology in Leskovac, University of Niš, Bulevar Oslobodjenja 124, 16000 Leskovac, Serbia
Interests: lipid nanosystems; experimental design; brain targeting; in vivo pharmacokinetics; skin delivery; skin bioengineering techniques; safety and efficacy testing

Special Issue Information

Dear Colleagues,

Despite increasing advances in the design and development of modern drug delivery systems and technologies, the effective treatment of many diseases/disorders such as cancer, neurodegenerative and neuromuscular disorders, inflammatory diseases and infections (to name a few) still remains a major challenge due to the presence of restrictive biological barriers (such as the mucosal epithelium in the intestine, lungs, nose and mouth, skin, blood–brain barrier, blood–retinal barrier). To deliver a sufficient therapeutic concentration of a drug at the intended site of action (diseased organ/tissue/target cells) in a predictable/controlled manner, thereby avoiding/reducing off-site toxicity and systemic adverse effects, local drug delivery strategies have been established as a promising approach. Recently, significant progress has been made in the field of local drug delivery, achieved either through local or systemic administration (targeted/triggered approach), largely due to the implementation of nanoparticles. Although diverse types of nanoparticles (lipid-based, polymeric, metallic, carbon nanotubes, dendrimers, etc.) have been developed for local/targeted/triggered delivery of various therapeutics (anticancer drugs, central nervous system drugs, anti-inflammatory drugs, antimicrobial agents, hormones, nucleic acids, etc.) via different routes of administration (e.g., intratumoral, intra-articular, (intra)nasal, (intra)ocular, (trans)dermal, (intra)oral, oromucosal, sublingual, dental, pulmonary/inhalation, vaginal/uterine, etc.), additional efforts are required to optimize drug incorporation and release, formulation stability and shelf-life, biocompatibility, safety, biodistribution and targeting, giving this topic permanent and growing interest.

We warmly invite researchers to share their ideas, insights and perspectives from the dynamic landscape of nanoparticles for local drug delivery, covering a wide range of topics related to the following areas, among others: formulation and optimization of drug-containing nanoparticles, passive/active targeting and triggering approaches for site-specific or site-avoidance drug delivery, controlled release mechanisms and kinetics, in vitro/in vivo fate and interactions with the biological environment, biocompatibility and safety assessments, clinical applications and translational research.

Prof. Dr. Snezana Savic
Dr. Tanja Ilić
Dr. Sanela Savic
Guest Editors

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Keywords

  • lipid nanoparticles
  • polymeric nanoparticles
  • inorganic nanoparticles
  • localized administration routes
  • targeted/triggered drug delivery
  • critical quality attributes
  • biocompatibility
  • clinical application and translation

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Published Papers (5 papers)

