The role of percutaneous penetration enhancers

Walker, Roderick B.; Smith, Eric W.

doi:10.1016/0169-409x(95)00078-l

Cited by 166 publications

(84 citation statements)

References 33 publications

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“…The enhancement of skin permeability of ketoprofen by oleic acid was mainly due to disturbance of the stratum corneum (Kim et al, 1993). More specifically, oleic acid was found to increase the freedom or fluidic movement of the skin lipid structures, thereby decreasing the phase transition temperatures of the skin lipids (Walker & Smith, 1996). In addition, the prevention of drug crystallization after film formation is of importance for metastable systems such as dermal formulations.…”

Section: Introductionmentioning

confidence: 99%

Formulation and in vitro/in vivo evaluation of chitosan-based film forming gel containing ketoprofen

Kang

Lee

et al. 2017

Drug Delivery

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The film forming gel, adhered to skin surfaces upon application and formed a film, has an advantage onto skin to provide protection and continuous drug release to the application site. This study aimed to prepare a chitosan-based film forming gel containing ketoprofen (CbFG) and to evaluate the CbFG and film from CbFG (CbFG-film). CbFG were prepared with chitosan, lactic acid and various skin permeation enhancers. The physicochemical characteristics were evaluated by texture analysis, viscometry, SEM, DSC, XRD and FT-IR. To identify the mechanism of skin permeation, in vitro skin permeation study was conducted with a Franz diffusion cell and excised SD-rat and hairless mouse dorsal skin. In vivo efficacy assessment in mono-iodoacetate (MIA)-induced rheumatoid arthritis animal model was also conducted. CbFG was successfully prepared and, after applying CbFG to the excised rat dorsal skin, the CbFG-film was also formed well. The physicochemical characteristics of CbFG and CbFG-film could be explained by the grafting of oleic acid onto chitosan in the absence of catalysts. In addition, CbFG containing oleic acid had a higher skin permeation rate in comparison with any other candidate enhancers. The in vivo efficacy study also confirmed significant anti-inflammatory and analgesic effects. Consequently, we report the successful preparation of chitosan-based film forming gel containing ketoprofen with excellent mechanical properties, skin permeation and anti-inflammatory and analgesic effects. ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 99%

Formulation and in vitro/in vivo evaluation of chitosan-based film forming gel containing ketoprofen

Kang

Lee

et al. 2017

Drug Delivery

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“…Since DMSO reported to causes skin erosion we have used propylene glycol as permeation enhancer in the preparation of the gel formulation (Walker, Smith, 1996). Disodium edetate and triethanolamine were used in the formulation in order to adjust the pH of the formulation.…”

Section: Formulation and Evaluation Of Topical Herbal Gelmentioning

confidence: 99%

Formulation and evaluation of topical herbal gel for the treatment of arthritis in animal model

Rajasekaran

Govindarjan

Arivukkarasu

2016

Braz. J. Pharm. Sci.

104

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The objective of the study is to formulate and evaluate a topical herbal gel containing Cardiospermum halicacabum and Vitex negundo leaf extracts for their anti-arthritic activity in rats. Twelve herbal gel formulations were prepared using 1.5% of gelling agents carbopol 934 (F1-F6) and carbopol 940 (F6-F12) and they were evaluated for physical appearance, net content, viscosity, extrudability, pH, spreadability, in vitro diffusion profile and primary skin irritation tests. The stability study for the topical herbal gel formulation was done as per ICH guidelines and anti-arthritic activity was evaluated by Freund's Complete Adjuvant (FCA) induced arthritis method. Assessment of body weight, paw volume, hematological and biochemical parameters, histopathological examination and In vitro determination of serum biomarkers were also carried out. Formulated gels were homogenous, stable and complied with the guidelines. Among the formulations, F4 showed better release (98.4 %) characteristics than other formulations. No erythema or edema was observed in the skin irritation test confirming the gel was nontoxic and safe. Topical application of the herbal gel F4 containing carbopol 934 displayed significant (p < 0.001) anti-arthritic activity compared to diseased rats. Reduction in paw volume, no agglutination in C -reactive protein and rheumatic factor, reduction in TNFα level, regaining of normal hematological, and biochemical parameters, reduction in spleen and thymus weight and histopathological examination supported the anti-arthritic activity of the gel formulation.Uniterms: Arthritis/treatment/herbal gel. Cardiospermum halicacabum/topical herbal gel. Vitex negundo/ topical herbal gel. Medicinal plants/arthritis.

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“…In addition to physical methods, drug permeation through the stratum corneum can use chemical penetration enhancers [25,42,43]. Cis-9-Octadecenoic acid (oleic acid, OA) was found to be a good penetration enhancer [25,44,45], and research regarding the impact of the penetration enhancer, oleic acid, on the barrier properties of stratum corneum lipid model membranes was conducted.…”

Section: Fick's Second Lawmentioning

confidence: 99%

Dermic diffusion and stratum corneum: A state of the art review of mathematical models

Couto

Fernandes

Cordeiro

et al. 2014

Journal of Controlled Release

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A B S T R A C TTransdermal biotechnologies are an ever increasing field of interest, due to the medical and pharmaceutical applications that they underlie. There are several mathematical models at use that permit a more inclusive vision of pure experimental data and even allow practical extrapolation for new dermal diffusion methodologies. However, they grasp a complex variety of theories and assumptions that allocate their use for specific situations. Models based on Fick's First Law found better use in contexts where scaled particle theory Models would be extensive in time-span but the reciprocal is also true, as context of transdermal diffusion of particular active compounds changes. This article reviews extensively the various theoretical methodologies for studying dermic diffusion in the rate limiting dermic barrier, the stratum corneum, and systematizes its characteristics, their proper context of application, advantages and limitations, as well as future perspectives.

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The role of percutaneous penetration enhancers

Cited by 166 publications

References 33 publications

Formulation and in vitro/in vivo evaluation of chitosan-based film forming gel containing ketoprofen

Formulation and in vitro/in vivo evaluation of chitosan-based film forming gel containing ketoprofen

Formulation and evaluation of topical herbal gel for the treatment of arthritis in animal model

Dermic diffusion and stratum corneum: A state of the art review of mathematical models

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