Varshosaz Jaleh, Hajhashemi Valiollah, Soltanzadeh Sindokht
Department of Pharmaceutics, Faculty of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan 81746-73461, Iran.
J Drug Deliv. 2011;2011:571272. doi: 10.1155/2011/571272. Epub 2011 Nov 17.
Previous reports show ineffective transdermal delivery of ketorolac by nanostructured lipid carriers (NLCs). The aim of the present work was enhancement of transdermal delivery of ketorolac by another colloidal carriers, lipid nanocapsules (LNCs). LNCs were prepared by emulsification with phase transition method and mixed in a Carbomer 934P gel base with oleic acid or propylene glycol as penetration enhancers. Permeation studies were performed by Franz diffusion cell using excised rat abdominal skin. Aerosil-induced rat paw edema model was used to investigate the in vivo performance. LNCs containing polyethylene glycol hydroxyl stearate, lecithin in Labrafac as the oily phase, and dilution of the primary emulsion with 3.5-fold volume of cold water produced the optimized nanoparticles. The 1% Carbomer gel base containing 10% oleic acid loaded with nanoparticles enhanced and prolonged the anti-inflammatory effects of this drug to more than 12 h in Aerosil-induced rat paw edema model.
先前的报道显示,酮咯酸通过纳米结构脂质载体(NLCs)进行经皮递送的效果不佳。本研究的目的是通过另一种胶体载体——脂质纳米囊(LNCs)来增强酮咯酸的经皮递送。脂质纳米囊通过相转变乳化法制备,并与含有油酸或丙二醇作为渗透促进剂的卡波姆934P凝胶基质混合。采用Franz扩散池,使用切除的大鼠腹部皮肤进行渗透研究。采用气溶素诱导的大鼠爪水肿模型来研究体内性能。含有聚乙二醇羟基硬脂酸酯、卵磷脂作为油相的Labrafac以及用3.5倍体积的冷水稀释初乳制备出了优化的纳米颗粒。在气溶素诱导的大鼠爪水肿模型中,含有10%油酸的1%卡波姆凝胶基质负载纳米颗粒增强并延长了该药物的抗炎作用至超过12小时。