Abstract

Traditional eye drops used for topically administering drugs have poor ocular bioavailability due to the biological barriers of the eye. There is an interest to design and develop novel drug delivery systems that would extend the precorneal residence time, reduce the frequency of administration and decrease dose-related toxicity. This study aimed to prepare Nanoparticles of Gemifloxacin Mesylate and incorporate them into an in situ gel. The nanoparticles were prepared by ionic gelation technique, using 3² factorial design. Sodium tripolyphosphate (STPP) was used to crosslink Chitosan. The optimized formulation of the nanoparticles (GF4) contained 0.15% Gemifloxacin Mesylate, 0.15% Chitosan and 0.20% STPP, producing 71 nm particle size and 81.11% entrapment efficiency. The prepared nanoparticles showed biphasic release, with an initial burst release of 15% in 1.0 hr and a cumulative drug release of 90.53% at the end of 24 hrs. After that, the prepared nanoparticles were incorporated into an in situ gel, using Poloxamer 407, producing a sustained drug release with efficient antimicrobial activity against gram-positive and gram-negative bacteria as confirmed by the cup plate method.

摘要

由于眼睛的生物屏障，用于局部给药的传统滴眼液具有较差的眼部生物利用度。有兴趣设计和开发新的药物递送系统，以延长角膜前停留时间，减少给药频率并降低剂量相关毒性。本研究旨在制备甲磺酸吉米沙星纳米颗粒并将其掺入原位凝胶中。采用离子凝胶技术制备纳米粒子，采用 3 ²析因设计。三聚磷酸钠 (STPP) 用于交联壳聚糖。纳米颗粒 (GF4) 的优化配方含有 0.15% 甲磺酸吉米沙星、0.15% 壳聚糖和 0.20% STPP，产生 71 nm 粒径和 81.11% 的包封率。制备的纳米颗粒显示双相释放，1.0 小时内初始突释为 15%，24 小时结束时累积药物释放为 90.53%。之后，使用 Poloxamer 407 将制备的纳米颗粒掺入原位凝胶中，产生持续的药物释放，并通过杯板法证实对革兰氏阳性和革兰氏阴性菌具有有效的抗菌活性。