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Pharmaceutics
Special Issues
Penetration Enhancement of Topical Formulations
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Penetration Enhancement of Topical Formulations

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (10 December 2017) | Viewed by 39823

Special Issue Editor

Dr. Keng Wooi Ng

E-Mail Website
Guest Editor
School of Pharmacy, Faculty of Medical Sciences, Newcastle University, Newcastle Upon Tyne NE1 7RU, UK
Interests: topical and transdermal drug delivery; microneedle technology; biosensors
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleague,

Topical drug delivery is the administration of therapeutic agents at the site of action. This route of delivery offers potential advantages, including better drug targeting, improved toxicity profiles, and amenability of dosing. Topical formulations can be applied to any accessible tissue surface, such as the skin, nail, eye and mucosal membranes, and thus have broad applications in a range of diseases. In any case, drug penetration into the target tissue is necessary for therapeutic success, yet it has always been one of the biggest challenges facing topical drug delivery. This is especially true of emerging treatments involving biologics, which are mostly macromolecules that do not traverse biological membranes readily. This Special Issue of Pharmaceutics will report innovative strategies in enhancing topical drug penetration. Suitable contributions may include, but are not limited to: chemical penetration enhancers, prodrugs, co-drugs, physical penetration enhancement techniques (e.g., microneedles, iontophoresis), and nanocarriers. Original research articles and reviews discussing such strategies at any stage of development, from proof of principle to finished pharmaceutical product, are welcomed.

Dr. Keng Wooi Ng
Guest Editor

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 formulations
  • Drug delivery
  • Penetration enhancer
  • Microneedles
  • Iontophoresis
  • Liposomes
  • Nanocarriers
  • Prodrugs
  • Co-drugs
  • Skin

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Published Papers (4 papers)

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Editorial

Jump to: Research

3 pages, 167 KiB  
Editorial
Penetration Enhancement of Topical Formulations
by Keng Wooi Ng
Pharmaceutics 2018, 10(2), 51; https://doi.org/10.3390/pharmaceutics10020051 - 17 Apr 2018
Cited by 33 | Viewed by 7130
Abstract
This special issue, which is entitled “Penetration Enhancement of Topical Formulations”, presents a selection of the latest research that elucidates the challenges facing topical formulations for human skin in addition to proposing interesting solutions.[…] Full article
(This article belongs to the Special Issue Penetration Enhancement of Topical Formulations)

