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微乳剂作为米诺地尔从凝胶中释放的增溶剂和渗透促进剂

Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels.

作者信息

Špaglová Miroslava, Čuchorová Mária, Čierna Martina, Poništ Silvester, Bauerová Katarína

机构信息

Department of Galenic Pharmacy, Faculty of Pharmacy, Comenius University, Odbojárov 10, SK-832 32 Bratislava, Slovakia.

Centre of Experimental Medicine, Slovak Academy of Sciences, Dúbravská cesta 9, SK-841 04 Bratislava, Slovakia.

出版信息

Gels. 2021 Mar 3;7(1):26. doi: 10.3390/gels7010026.

Abstract

Micro- and nanoemulsions are potential drug solubilizers and penetration enhancers through the high surfactant/co-surfactant content. This study aimed to evaluate the influence of minoxidil (MXD) solubilized in the microemulsions (MEs) on drug release by in vitro/ex vivo diffusion through the semi-permeable membrane Spectra/Por (Spectrum Laboratory, Gardena, CA, USA) and porcine ear skin. Moreover, a residual amount of drug in the skin after ex vivo diffusion was evaluated. The reference ME, lecithin-containing ME, and gelatin-containing ME were characterized in terms of their size, polydispersity index, density, viscosity, electrical conductivity and surface tension. Based on the in vitro diffusion, it can be argued that ME slowed down the drug release, while ME and ME have no significant effect compared to the sample, in which propylene glycol (PG) was used as a solubilizer. Determination of the residual drug amount in the skin after 6 h of the ex vivo permeation was demonstrated as the most valuable method to evaluate the effectiveness of the ME's application. The results indicate that the most optimal MXD permeation enhancers in alginate gel were the natural surfactants containing MEs. MXD solubilization in ME and ME had caused more than 5% of the drug remaining in the skin, which is almost a 1.5-fold higher amount compared to the reference gel.

摘要

微乳剂和纳米乳剂由于其高表面活性剂/助表面活性剂含量,是潜在的药物增溶剂和渗透促进剂。本研究旨在评估微乳剂(MEs)中溶解的米诺地尔(MXD)通过半透膜Spectra/Por(美国加利福尼亚州加迪纳市Spectrum Laboratory公司)和猪耳皮肤进行体外/离体扩散对药物释放的影响。此外,还评估了离体扩散后皮肤中药物的残留量。对参比微乳剂、含卵磷脂微乳剂和含明胶微乳剂的粒径、多分散指数、密度、粘度、电导率和表面张力进行了表征。基于体外扩散结果,可以认为微乳剂减缓了药物释放,而与以丙二醇(PG)作为增溶剂的样品相比,含卵磷脂微乳剂和含明胶微乳剂没有显著影响。离体渗透6小时后皮肤中残留药物量的测定被证明是评估微乳剂应用效果最有价值的方法。结果表明藻酸盐凝胶中最理想的米诺地尔渗透促进剂是含微乳剂的天然表面活性剂。米诺地尔在含卵磷脂微乳剂和含明胶微乳剂中的溶解导致皮肤中残留超过5%的药物,这几乎是参比凝胶中残留量的1.5倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b5df/7931056/ffb11c386f0c/gels-07-00026-g001.jpg

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