Algul Derya, Duman Gulengul, Ozdemir Samet, Acar Ebru Turkoz, Yener Gulgun
Department of Pharmaceutical Technology, Faculty of Pharmacy, Yeditepe University, Istanbul 34755, Turkey (D.A., G.D., S.O.), Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Yeditepe University, Istanbul 34755, Turkey (E.T.A.), and Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Istanbul 34116, Turkey (G.Y.).
J Cosmet Sci. 2018 May/Jun;69(3):165-173.
Encapsulation of active agents in solid lipid nanoparticles (SLNs) is an alternative to other controlled release systems for topical delivery. In this study, caffeine was encapsulated in SLNs to produce a delivery system with controlled release. Caffeine-loaded SLNs (Caf-SLNs) were prepared using the double emulsion method with homogenization and ultrasonication. The characterization studies were performed using dynamic light scattering (DLS), zeta potential, scanning electron microscopy (SEM), and differential scanning calorimetry (DSC) analyses. The encapsulation efficiency tests were performed using UV spectrophotometry. release studies were conducted using a dialysis bag technique and high-performance liquid chromatography (HPLC) for the quantification of caffeine (Caf). The results from the DLS analysis showed that all formulations had a polydispersity index <0.3 with particle sizes <210 nm. The DSC and SEM results showed that Caf was dispersed in the SLNs. The encapsulation efficiency was 49.22%. The release studies indicated that after an initial burst at 3 min, the SLNs released Caf in a controlled manner over a 6-h period. Taken together, the SLNs can be used as a carrier for the topical delivery of Caf.
将活性剂包裹于固体脂质纳米粒（SLNs）中是用于局部给药的其他控释系统的一种替代方法。在本研究中，咖啡因被包裹于固体脂质纳米粒中以制备具有控释功能的给药系统。采用双乳化法并结合均质化和超声处理制备了负载咖啡因的固体脂质纳米粒（Caf-SLNs）。使用动态光散射（DLS）、ζ电位、扫描电子显微镜（SEM）和差示扫描量热法（DSC）分析进行表征研究。使用紫外分光光度法进行包封率测试。采用透析袋技术和高效液相色谱（HPLC）进行释放研究以定量咖啡因（Caf）。DLS分析结果表明，所有制剂的多分散指数<0.3，粒径<210 nm。DSC和SEM结果表明，咖啡因分散于固体脂质纳米粒中。包封率为49.22%。释放研究表明，在最初3分钟的突释之后，固体脂质纳米粒在6小时内以控释方式释放咖啡因。综上所述，固体脂质纳米粒可用作咖啡因局部给药的载体。
