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Nanostructured gel for topical delivery of azelaic acid: Designing, characterization, and in-vitro evaluation

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Abstract The study is designed to formulate, optimize and evaluate Azelaic acid loaded nano-structured lipid carrier (NLCs) with an aim to enhance its skin targeting, retention, and achieve sustained release… Click to show full abstract

Abstract The study is designed to formulate, optimize and evaluate Azelaic acid loaded nano-structured lipid carrier (NLCs) with an aim to enhance its skin targeting, retention, and achieve sustained release with reduced drug related side effects. NLCs were formulated by melt emulsification and ultra-sonication technique and optimized employing 33 full factorial design taking lipid:drug ratio, surfactant concentration and sonication time as independent variables with particle size (PS) and entrapment efficiency (EE) as dependent variables. The optimized formulation (F23) exhibited spherical surfaced stable nano particles of 49.6 ± 1.24 nm size and 83.4 ± 2.14% EE. Formulation F23 was then incorporate to aloe-vera based carbopol gel and evaluated for its physiological properties, drug content, in-vitro release and skin distribution (fluorescent microscopy) analysis. The gel was found to be non-irritating, homogenous, with optimum moisture content, spreadability and occlusivity. In-vitro permeation studies showed NLC preparation to markedly enhance the dug's skin retention in comparison to drug suspended in gel and marketed preparation. The skin distribution studies employing rhodamine 6G further confirmed the permeation of NLCs to the deeper layers of skin. The experimental findings suggested that NLCs could serve as a promising carrier for site specific targeting with better skin retention abilities.

Keywords: drug; gel topical; azelaic acid; nanostructured gel; topical delivery

Journal Title: Journal of Drug Delivery Science and Technology
Year Published: 2018

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