Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: formulation characterization and assessment of dermal delivery compared to referent ointment

Publication date: Available online 13 August 2019Source: International Journal of PharmaceuticsAuthor(s): Vedrana Savić, Tanja Ilić, Ines Nikolić, Bojan Marković, Bojan Čalija, Nebojša Cekić, Snežana SavićAbstractNanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54±92.38 ng/cm2), followed by NE (128.17±48.87 ng/cm2) and Protopic® (77.61±43.25 ng/cm2). Contrary, the highest permeation rate through full-thicknes...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research