Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi, India.
J Drug Target. 2010 Apr;18(3):191-204. doi: 10.3109/10611860903338462.
This article describes the preparation and characterization of solid lipid nanoparticles (SLNs) prepared with stearic acid (SLN-A) and a mixture of stearic acid and Compritol (SLN-B) as lipid matrix and poloxamer-188 as surfactant, using sodium taurocholate and ethanol as co-surfactant mixture, with a view to applying the SLN in topical ocular drug delivery. The SLNs were prepared by o/w microemulsion technique and characterized by time-resolved particle size analysis, polydispersity index, zeta(zeta)-potential, differential scanning calorimetry (DSC), IR-spectroscopy, and wide-angle X-ray diffractometry (WAXD). The results obtained in these studies were compared with SLN prepared with stearic acid alone. IR, WAXD, and DSC studies revealed low-crystalline SLN and were having positive zeta-potentials after three-months of storage. Results indicated mixed lipid-matrix produced SLN with low-crystallinity and smaller particle sizes and higher drug entrapment compared with SLN prepared with stearic acid alone, therefore SLN-B would be suitable for the preparation of nanosuspension. Nanosuspensions were subjected to rheological and physicochemical evaluation, in vitro drug release and ex vivo corneal permeation studies and their effect were evaluated on corneal hydration-level. SLN composed of stearic acid and compritol would prove to be a good ocular drug delivery system considering the smaller particle size, particle size stability, and physiologically tolerable components.
本文描述了使用硬脂酸（SLN-A）和硬脂酸与 Compritol 的混合物（SLN-B）作为脂质基质，泊洛沙姆 188 作为表面活性剂，用牛磺胆酸钠和乙醇作为辅助表面活性剂混合物制备固体脂质纳米粒（SLN）的方法，并将其应用于眼部局部药物传递。SLN 是通过 o/w 微乳液技术制备的，并通过时间分辨粒径分析、多分散指数、Zeta（ζ）-电位、差示扫描量热法（DSC）、红外光谱（IR）和广角 X 射线衍射（WAXD）进行表征。这些研究的结果与单独使用硬脂酸制备的 SLN 进行了比较。IR、WAXD 和 DSC 研究表明，低结晶度的 SLN 在储存三个月后具有正 Zeta 电位。结果表明，与单独使用硬脂酸制备的 SLN 相比，混合脂质基质制备的 SLN 具有低结晶度、较小的粒径和较高的药物包封率，因此 SLN-B 适合制备纳米混悬剂。纳米混悬剂进行了流变学和物理化学评价、体外药物释放和离体角膜渗透研究，并评估了它们对角膜水合水平的影响。考虑到较小的粒径、粒径稳定性和生理上可耐受的成分，由硬脂酸和 Compritol 组成的 SLN 将被证明是一种良好的眼部药物传递系统。
