Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) enriched hydrogels for transdermal delivery of flurbiprofen: formulation, in vitro characterisation, pharmacokinetic and pharmacodynamic studies in animals

K. Bhaskar
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Abstract

Aqueous dispersions of flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenisation followed by sonication technique were prepared and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterised for particle size, DSC, shape and surface morphology, in vitro drug release, rheological behaviour and in vivo studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1) and NLC gel (B1) for 24h were evaluated. The Cmax of the NLC gel formulation was 38.67 ± 2.77 μg/ml, which was significantly higher than the SLN gel formulation (Cmax = 21.79 ± 2.96 μg/ml). The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the carrageenan-induced paw edema in rat was significantly higher for NLC gel and SLN gel formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24h.
固体脂质纳米颗粒(SLN)和纳米结构脂质载体(NLC)富集水凝胶用于氟比洛芬透皮给药:配方、体外表征、动物药代动力学和药效学研究
通过热均质和超声技术制备氟比洛芬固体脂质纳米颗粒(flflln)和氟比洛芬纳米结构脂质载体(FLUNLC)的水分散体,然后将其掺入新制备的水凝胶中进行透皮给药。它们的特点是粒度,DSC,形状和表面形态,体外药物释放,流变行为和体内研究。用SLN凝胶(A1)和NLC凝胶(B1)给药24h,观察氟比洛芬在大鼠体内的药动学。NLC凝胶制剂的Cmax为38.67±2.77 μg/ml,显著高于SLN凝胶制剂(Cmax = 21.79±2.96 μg/ml)。口服氟比洛芬凝胶制剂的生物利用度提高4.4倍。NLC凝胶和SLN凝胶制剂对卡拉胶所致大鼠足跖水肿的抗炎作用明显高于口服氟比洛芬。SLN和NLC的分散体和富含SLN和NLC的凝胶在24小时内均具有持续的药物释放。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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