Drug Nanocarriers for Pharmaceutical Applications

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

Deadline for manuscript submissions: 20 May 2025 | Viewed by 8463

Special Issue Editors


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Guest Editor
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, 41012 Seville, Spain
Interests: drug delivery; drug carriers; nanomedicine; nanoparticles; gemini surfactants; biopolymers
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Guest Editor
Department of Cellular Biology, Physiology and Immunology, Faculty of Science, University of Córdoba, 14014 Cordoba, Spain
Interests: biotechnology; biochemistry; neurodegeneration and related iseases
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Physical Chemistry, Faculty of Chemistry, University of Seville, 41012 Seville, Spain
Interests: DNA-NPs; proteins-NPs interactions; thermodynamics; kinetics and ligand-ligand interactions
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nanocarriers have shown great promise in the area of drug delivery and pharmaceutical applications. Colloidal drug carrier systems contribute to improve relevant aspects of pharmaceutical formulations, such as pharmacokinetics, biodistribution, biocompatibility, solubility, and stability. Moreover, their tunable physiochemical properties decrease toxicities with respect to free drugs and have the ability to transport drugs to a specific site and control the release, effectively decreasing side effects in patients. Due to their promising properties, nanocarriers are prominent in medicine. For instance, in the field of cancer therapy, nanocarriers for transporting anticancer drugs serve to resolve specific problems related to poor specificity, high toxicity, or even drug resistance. In the area of antibiotic design, loading drugs into carriers provides benefits over conventional treatment using free drugs, protecting drugs from bacterial resistance. This way, action time is minimized, and therefore, bacterial resistance is avoided. In this context, it is noteworthy that metallic nanoparticles by themselves can serve as potential antibacterial agents due to their unique physiochemical properties at the nanoscale level. These characteristics contribute to producing a synergistic effect between the nanomaterial and the loaded drug that enhances its antibiotic effect. Another example of drug nanocarriers’ versatility is in the field of veterinary and human medicine, where stabilized nanoparticles loading different bioelements are used to create new, low-toxic, highly effective, biocompatible nanomedicine.

This Special Issue aims to consider all of these key factors that may be taken into account when preparing nanocarriers suitable for drug delivery. We invite authors to contribute original research articles or review articles covering different topics of interest, such as (i) the synthesis and characterization of new types of nanocarriers; (ii). the effective control and study of different relevant aspects in nanoformulation, such as size distribution, aggregation state, charge, drug loading and release, stability, viability assays, or nanocarrier internalization; and (iii) the use of drug carriers for improving effectivity and decreasing side effects with respect to free drugs, with relevant applications in nanomedicine and pharmacy.

Dr. Elia M. Grueso
Dr. Rosa María Giráldez-Pérez
Prof. Dr. Rafael Prado-Gotor
Guest Editors

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Keywords

  • drug nanocarriers
  • nanomedicine
  • physicochemical properties
  • cancer targeting
  • antibiotic resistance
  • bioelements

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Published Papers (5 papers)

