Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Eini Street, Cairo 11562, Egypt.
Mol Pharm. 2010 Apr 5;7(2):576-85. doi: 10.1021/mp900279c.
A fluoroquinolone/glucocorticoid combination for the treatment of bacterial keratitis in the form of mucoadhesive nanoparticle suspensions was developed to prolong the release and improve patient compliance. Gatifloxacin/prednisolone loaded nanoparticles were prepared using Eudragit RS 100 and RL 100 and coated with the bioadhesive polymer, hyaluronic acid. FT-IR and DSC studies revealed no interaction between gatifloxacin and prednisolone. The effects of the drug:polymer ratio (D:P) and the RS/RL ratio were studied. The obtained nanoparticles were distinct and spherical with a solid dense structure. They have average particle size range of 315.2 to 973.65 nm. Increasing the D:P ratio significantly lowered the entrapment efficiency for both drugs (p < 0.05). The nanoparticle suspensions revealed significantly prolonged drug release comparing to the free drugs (p < 0.05) with no burst effect. Increasing the polymer concentration and the Eudragit RS ratio significantly decreased the release efficiency values. Gatifloxacin showed anomalous release (n = 0.4943) from 1:1 D:P ratio nanoparticle suspension and Fickian diffusion mechanism (n < 0.45) from formulas prepared at higher D:P ratios. Gatifloxacin showed better bioavailability and sustained action in aqueous humor and corneal tissue from the nanoparticles compared to the commercial eye drops. The resulting nanoparticle suspension is promising in reducing dose frequency and improving patient compliance.
为了延长释放时间并提高患者的依从性，开发了一种将氟喹诺酮/糖皮质激素组合制成粘弹性纳米颗粒混悬剂的方法，用于治疗细菌性角膜炎。将加替沙星/泼尼松龙负载的纳米颗粒用 Eudragit RS 100 和 RL 100 制备，并涂覆生物粘附聚合物透明质酸。FT-IR 和 DSC 研究表明加替沙星和泼尼松龙之间没有相互作用。研究了药物：聚合物比（D：P）和 RS/RL 比的影响。获得的纳米颗粒是独特的球形，具有实心致密结构。它们的平均粒径范围为 315.2 至 973.65nm。D：P 比的增加显著降低了两种药物的包封效率（p < 0.05）。与游离药物相比，纳米颗粒混悬剂显示出明显延长的药物释放（p < 0.05），没有爆发效应。聚合物浓度和 Eudragit RS 比的增加显著降低了释放效率值。加替沙星在 1：1 D：P 比的纳米颗粒混悬剂中表现出异常释放（n = 0.4943），在较高 D：P 比的制剂中呈现菲克扩散机制（n < 0.45）。与商业滴眼液相比，纳米颗粒在房水中和角膜组织中显示出更好的生物利用度和持续作用。所得的纳米颗粒混悬剂有望减少剂量频率并提高患者的依从性。
