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Pharmaceutics
Special Issues
Topical Drug Carriers: Recent Advances and Future Challenges
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Topical Drug Carriers: Recent Advances and Future Challenges

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (20 September 2024) | Viewed by 4760

Special Issue Editors

Dr. Anna Czajkowska-Kośnik

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Guest Editor
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, 15-222 Białystok, Poland
Interests: lipid carriers; low solubility; pharmaceutical technology; nanocarriers; topical drug delivery; formulation and characterization of dosage forms; drug release; skin permeation
Special Issues, Collections and Topics in MDPI journals
Dr. Magdalena Wróblewska

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, 15-222 Białystok, Poland
Interests: lipid carriers; pharmaceutical technology; drug formulation; characterization of dosage forms; solubilization techniques; polymers; antimicrobial activity; skin penetration; topical drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Topical drug carriers represent an important form of drug delivery system, and their use in therapy as an alternative to oral administration is becoming more widespread. The goal in designing these formulations is to obtain systems with optimized drug loading and release properties, which are able to ensure adequate penetration of the active substance. The therapeutic efficacy of topical formulations depends on both the physicochemical properties of the active substance and the type of carrier. It is well known that vehicles used in topical dosage forms may greatly affect the rate and extent of drug permeation. Recent advances in topical and transdermal drug delivery systems have enabled targeted delivery of therapeutics to the site of action by enhancing drug permeation across the stratum corneum and increased bioavailability. Although latest innovations in nanotechnology have enhanced the ability of molecules to pass through the skin by improving the pharmacokinetics of drugs, an appropriate vehicle remains to be developed to ensure drug delivery using noninvasive techniques.

We welcome the submission of articles on the latest aspects of topical and transdermal drug delivery, particularly those focusing on improving drug efficacy and safety.

Dr. Anna Czajkowska-Kośnik
Dr. Magdalena Wróblewska
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • topical and transdermal delivery
  • nanocarriers
  • new technologies
  • drug permeation
  • skin absorption
  • therapeutic agent
  • innovative delivery systems
  • mucoadhesion
  • dosage form development
  • physicochemical properties

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Published Papers (4 papers)