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Research

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18 pages, 4965 KiB  
Article
T14diLys/DOPE Liposomes: An Innovative Option for siRNA-Based Gene Knockdown?
by Sophie Meinhard, Frank Erdmann, Henrike Lucas, Maria Krabbes, Stephanie Krüger, Christian Wölk and Karsten Mäder
Pharmaceutics 2025, 17(1), 25; https://doi.org/10.3390/pharmaceutics17010025 - 27 Dec 2024
Viewed by 862
Abstract
Background/Objectives: Bringing small interfering RNA (siRNA) into the cell cytosol to achieve specific gene silencing is an attractive but also very challenging option for improved therapies. The first step for successful siRNA delivery is the complexation with a permanent cationic or ionizable compound. [...] Read more.
Background/Objectives: Bringing small interfering RNA (siRNA) into the cell cytosol to achieve specific gene silencing is an attractive but also very challenging option for improved therapies. The first step for successful siRNA delivery is the complexation with a permanent cationic or ionizable compound. This protects the negatively charged siRNA and enables transfection through the cell membrane. The current study explores the performance of the innovative, ionizable lipid 2-Tetradecylhexadecanoic acid-(2-bis{[2-(2,6-diamino-1-oxohexyl)amino]ethyl}aminoethyl)-amide (T14diLys), in combination with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), for siRNA delivery and the impact of the production method (sonication vs. extrusion) on the particle properties. Methods: Liposomes were produced either with sonication or extrusion and characterized. The extruded liposomes were combined with siRNA at different N/P ratios and investigated in terms of size zeta potential, encapsulation efficiency, lipoplex stability against RNase A, and knockdown efficiency using enhanced green fluorescent protein (eGFP)-marked colon adenocarcinoma cells. Results: The liposomes prepared by extrusion were smaller and had a narrower size distribution than the sonicated ones. The combination of siRNA and liposomes at a nitrogen-to-phosphate (N/P) ratio of 5 had optimal particle properties, high encapsulation efficiency, and lipoplex stability. Gene knockdown tests confirmed this assumption. Conclusions: Liposomes produced with extrusion were more reproducible and provided enhanced particle properties. The physicochemical characterization and in vitro experiments showed that an N/P ratio of 5 was the most promising ratio for siRNA delivery. Full article
(This article belongs to the Special Issue Drug Nanocarriers for Pharmaceutical Applications)
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16 pages, 3140 KiB  
Article
Cationic Hydroxyethyl Cellulose Nanocomplexes and RANK siRNA/Zoledronate Co-Delivery Systems for Osteoclast Inhibition
by Sohyun Lee, Seoyeon Park and Tae-il Kim
Pharmaceutics 2024, 16(12), 1623; https://doi.org/10.3390/pharmaceutics16121623 - 22 Dec 2024
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Abstract
Background/Objectives: In this study, HECP2k polymer, polyethylenimine2k (PEI2k)-modified hydroxyethyl cellulose (HEC) was utilized to form the nanocomplexes with receptor activator of nuclear factor k-B (RANK) siRNA and zoledronate (Zol) for osteoclast inhibition. HECP2k/(RANK siRNA + Zol) nanocomplexes prepared by simple mixing were anticipated [...] Read more.
Background/Objectives: In this study, HECP2k polymer, polyethylenimine2k (PEI2k)-modified hydroxyethyl cellulose (HEC) was utilized to form the nanocomplexes with receptor activator of nuclear factor k-B (RANK) siRNA and zoledronate (Zol) for osteoclast inhibition. HECP2k/(RANK siRNA + Zol) nanocomplexes prepared by simple mixing were anticipated to overcome the low transfection efficiency of siRNA and the low bioavailability of Zol. Methods: The characterization of both HECP2k/(pDNA + Zol) nanocomplexes and HECP2k/(RANK siRNA + Zol) nanocomplexes was performed. Results: The nanocomplexes were successfully formed even in the presence of Zol, showing about 200 nm sizes and about 20 mV of positive zeta potential values suitable for efficient cellular uptake. They also possessed high endosome buffering ability by PEI and Zol, suggesting the potential for efficient endosomal escape. It was found that the low cytotoxic nanocomplexes (>90% cell viability) displayed greater transfection efficiency than PEI25k and even HECP2k polyplexes. Finally, it was found by tartrate-resistant acid phosphatase (TRAP) assay and qPCR analysis that HECP2k/(RANK siRNA + Zol) nanocomplexes could inhibit the TRAP to about 50% value and another characteristic osteoclastic gene expression, increasing FAS gene expression to about 16 times higher than control and more efficiently (about 3 times and 5 times higher, respectively) than HECP2k/siRNA polyplexes and Zol only. Conclusions: HECP2k/(RANK siRNA + Zol) nanocomplexes formed by simple mixing showed great potential for inhibiting osteoclast differentiation and osteoclast activity, inducing the apoptosis via combinatorial effects of RANK siRNA and Zol. Full article
(This article belongs to the Special Issue Drug Nanocarriers for Pharmaceutical Applications)
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18 pages, 4626 KiB  
Article
Ivermectin-Loaded Mesoporous Silica and Polymeric Nanocapsules: Impact on Drug Loading, In Vitro Solubility Enhancement, and Release Performance
by Maiara Callegaro Velho, Nadine Lysyk Funk, Monique Deon, Edilson Valmir Benvenutti, Silvio Buchner, Ruth Hinrichs, Diogo André Pilger and Ruy Carlos Ruver Beck
Pharmaceutics 2024, 16(3), 325; https://doi.org/10.3390/pharmaceutics16030325 - 26 Feb 2024
Cited by 5 | Viewed by 2546
Abstract
Ivermectin (IVM), a widely used drug for parasitic infections, faces formulation and application challenges due to its poor water solubility and limited bioavailability. Pondering the impact of IVM’s high partition coefficient value (log P) on its drug release performance, it is relevant to [...] Read more.
Ivermectin (IVM), a widely used drug for parasitic infections, faces formulation and application challenges due to its poor water solubility and limited bioavailability. Pondering the impact of IVM’s high partition coefficient value (log P) on its drug release performance, it is relevant to explore whether IVM nanoencapsulation in organic or inorganic nanoparticles would afford comparable enhanced aqueous solubility. To date, the use of inorganic nanoparticles remains an unexplored approach for delivering IVM. Therefore, here we loaded IVM in mesoporous silica particles (IVM-MCM), as inorganic nanomaterial, and in well-known poly(ε-caprolactone) nanocapsules (IVM-NC). IVM-MCM had a well-organized hexagonal mesoporous structure, reduced surface area, and high drug loading of 10% w/w. IVM-NC had a nanometric mean size (196 nm), high encapsulation efficiency (100%), physicochemical stability as an aqueous dispersion, and drug loading of 0.1% w/w. Despite differing characteristics, both nanoencapsulated forms enhance IVM’s aqueous intrinsic solubility compared to a crystalline IVM: after 72 h, IVM-MCM and IVM-NC achieve 72% and 78% releases through a dialysis bag, whereas crystalline IVM dispersion achieves only 40% drug diffusion. These results show distinct controlled release profiles, where IVM-NC provides a deeper sustained controlled release over the whole experiment compared to the inorganic nanomaterial (IVM-MCM). Discussing differences, including drug loading and release kinetics, is crucial for optimizing IVM’s therapeutic performance. The study design, combined with administration route plans and safety considerations for humans and animals, may expedite the rational optimization of IVM nanoformulations for swift clinical translation. Full article
(This article belongs to the Special Issue Drug Nanocarriers for Pharmaceutical Applications)
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18 pages, 13330 KiB  
Article
Development of a Novel Red Clay-Based Drug Delivery Carrier to Improve the Therapeutic Efficacy of Acyclovir in the Treatment of Skin Cancer
by Arul Prakash Francis, Aftab Ahmad, Sri Durga Devi Nagarajan, Harish Sundar Yogeeswarakannan, Krishnaraj Sekar, Shah Alam Khan, Dhanalekshmi Unnikrishnan Meenakshi, Asif Husain, Mohammed A. Bazuhair and Nandakumar Selvasudha
Pharmaceutics 2023, 15(7), 1919; https://doi.org/10.3390/pharmaceutics15071919 - 10 Jul 2023
Cited by 1 | Viewed by 2270
Abstract
Acyclovir (ACV) is a promising candidate for drug repurposing because of its potential to provide an effective treatment for viral infections and non-viral diseases, such as cancer, for which limited treatment options exist. However, its poor physicochemical properties limit its application. This study [...] Read more.
Acyclovir (ACV) is a promising candidate for drug repurposing because of its potential to provide an effective treatment for viral infections and non-viral diseases, such as cancer, for which limited treatment options exist. However, its poor physicochemical properties limit its application. This study aimed to formulate and evaluate an ACV-loaded red clay nanodrug delivery system exhibiting an effective cytotoxicity. The study focused on the preparation of a complex between ACV and red clay (RC) using sucrose stearate (SS) (nanocomplex F1) as an immediate-release drug-delivery system for melanoma treatment. The synthesized nanocomplex, which had nanosized dimensions, a negative zeta potential and the drug release of approximately 85% after 3 h, was found to be promising. Characterization techniques, including FT-IR, XRD and DSC-TGA, confirmed the effective encapsulation of ACV within the nanocomplex and its stability due to intercalation. Cytotoxicity experiments conducted on melanoma cancer cell lines SK-MEL-3 revealed that the ACV release from the nanocomplex formulation F1 effectively inhibited the growth of melanoma cancer cells, with an IC50 of 25 ± 0.09 µg/mL. Additionally, ACV demonstrated a significant cytotoxicity at approximately 20 µg/mL in the melanoma cancer cell line, indicating its potential repurposing for skin cancer treatment. Based on these findings, it can be suggested that the RC-SS complex could be an effective drug delivery carrier for localized cancer therapy. Furthermore, the results of an in silico study suggested the addition of chitosan to the formulation for a more effective drug delivery. Energy and interaction analyses using various modules in a material studio demonstrated the high stability of the composite comprising red clay, sucrose stearate, chitosan and ACV. Thus, it could be concluded that the utilization of the red clay-based drug delivery system is a promising strategy to improve the effectiveness of targeted cancer therapy. Full article
(This article belongs to the Special Issue Drug Nanocarriers for Pharmaceutical Applications)
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Review