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Research

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14 pages, 6702 KiB  
Article
Antimicrobial Peptide Octoprohibitin-Encapsulated Chitosan Nanoparticles Enhanced Antibacterial Activity against Acinetobacter baumannii
by E. H. T. Thulshan Jayathilaka, Jinwook Han, Mahanama De Zoysa and Ilson Whang
Pharmaceutics 2024, 16(10), 1245; https://doi.org/10.3390/pharmaceutics16101245 - 25 Sep 2024
Viewed by 545
Abstract
Background: This study focused on evaluating the physiochemical characteristics and antibacterial activity of Octoprohibitin-encapsulated CNPs (Octoprohibitin-CNPs) against Acinetobacter baumannii. Methods: Octoprohibitin was encapsulated into CNPs via ionotropic gelation with carboxymethyl chitosan (CMC) and low molecular weight chitosan (CS). Octoprohibitin-CNPs were dispersed in [...] Read more.
Background: This study focused on evaluating the physiochemical characteristics and antibacterial activity of Octoprohibitin-encapsulated CNPs (Octoprohibitin-CNPs) against Acinetobacter baumannii. Methods: Octoprohibitin was encapsulated into CNPs via ionotropic gelation with carboxymethyl chitosan (CMC) and low molecular weight chitosan (CS). Octoprohibitin-CNPs were dispersed in phosphate-buffered saline and the release kinetic profile was determined. Then Octoprohibitin-CNPs were examined using field-emission transmission electron microscopy and physicochemical characterization was performed. Antibacterial activity of Octoprohibitin-CNPs against A. baumannii was evaluated. Biofilm inhibition and eradication assays were performed using the crystal violet (CV) staining-based method for biofilm quantification. Results: The average diameter, zeta potential, encapsulation efficiency, and loading capacity of Octoprohibitin-CNPs were 244.5 ± 21.97 nm, +48.57 ± 0.38 mV, and 85.7% and 34.2%, respectively. TEM analysis imaging revealed that Octoprohibitin-CNPs are irregularly shaped, with fewer aggregates than CNPs. Octoprohibitin-CNPs exhibited a biphasic release pattern, characterized by an initial rapid phase followed by a sustained release over time, extending up to 93.68 ± 6.48% total release until 96 h. In vitro, Octoprohibitin-CNPs showed lower cytotoxicity compared to Octoprohibitin alone. Time-kill kinetic and bacterial viability reduction assays showed Octoprohibitin-CNPs exhibited slightly higher antibacterial activity against A. baumannii than Octoprohibitin. Conclusions: Octoprohibitin-CNP-treated A. baumannii exhibited higher levels of morphological deviation, increased membrane permeability, and the production of reactive oxygen species, as well as antibiofilm activity with greater biofilm inhibition and eradication than Octoprohibitin. These findings show that Octoprohibitin-CNPs perform better against A. baumannii compared to Octoprohibitin alone. Full article
(This article belongs to the Special Issue Nanoparticles for Local Drug Delivery)
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25 pages, 41882 KiB  
Article
Chitosan Alginate Nanoparticles of Protein Hydrolysate from Acheta domesticus with Enhanced Stability for Skin Delivery
by Kankanit Yeerong, Panuwan Chantawannakul, Songyot Anuchapreeda, Saranya Juntrapirom, Watchara Kanjanakawinkul, Anette Müllertz, Thomas Rades and Wantida Chaiyana
Pharmaceutics 2024, 16(6), 724; https://doi.org/10.3390/pharmaceutics16060724 - 28 May 2024
Cited by 1 | Viewed by 1153
Abstract
This study aimed to develop chitosan alginate nanoparticles (CANPs) for enhanced stability for dermal delivery of protein hydrolysate from Acheta domesticus (PH). CANPs, developed using ionotropic pre-gelation followed by the polyelectrolyte complex technique, were characterized for particle size, polydispersity index (PDI), and zeta [...] Read more.
This study aimed to develop chitosan alginate nanoparticles (CANPs) for enhanced stability for dermal delivery of protein hydrolysate from Acheta domesticus (PH). CANPs, developed using ionotropic pre-gelation followed by the polyelectrolyte complex technique, were characterized for particle size, polydispersity index (PDI), and zeta potential. After the incorporation of PH into CANPs, a comprehensive assessment included encapsulation efficiency, loading capacity, morphology, chemical analyses, physical and chemical stability, irritation potential, release profile, skin permeation, and skin retention. The most optimal CANPs, comprising 0.6 mg/mL sodium alginate, 1.8 mg/mL calcium chloride, and 0.1 mg/mL chitosan, exhibited the smallest particle size (309 ± 0 nm), the narrowest PDI (0.39 ± 0.01), and pronounced negative zeta potential (−26.0 ± 0.9 mV), along with an encapsulation efficiency of 56 ± 2%, loading capacity of 2.4 ± 0.1%, release of 40 ± 2% after 48 h, and the highest skin retention of 12 ± 1%. The CANPs induced no irritation and effectively enhanced the stability of PH from 44 ± 5% of PH remaining in a solution to 74 ± 4% after three-month storage. Therefore, the findings revealed the considerable potential of CANPs in improving PH stability and skin delivery, with promising applications in cosmetics and related fields. Full article
(This article belongs to the Special Issue Nanoparticles for Local Drug Delivery)
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27 pages, 4694 KiB  
Article
Thermosensitive Polymeric Nanoparticles for Drug Co-Encapsulation and Breast Cancer Treatment
by Vanessa Franco Carvalho Dartora, Julia S. Passos, Leticia V. Costa-Lotufo, Luciana B. Lopes and Alyssa Panitch
Pharmaceutics 2024, 16(2), 231; https://doi.org/10.3390/pharmaceutics16020231 - 5 Feb 2024
Cited by 1 | Viewed by 1918
Abstract
Despite advances in breast cancer treatment, there remains a need for local management of noninvasive, low-grade ductal carcinoma in situ (DCIS). These focal lesions are well suited for local intraductal treatment. Intraductal administration supported target site drug retention, improved efficacy, and reduced systemic [...] Read more.
Despite advances in breast cancer treatment, there remains a need for local management of noninvasive, low-grade ductal carcinoma in situ (DCIS). These focal lesions are well suited for local intraductal treatment. Intraductal administration supported target site drug retention, improved efficacy, and reduced systemic exposure. Here, we used a poly(N-isopropyl acrylamide, pNIPAM) nanoparticle delivery system loaded with cytotoxic piplartine and an MAPKAP Kinase 2 inhibitor (YARA) for this purpose. For tumor environment targeting, a collagen-binding peptide SILY (RRANAALKAGELYKSILYGSG-hydrazide) was attached to pNIPAM nanoparticles, and the nanoparticle diameter, zeta potential, drug loading, and release were assessed. The system was evaluated for cytotoxicity in a 2D cell culture and 3D spheroids. In vivo efficacy was evaluated using a chemical carcinogenesis model in female Sprague–Dawley rats. Nanoparticle delivery significantly reduced the IC50 of piplartine (4.9 times) compared to the drug in solution. The combination of piplartine and YARA in nanoparticles further reduced the piplartine IC50 (~15 times). Treatment with these nanoparticles decreased the in vivo tumor incidence (5.2 times). Notably, the concentration of piplartine in mammary glands treated with nanoparticles (35.3 ± 22.4 μg/mL) was substantially higher than in plasma (0.7 ± 0.05 μg/mL), demonstrating targeted drug retention. These results indicate that our nanocarrier system effectively reduced tumor development with low systemic exposure. Full article
(This article belongs to the Special Issue Nanoparticles for Local Drug Delivery)
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Review

