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载有米诺地尔的纳米结构脂质载体(NLC):局部用制剂的表征及流变行为

Minoxidil-loaded nanostructured lipid carriers (NLC): characterization and rheological behaviour of topical formulations.

作者信息

Silva A C, Santos D, Ferreira D C, Souto E B

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Porto University, Portugal.

出版信息

Pharmazie. 2009 Mar;64(3):177-82.

Abstract

Lipid nanoparticles are used as biocompatible carriers for several types of drugs intended for pharmaceutical, cosmetic, and biochemical purposes. The wide range of lipids and surfactants available for the production of such particles turns these carriers highly suitable for distinct applications (topical, dermal and transdermal, parenteral, pulmonary, and oral administration). This work describes the development of a special type of lipid particles, namely nanostructured lipid carriers (NLC), for minoxidil as an alternative to conventional topical alcoholic solutions. NLC were composed of stearic acid and oleic acid, being the matrix stabilized with poloxamer 188 in aqueous dispersion. To develop a suitable topical formulation, lipid dispersions were further mixed with freshly prepared Carbopol or perfluorocarbon based hydrogels. Minoxidil-loaded NLC were approximately 250 nm in size before the entrapment within the gel network and remained below 500 nm after mixing with both types of hydrogels. The occurrence of minoxidil crystallization in the aqueous phase of lipid dispersions was discarded under analysis by light microscopy and by scanning electron microscopy. Differential scanning calorimetry was used to assess the recrystallization index (i.e. measure of the percentage of lipid matrix that is crystallized) of the particles, which was shown to be 62% for minoxidil-free dispersions and 68% for minoxidil-loaded NLC dispersions. Rheological analysis of hydrogels containing NLC dispersions showed typical pseudoplastic behaviour which makes them suitable for topical purposes.

摘要

脂质纳米颗粒被用作多种药物的生物相容性载体,这些药物用于制药、化妆品和生化目的。可用于生产此类颗粒的脂质和表面活性剂种类繁多,使这些载体非常适合不同的应用(局部、皮肤和透皮、肠胃外、肺部和口服给药)。这项工作描述了一种特殊类型的脂质颗粒,即纳米结构脂质载体(NLC)的开发,用于替代传统的局部酒精溶液来载运米诺地尔。NLC由硬脂酸和油酸组成,在水分散体中用泊洛沙姆188稳定基质。为了开发合适的局部制剂,将脂质分散体与新制备的基于卡波姆或全氟化碳的水凝胶进一步混合。在被包裹在凝胶网络之前,载有米诺地尔的NLC尺寸约为250纳米,与两种类型的水凝胶混合后仍低于500纳米。通过光学显微镜和扫描电子显微镜分析,排除了脂质分散体水相中米诺地尔结晶的发生。差示扫描量热法用于评估颗粒的重结晶指数(即结晶的脂质基质百分比的测量值),结果显示,不含米诺地尔的分散体为62%,载有米诺地尔的NLC分散体为68%。对含有NLC分散体的水凝胶进行流变学分析,结果显示出典型的假塑性行为,这使其适合局部应用。

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