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      Enhancement of Dermal Delivery of Finasteride Using Microemulsion Systems

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          Abstract

          Purpose: Finasteride is a pharmaceutical agent that treats hair loss and acne with hormonal patterns. Due to its poor water solubility, and the smaller surface area in comparison to total skin surface area, penetration of the drug into hair follicles and skin is low. The aim of this research was to formulate, characterize and evaluate in vitro skin permeability of finasteride microemulsions (MEs).

          Methods: Finasteride MEs were prepared using a pseudo-ternary phase diagram method with an appropriate ratio of oil mixture, surfactant-co-surfactant mixture and water. MEs containing 1% finasteride were prepared with a suitable amount of oily phase and surfactant and cosurfactant. The physicochemical properties of these MEs and in vitro skin permeability of MEs were evaluated.

          Results: The results showed that the mean droplet size range of ME samples was 5–17 nm and pH was 5.1–5.7. The viscosity of MEs ranged from 86.4–209.6 cps. The drug release profile showed that 49.510% of the drug was released (ME-F-6) over the 24 hours of the experiment. The kinetics of drug release from all selected MEs were approximately described by Higuchi and first-order modeling. All ME formulations with different compositions and properties significantly increased flux and permeability coefficient from rat skin. The selected MEs exhibit 99.9% finasteride after six months of storage.

          Conclusion: This study showed that any change in the content and composition of MEs could change the physical and chemical properties in addition to ME permeability parameters. The MEs increased permeability of the skin to finasteride.

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          Most cited references40

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          Theory of self-assembly of hydrocarbon amphiphiles into micelles and bilayers

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            Overcoming the Stratum Corneum: The Modulation of Skin Penetration

            It is preferred that topically administered drugs act either dermally or transdermally. For that reason they have to penetrate into the deeper skin layers or permeate the skin. The outermost layer of the human skin, the stratum corneum, is responsible for its barrier function. Most topically administered drugs do not have the ability to penetrate the stratum corneum. In these cases modulations of the skin penetration profiles of these drugs and skin barrier manipulations are necessary. A skin penetration enhancement can be achieved either chemically, physically or by use of appropriate formulations. Numerous chemical compounds have been evaluated for penetration-enhancing activity, and different modes of action have been identified for skin penetration enhancement. In addition to chemical methods, skin penetration of drugs can be improved by physical options such as iontophoresis and phonophoresis, as well as by combinations of both chemical and physical methods or by combinations of several physical methods. There are cases where skin penetration of the drug used in the formulation is not the aim of the topical administration. Penetration reducers can be used to prevent chemicals entering the systemic circulation. This article concentrates on the progress made mainly over the last decade by use of chemical penetration enhancers. The different action modes of these substances are explained, including the basic principles of the physical skin penetration enhancement techniques and examples for their application.
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              The definition of microemulsion

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                Author and article information

                Journal
                Adv Pharm Bull
                Adv Pharm Bull
                Adv Pharm Bull
                APB
                TBZMED
                Advanced Pharmaceutical Bulletin
                Tabriz University of Medical Sciences
                2228-5881
                2251-7308
                October 2019
                24 October 2019
                : 9
                : 4
                : 584-592
                Affiliations
                1Student Research Committee, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
                2Department of Pharmaceutics, Faculty of pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
                3Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
                Author notes
                [* ] Corresponding Author: Anayatollah Salimi, Tel/Fax: +98 916 3130905, Email: salimi-a@ 123456ajums.ac.ir
                Author information
                https://orcid.org/0000-0003-1462-3930
                https://orcid.org/0000-0003-1505-7969
                Article
                10.15171/apb.2019.067
                6912190
                31857962
                e77a6608-b0ba-48a3-a78a-7921ac5570c5
                © 2019 The Author (s)

                This is an Open Access article distributed under the terms of the Creative Commons Attribution (CC BY), which permits unrestricted use, distribution, and reproduction in any medium, as long as the original authors and source are cited. No permission is required from the authors or the publishers.

                History
                : 07 February 2019
                : 24 June 2019
                : 25 June 2019
                Page count
                Figures: 2, Tables: 6, References: 42, Pages: 9
                Categories
                Research Article

                dermal drug delivery,finasteride,microemulsion,permeability,release

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