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30 pages, 1527 KiB  
Review
Integrin-Specific Stimuli-Responsive Nanomaterials for Cancer Theranostics
by Zahra Taheri, Negin Mozafari, Ghazal Moradian, Denise Lovison, Ali Dehshahri and Rossella De Marco
Pharmaceutics 2024, 16(11), 1441; https://doi.org/10.3390/pharmaceutics16111441 - 11 Nov 2024
Viewed by 1371
Abstract
Background: Cancer is one of the leading causes of death worldwide. The tumor microenvironment makes the tumor difficult to treat, favoring drug resistance and the formation of metastases, resulting in death. Methods: Stimuli-responsive nanoparticles have shown great capacity to be used [...] Read more.
Background: Cancer is one of the leading causes of death worldwide. The tumor microenvironment makes the tumor difficult to treat, favoring drug resistance and the formation of metastases, resulting in death. Methods: Stimuli-responsive nanoparticles have shown great capacity to be used as a powerful strategy for cancer treatment, diagnostic, as well as theranostic. Nanocarriers are not only able to respond to internal stimuli such as oxidative stress, weakly acidic pH, high temperature, and the high expression of particular enzymes, but also to external stimuli such as light and paramagnetic characteristics to be exploited. Results: In this work, stimulus-responsive nanocarriers functionalized with arginine-glycine-aspartic acid (Arg-Gly-Asp) sequence as well as mimetic sequences with the capability to recognize integrin receptors are analyzed. Conclusions: This review highlights the progress that has been made in the development of new nanocarriers, capable of responding to endogenous and exogenous stimuli essential to combat cancer. Full article
(This article belongs to the Special Issue Drug Nanocarriers for Pharmaceutical Applications)
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