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20 pages, 5516 KiB  
Article
Lipid-Based Formulation of Baricitinib for the Topical Treatment of Psoriasis
by Roya Mohammadi-Meyabadi, Mireia Mallandrich, Negar Beirampour, Núria Garrós, Lupe Carolina Espinoza, Lilian Sosa, Joaquim Suñer-Carbó, María José Rodríguez-Lagunas, María Luisa Garduño-Ramírez and Ana C. Calpena-Campmany
Pharmaceutics 2024, 16(10), 1287; https://doi.org/10.3390/pharmaceutics16101287 - 30 Sep 2024
Viewed by 986
Abstract
Background: Baricitinib, commonly used for autoimmune diseases, is typically administered orally, which can lead to systemic adverse effects. A topical formulation could potentially offer localized therapeutic effects while minimizing these side effects. Objectives: This study focuses on developing a lipid-based topical formulation of [...] Read more.
Background: Baricitinib, commonly used for autoimmune diseases, is typically administered orally, which can lead to systemic adverse effects. A topical formulation could potentially offer localized therapeutic effects while minimizing these side effects. Objectives: This study focuses on developing a lipid-based topical formulation of baricitinib (BCT-OS) for treating psoriasis. Methods: The optimized formulation was then assessed for physical, chemical, and biopharmaceutical characterization. Furthermore, the anti-inflammatory efficacy of the formulation was tested in a model of psoriasis induced by imiquimod in mice, and its tolerance was determined by the evaluation of biomechanical skin properties and an inflammation test model induced by xylol in mice. Results: BCT-OS presented appropriate characteristics for skin administration in terms of pH, rheology, extensibility, and stability. The formulation also demonstrated a notable reduction in skin inflammation in the mouse model, and high tolerability without affecting the skin integrity. Conclusions: BCT-OS shows promise as an alternative treatment for psoriasis, offering localized therapeutic benefits with a potentially improved safety profile compared to systemic administration. Full article
(This article belongs to the Special Issue Topical Drug Carriers: Recent Advances and Future Challenges)
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15 pages, 14810 KiB  
Article
Improving Water Solubility and Skin Penetration of Ursolic Acid through a Nanofiber Process to Achieve Better In Vitro Anti-Breast Cancer Activity
by Hsuan Fu, Tzu-Hui Wu, Chih-Peng Ma and Feng-Lin Yen
Pharmaceutics 2024, 16(9), 1147; https://doi.org/10.3390/pharmaceutics16091147 - 29 Aug 2024
Viewed by 748
Abstract
Woman’s breast cancer has always been among the top ten causes of cancer death, and nearly 2% to 5% of locally advanced breast cancers develop a fungating breast wound. Fungal breast cancer leads to skin ulcers, wound ruptures, and other bacterial infections in [...] Read more.
Woman’s breast cancer has always been among the top ten causes of cancer death, and nearly 2% to 5% of locally advanced breast cancers develop a fungating breast wound. Fungal breast cancer leads to skin ulcers, wound ruptures, and other bacterial infections in patients. Ursolic acid (UA), a natural pentacyclic triterpene compound, is widely distributed in many fruits. Previous studies demonstrated that UA has anti-breast cancer, antifungal, and improved wound-healing effects. UA, however, had poor water solubility and low bioavailability, restricting its clinical application. Nanofibers have the advantages of rapid dissolution, improved stability, and bioavailability of active ingredients. We had successfully prepared ursolic acid nanofibers (UANFs) and effectively improved their water solubility and skin penetration. UANFs can increase water solubility by improving the physicochemical properties, including increased surface area, intermolecular bonding with excipients, and amorphous transformation. Furthermore, UANFs had better anti-breast cancer activity than raw UA. UANFs inhibited the expression of phospho-signal transducer and activator of transcription 3 (STAT3) and phospho-extracellular regulated protein kinases (ERK)1/2, and induced cleaved caspase-3 protein expression, but had no effect on the raw UA treatment. In summary, UANFs enhanced the skin absorption of UA and improved its anti-breast cancer efficacy. We expect that UANFs can be used as an anti-breast cancer treatment and reduce the discomfort of breast cancer patients during dressing changes, but more detailed efficacy and safety trials still need to be conducted in further studies. Full article
(This article belongs to the Special Issue Topical Drug Carriers: Recent Advances and Future Challenges)
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28 pages, 6006 KiB  
Article
Design and Biocompatibility of Biodegradable Poly(octamethylene suberate) Nanoparticles to Treat Skin Diseases
by Dragana P. C. de Barros, Luís P. Fonseca, Luís G. Gonçalves, Diogo S. Serrano and Abel Oliva
Pharmaceutics 2024, 16(6), 753; https://doi.org/10.3390/pharmaceutics16060753 - 3 Jun 2024
Viewed by 819
Abstract
Biodegradable aliphatic polyester formulations as carriers for topical drug delivery show the potential to encapsulate structurally different therapeutic compounds. Poly(octamethylene suberate) (POS) nanoparticles (POS-NPs) were used as a matrix to encapsulate four therapeutic molecules used to treat skin disorders: caffeine (CF), quercetin (QR), [...] Read more.
Biodegradable aliphatic polyester formulations as carriers for topical drug delivery show the potential to encapsulate structurally different therapeutic compounds. Poly(octamethylene suberate) (POS) nanoparticles (POS-NPs) were used as a matrix to encapsulate four therapeutic molecules used to treat skin disorders: caffeine (CF), quercetin (QR), hydrocortisone (HC), and adapalene (AD). Hydrophobicity and chemical structure of bioactive compounds (BCs) influenced the physicochemical stability of drug-loaded nanoparticles. The particle size of drug-loaded nanoparticles was between 254.9 nm for the CF-POS-NP and 1291.3 for QR-POS-NP. Particles had a negative charge from −27.6 mV (QR) to −49.2 mV (HC). Drug loading content for all BC-POS-NPs varies between 36.11 ± 1.48% (CF-POS-NP) and 66.66 ± 4.87% (AD-POS-NP), and their entrapment efficiency is relatively high (28.30 ± 1.81% and 99.95 ± 0.04%, respectively). Calorimetric analysis showed the appearance of polymorphism for AD- and HC-loaded systems and the drug’s complete solubilisation into all nanoparticle formulations. FTIR and NMR spectra showed apparent drug incorporation into the polymer matrix of NPs. The encapsulation of BCs enhanced the antioxidative effect. The prepared POS nanoparticles’ cytotoxicity was studied using two dermal cell lines, keratinocyte (HaCaT) cells and fibroblasts (HDFn). The nanoparticle cytotoxic effect was more substantial on HaCaT cell lines. A reconstructed human epidermis (RHE) was successfully used to investigate the penetration of polymeric NPs. Based on permeation and histology studies, HC-POS-NPs and CF-POS-NPs were shown not to be suitable for dermal applications with the explored drug concentrations. AD presents a high permeation rate and no toxic impact on RHE. Full article
(This article belongs to the Special Issue Topical Drug Carriers: Recent Advances and Future Challenges)
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17 pages, 6150 KiB  
Article
Foams Set a New Pace for the Release of Diclofenac Sodium
by Fanni Falusi, Szilvia Berkó, Mária Budai-Szűcs, Zoltán Veréb and Anita Kovács
Pharmaceutics 2024, 16(2), 287; https://doi.org/10.3390/pharmaceutics16020287 - 18 Feb 2024
Viewed by 1580
Abstract
Medicated foams have emerged as promising alternatives to traditional carrier systems in pharmaceutical research. Their rapid and convenient application allows for effective treatment of extensive or hirsute areas, as well as sensitive or inflamed skin surfaces. Foams possess excellent spreading capabilities on the [...] Read more.
Medicated foams have emerged as promising alternatives to traditional carrier systems in pharmaceutical research. Their rapid and convenient application allows for effective treatment of extensive or hirsute areas, as well as sensitive or inflamed skin surfaces. Foams possess excellent spreading capabilities on the skin, ensuring immediate drug absorption without the need for intense rubbing. Our research focuses on the comparison of physicochemical and biopharmaceutical properties of three drug delivery systems: foam, the foam bulk liquid, and a conventional hydrogel. During the development of the composition, widely used diclofenac sodium was employed. The safety of the formulae was confirmed through an in vitro cytotoxicity assay. Subsequently, the closed Franz diffusion cell was used to determine drug release and permeation in vitro. Ex vivo Raman spectroscopy was employed to investigate the presence of diclofenac sodium in various skin layers. The obtained results of the foam were compared to the bulk liquid and to a conventional hydrogel. In terms of drug release, the foam showed a rapid release, with 80% of diclofenac released within 30 min. In summary, the investigated foam holds promising potential as an alternative to traditional dermal carrier systems, offering faster drug release and permeation. Full article
(This article belongs to the Special Issue Topical Drug Carriers: Recent Advances and Future Challenges)
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