Research

Jump to: Editorial

14 pages, 469 KiB  
Article
In Vitro Evaluation of Sunscreen Safety: Effects of the Vehicle and Repeated Applications on Skin Permeation from Topical Formulations
by Lucia Montenegro, Rita Turnaturi, Carmela Parenti and Lorella Pasquinucci
Pharmaceutics 2018, 10(1), 27; https://doi.org/10.3390/pharmaceutics10010027 - 27 Feb 2018
Cited by 25 | Viewed by 8883
Abstract
The evaluation of UV-filter in vitro percutaneous absorption allows the estimation of the systemic exposure dose (SED) and the margin of safety (MoS) of sunscreen products. As both the vehicle and pattern of application may affect sunscreen safety and efficacy, we evaluated in [...] Read more.
The evaluation of UV-filter in vitro percutaneous absorption allows the estimation of the systemic exposure dose (SED) and the margin of safety (MoS) of sunscreen products. As both the vehicle and pattern of application may affect sunscreen safety and efficacy, we evaluated in vitro release and skin permeation of two widely used UV-filters, octylmethoxycinnamate (OMC) and butylmethoxydibenzoylmethane (BMBM) from topical formulations with different features (oil in water (O/W) emulsions with different viscosity, water in oil (W/O) emulsion, oils with different lipophilicity). To mimic in-use conditions, we carried out experiments repeating sunscreen application on the skin surface for three consecutive days. BMBM release from all these vehicles was very low, thus leading to poor skin permeation. The vehicle composition significantly affected OMC release and skin permeation, and slight increases of OMC permeation were observed after repeated applications. From skin permeation data, SED and MoS values of BMBM and OMC were calculated for all the investigated formulations after a single application and repeated applications. While MoS values of BMBM were always well beyond the accepted safety limit, the safety of sunscreen formulations containing OMC may depend on the vehicle composition and the application pattern. Full article
(This article belongs to the Special Issue Penetration Enhancement of Topical Formulations)
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12 pages, 1597 KiB  
Article
Minoxidil Skin Delivery from Nanoemulsion Formulations Containing Eucalyptol or Oleic Acid: Enhanced Diffusivity and Follicular Targeting
by Eman Abd, Heather A. E. Benson, Michael S. Roberts and Jeffrey E. Grice
Pharmaceutics 2018, 10(1), 19; https://doi.org/10.3390/pharmaceutics10010019 - 25 Jan 2018
Cited by 58 | Viewed by 10329
Abstract
In this work, we examined enhanced skin delivery of minoxidil applied in nanoemulsions incorporating skin penetration enhancers. Aliquots of fully characterized oil-in-water nanoemulsions (1 mL), containing minoxidil (2%) and the skin penetration enhancer oleic acid or eucalyptol as oil phases, were applied to [...] Read more.
In this work, we examined enhanced skin delivery of minoxidil applied in nanoemulsions incorporating skin penetration enhancers. Aliquots of fully characterized oil-in-water nanoemulsions (1 mL), containing minoxidil (2%) and the skin penetration enhancer oleic acid or eucalyptol as oil phases, were applied to full-thickness excised human skin in Franz diffusion cells, while aqueous solutions (1 mL) containing minoxidil were used as controls. Minoxidil in the stratum corneum (SC), hair follicles, deeper skin layers, and flux through the skin over 24 h was determined, as well as minoxidil solubility in the formulations and in the SC. The nanoemulsions significantly enhanced the permeation of minoxidil through skin compared with control solutions. The eucalyptol formulations (NE) promoted minoxidil retention in the SC and deeper skin layers more than did the oleic acid formulations, while the oleic acid formulations (NO) gave the greatest hair follicle penetration. Minoxidil maximum flux enhancement was associated with increases in both minoxidil SC solubility and skin diffusivity in both nanoemulsion systems. The mechanism of enhancement appeared to be driven largely by increased diffusivity, rather than increased partitioning into the stratum corneum, supporting the concept of enhanced fluidity and disruption of stratum corneum lipids. Full article
(This article belongs to the Special Issue Penetration Enhancement of Topical Formulations)
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1975 KiB  
Article
Development and Evaluation of Topical Gabapentin Formulations
by Christopher J. Martin, Natalie Alcock, Sarah Hiom and James C. Birchall
Pharmaceutics 2017, 9(3), 31; https://doi.org/10.3390/pharmaceutics9030031 - 30 Aug 2017
Cited by 20 | Viewed by 12075
Abstract
Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions whilst avoiding systemic side effects. To date, reports of topical gabapentin delivery in vitro have been variable and dependent on the skin model employed, primarily involving rodent and porcine models. In [...] Read more.
Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions whilst avoiding systemic side effects. To date, reports of topical gabapentin delivery in vitro have been variable and dependent on the skin model employed, primarily involving rodent and porcine models. In this study a variety of topical gabapentin formulations were investigated, including Carbopol® hydrogels containing various permeation enhancers, and a range of proprietary bases including a compounded Lipoderm® formulation; furthermore microneedle facilitated delivery was used as a positive control. Critically, permeation of gabapentin across a human epidermal membrane in vitro was assessed using Franz-type diffusion cells. Subsequently this data was contextualised within the wider scope of the literature. Although reports of topical gabapentin delivery have been shown to vary, largely dependent upon the skin model used, this study demonstrated that 6% (w/w) gabapentin 0.75% (w/w) Carbopol® hydrogels containing 5% (w/w) DMSO or 70% (w/w) ethanol and a compounded 10% (w/w) gabapentin Lipoderm® formulation were able to facilitate permeation of the molecule across human skin. Further pre-clinical and clinical studies are required to investigate the topical delivery performance and pharmacodynamic actions of prospective formulations. Full article
(This article belongs to the Special Issue Penetration Enhancement of Topical Formulations)
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