4.6 Article

Development and characterization of nano-emulsions and nano-emulgels for transdermal delivery of statins

期刊

EXPERT OPINION ON DRUG DELIVERY
卷 18, 期 6, 页码 789-801

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/17425247.2021.1867533

关键词

Nano-emulsions; nano-emulgels; oil-in-water; statins; transdermal; familial hypercholesterolemia

资金

  1. South African National Research Foundation (NRF): Competitive Support for Unrated Researchers (CSUR) [105913]
  2. Centre of Excellence for Pharmaceutical Sciences (Pharmacen(TM)) of the North-West University, Potchefstroom Campus, South Africa

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This research explores the development of nano-emulsions and nano-emulgels as potential alternative delivery systems for statins via transdermal administration. Characterization of the nano-formulations revealed efficient encapsulation of the statins and differential release profiles. These results suggest the potential benefits of nano-emulsions and nano-emulgels as alternative transdermal delivery systems for statins.
Background Oral administration of statins for the treatment of familial hypercholesterolemia results in poor therapeutic outcomes and patient compliance. An alternative administration route is proposed to circumvent the current limitations. This research is aimed at developing nano-emulsions and nano-emulgels as the ultimate potential delivery systems of statins for administration via the transdermal route. Methods Oil-in-water (o/w) nano-formulations (nano-emulsions and nano-emulgels) containing 2% (w/w) of the selected statin and 8% apricot kernel oil as oil phase were formulated. The nano-formulations were characterized using transmission electron microscopy (TEM), pH, viscosity, droplet size and zeta-potential. Results Nano-emulsions' and nano-emulgels' droplet size ranged between 114.23-169.83 nm and 149.83-267.53 nm, respectively. The addition of Carbopol (R) Ultrez 20 increased the nano-emulsions' viscosity (3.59-8.38 cP) resulting in the formation of nano-emulgels (viscosity: 1911.00-46,090.00 cP). The entrapment efficiency (90.77-99.55%) confirmed the incorporation of the statins. Membrane release studies indicated that statins were released at higher flux values in nano-emulsions compared to their respective nano-emulgels. Ex vivo (skin diffusion) studies indicated higher median values in the nano-emulgels compared to their nano-emulsion counterparts. Conclusions The results indicate the benefits of nano-emulsions and nano-emulgels as potential alternative delivery systems for the transdermal delivery of statins.

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