Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt.
Department of Ophthalmology, Faculty of Medicine, Cairo University, Cairo, Egypt.
Drug Des Devel Ther. 2021 Feb 5;15:399-418. doi: 10.2147/DDDT.S293127. eCollection 2021.
Norfloxacin (NFX) has low ocular bioavailability. The current work aimed to develop NFX-loaded nanoparticle (NP)-laden hydrogels to improve the ocular potential of NFX, minimize the need for frequent instillations and lower undesirable side effects.
NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 2.4 full factorial design, using two types of polylactic-co-glycolic acid (PLGA) polymer and four (drug: polymer) ratios. NPs were evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), drug entrapment efficiency percentage (EE%), drug percentage released after 30 min (Q) and 12 hours (Q), drug percentage permeated through goat corneas after 30 min (P) and 12 hours (P) and morphology. Two formulae were statistically selected and incorporated into hydroxypropyl methylcellulose (HPMC)-based hydrogels; G1 - G4. The latter systems were evaluated for appearance, clarity, pH, spreadability, rheology, drug percentages released, drug percentages permeated, antimicrobial activity against , and histopathological changes.
The selected NPs (NP2 and NP6) were spherical in shape and possessed suitable PS (392.02 nm and 190.51 nm) and PDI (0.17 and 0.18), high magnitude of ZP (-30.43 mV and -33.62 mV), high EE% (79.24% and 91.72%), low Q (10.96% and 16.65%) and P (17.39% and 21.05%) and promising Q (58.23% and 71.20%) and P (53.31% and 65.01%), respectively. Clear, spreadable, tolerable, pseudoplastic, and thixotropic HPMC-based hydrogels were developed. They showed more prolonged drug release and drug permeation profiles. NP2- and NP6-laden hydrogels (G3 and G4 systems, respectively) had promising antibacterial activity, and reasonable histopathological safety.
G3 and G4 are potential ocular delivery systems for NFX.
诺氟沙星（NFX）的眼部生物利用度较低。本研究旨在开发载诺氟沙星的纳米颗粒（NP）载药纳米凝胶，以提高 NFX 的眼部潜力，减少频繁滴眼的需求，并降低不良的副作用。
采用双乳液/溶剂蒸发技术，根据 2.4 全因子设计，使用两种类型的聚乳酸-聚乙二醇酸（PLGA）聚合物和四种（药物：聚合物）比例，制备 NFX 载 NP。对 NP 的粒径（PS）、多分散指数（PDI）、Zeta 电位（ZP）、药物包封效率百分比（EE%）、30 分钟和 12 小时后的药物释放百分比（Q）、30 分钟和 12 小时后的药物透过山羊角膜的百分比（P）和形态进行评价。从统计学上选择两种配方并纳入羟丙基甲基纤维素（HPMC）基水凝胶中；G1-G4。对后者系统进行外观、透明度、pH 值、铺展性、流变学、药物释放百分比、药物透过百分比、对 的抗菌活性和组织病理学变化进行评价。
选择的 NPs（NP2 和 NP6）呈球形，具有合适的 PS（392.02nm 和 190.51nm）和 PDI（0.17 和 0.18）、高 ZP（-30.43mV 和-33.62mV）、高 EE%（79.24%和 91.72%）、低 Q（10.96%和 16.65%）和 P（17.39%和 21.05%）和有前景的 Q（58.23%和 71.20%）和 P（53.31%和 65.01%）。开发了透明、可铺展、可耐受、假塑性和触变性的 HPMC 基水凝胶。它们显示出更持久的药物释放和药物渗透曲线。载有 NP2 和 NP6 的水凝胶（G3 和 G4 系统）具有良好的抗菌活性和合理的组织病理学安全性。
G3 和 G4 是 NFX 的潜在眼部给药系统。