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47 pages, 3150 KiB  
Review
Progress in Topical and Transdermal Drug Delivery Research—Focus on Nanoformulations
by Dominique Lunter, Victoria Klang, Adina Eichner, Sanela M. Savic, Snezana Savic, Guoping Lian and Franciska Erdő
Pharmaceutics 2024, 16(6), 817; https://doi.org/10.3390/pharmaceutics16060817 - 16 Jun 2024
Cited by 2 | Viewed by 2526
Abstract
Skin is the largest organ and a multifunctional interface between the body and its environment. It acts as a barrier against cold, heat, injuries, infections, chemicals, radiations or other exogeneous factors, and it is also known as the mirror of the soul. The [...] Read more.
Skin is the largest organ and a multifunctional interface between the body and its environment. It acts as a barrier against cold, heat, injuries, infections, chemicals, radiations or other exogeneous factors, and it is also known as the mirror of the soul. The skin is involved in body temperature regulation by the storage of fat and water. It is an interesting tissue in regard to the local and transdermal application of active ingredients for prevention or treatment of pathological conditions. Topical and transdermal delivery is an emerging route of drug and cosmetic administration. It is beneficial for avoiding side effects and rapid metabolism. Many pharmaceutical, technological and cosmetic innovations have been described and patented recently in the field. In this review, the main features of skin morphology and physiology are presented and are being followed by the description of classical and novel nanoparticulate dermal and transdermal drug formulations. The biophysical aspects of the penetration of drugs and cosmetics into or across the dermal barrier and their investigation in diffusion chambers, skin-on-a-chip devices, high-throughput measuring systems or with advanced analytical techniques are also shown. The current knowledge about mathematical modeling of skin penetration and the future perspectives are briefly discussed in the end, all also involving nanoparticulated systems. Full article
(This article belongs to the Special Issue Nanoparticles for Local Drug Delivery)
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44 pages, 2418 KiB  
Review
Recent Approaches for the Topical Treatment of Psoriasis Using Nanoparticles
by Krisztina Bodnár, Pálma Fehér, Zoltán Ujhelyi, Ildikó Bácskay and Liza Józsa
Pharmaceutics 2024, 16(4), 449; https://doi.org/10.3390/pharmaceutics16040449 - 25 Mar 2024
Cited by 6 | Viewed by 4111
Abstract
Psoriasis (PSO) is a chronic autoimmune skin condition characterized by the rapid and excessive growth of skin cells, which leads to the formation of thick, red, and scaly patches on the surface of the skin. These patches can be itchy and painful, and [...] Read more.
Psoriasis (PSO) is a chronic autoimmune skin condition characterized by the rapid and excessive growth of skin cells, which leads to the formation of thick, red, and scaly patches on the surface of the skin. These patches can be itchy and painful, and they may cause discomfort for patients affected by this condition. Therapies for psoriasis aim to alleviate symptoms, reduce inflammation, and slow down the excessive skin cell growth. Conventional topical treatment options are non-specific, have low efficacy and are associated with adverse effects, which is why researchers are investigating different delivery mechanisms. A novel approach to drug delivery using nanoparticles (NPs) shows promise in reducing toxicity and improving therapeutic efficacy. The unique properties of NPs, such as their small size and large surface area, make them attractive for targeted drug delivery, enhanced drug stability, and controlled release. In the context of PSO, NPs can be designed to deliver active ingredients with anti-inflammatory effect, immunosuppressants, or other therapeutic compounds directly to affected skin areas. These novel formulations offer improved access to the epidermis and facilitate better absorption, thus enhancing the therapeutic efficacy of conventional anti-psoriatic drugs. NPs increase the surface-to-volume ratio, resulting in enhanced penetration through the skin, including intracellular, intercellular, and trans-appendage routes. The present review aims to discuss the latest approaches for the topical therapy of PSO using NPs. It is intended to summarize the results of the in vitro and in vivo examinations carried out in the last few years regarding the effectiveness and safety of nanoparticles. Full article
(This article belongs to the Special Issue Nanoparticles for Local Drug Delivery)
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