Mandawgade Sagar D, Patravale Vandana B
Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, Maharashtra, India.
Int J Pharm. 2008 Nov 3;363(1-2):132-8. doi: 10.1016/j.ijpharm.2008.06.028. Epub 2008 Jul 6.
The aim of this investigation was to develop solid lipid nanoparticles (SLNs) from indigenous, natural solid lipids by using a simple microemulsion technique. Furthermore, the aim was to characterize these SLNs and evaluate its potential in the topical delivery of a lipophilic drug, tretinoin (TRN). The developed SLNs were characterized for particle size, polydispersity index, entrapment efficiency of TRN and morphology. TRN-loaded SLN-based topical gels were formulated and the gels were evaluated comparatively with the commercial product with respect to primary skin irritation, in vitro occlusivity and skin permeation. The results of the study showed mean particle size <100nm of the SLN dispersions with the novel lipids. Up to 46% of drug entrapment in the lipids was attained. Lesser skin irritancy, greater skin tolerance, occlusivity and slow drug release was observed with the developed TRN-loaded SLN-based gels than the commercial product. The research work could be concluded as successful production of SLNs using highly purified stearine fraction of natural solid lipids. The results of the characterization and evaluation established the safety for use, suitability and compatibility of indigenous natural lipids as a novel excipient.
本研究的目的是通过简单的微乳液技术,利用本土天然固体脂质制备固体脂质纳米粒(SLNs)。此外,目的是对这些SLNs进行表征,并评估其在亲脂性药物维甲酸(TRN)局部给药中的潜力。对所制备的SLNs进行粒径、多分散指数、TRN包封率和形态表征。制备了基于载TRN的SLN的局部凝胶,并就原发性皮肤刺激性、体外封闭性和皮肤渗透性方面与市售产品进行了比较评估。研究结果表明,新型脂质的SLN分散体平均粒径<100nm。脂质中药物包封率高达46%。与市售产品相比,所制备的基于载TRN的SLN凝胶表现出较低的皮肤刺激性、较高的皮肤耐受性、封闭性和缓慢的药物释放。该研究工作可得出结论:利用天然固体脂质的高纯度硬脂酸馏分成功制备了SLNs。表征和评估结果确定了本土天然脂质作为新型辅料使用的安全性、适用性和相容性。