Formulation of Natural Oil Nano-Emulsions for the Topical Delivery of Clofazimine, Artemisone and Decoquinate.

Pharm Res

Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Private Bag X6001, Potchefstroom, 2520, South Africa.

Published: August 2018

AI Article Synopsis

  • The study focused on creating nano-emulsions with natural oils to enhance the topical delivery of three active pharmaceutical ingredients (APIs): clofazimine (CLF), artemisone (ATM), and decoquinate (DQ).
  • The formulation demonstrated effective skin penetration and showed no toxicity to human keratinocyte cells, alongside the ability to inhibit Mycobacterium tuberculosis in lab tests.
  • These findings suggest that natural oil nano-emulsions could serve as a supplementary treatment for cutaneous tuberculosis (CTB).

Article Abstract

Purpose: The aim of this study was to formulate nano-emulsions comprising natural oils and the active pharmaceutical ingredients (APIs) clofazimine (CLF), artemisone (ATM) and decoquinate (DQ) in order to determine effectiveness of the nano-emulsions for topical delivery of the APIs. The APIs alone do not possess suitable physicochemical properties for topical drug delivery.

Methods: Nano-emulsions were formulated with olive and safflower oils encapsulating the APIs. Skin diffusion and tape stripping studies were performed. By using the lactate dehydrogenase (LDH) assay, in vitro toxicity studies were carried out on immortalized human keratinocytes (HaCaT) cell line to determine cytotoxicities due to the APIs and the nano-emulsions incorporating the APIs.

Results: The nano-emulsions were effective in delivering the APIs within the stratum corneum-epidermis and the epidermis-dermis, were non-cytotoxic towards HaCaT cell lines (p < 0.05) and inhibited Mycobacterium tuberculosis in vitro.

Conclusion: Natural oil nano-emulsions successfully deliver CLF, ATM and DQ and in principle could be used as supplementary topical treatment of cutaneous tuberculosis (CTB). Graphical Abstract ᅟ.

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Source
http://dx.doi.org/10.1007/s11095-018-2471-9DOI Listing

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