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Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2021-02-05 , DOI: 10.2147/dddt.s293127 Rana M Gebreel 1 , Noha A Edris 2 , Hala M Elmofty 2 , Mina I Tadros 3, 4 , Mohamed A El-Nabarawi 3 , Doaa H Hassan 1
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2021-02-05 , DOI: 10.2147/dddt.s293127 Rana M Gebreel 1 , Noha A Edris 2 , Hala M Elmofty 2 , Mina I Tadros 3, 4 , Mohamed A El-Nabarawi 3 , Doaa H Hassan 1
Affiliation
Aim: 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.
Methods: NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 21 .41 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 (Q30min) and 12 hours (Q12h), drug percentage permeated through goat corneas after 30 min (P30min) and 12 hours (P12h) 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 Pseudomonas aeruginosa, and histopathological changes.
Results: 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 Q30min (10.96% and 16.65%) and P30min (17.39% and 21.05%) and promising Q12h (58.23% and 71.20%) and P12h (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.
Conclusion: G3 and G4 are potential ocular delivery systems for NFX.
Keywords: norfloxacin, nanoparticles, PLGA, ocular delivery, Pseudomonas keratitis
中文翻译：
PLGA 纳米颗粒载水凝胶的开发和表征，用于诺氟沙星在治疗假单胞菌角膜炎中的持续眼部给药：一项实验研究
目的：诺氟沙星 (NFX) 的眼部生物利用度较低。目前的工作旨在开发负载 NFX 的纳米颗粒 (NP) 水凝胶，以提高 NFX 的眼部潜力，最大限度地减少频繁滴注的需要并降低不良副作用。
方法：根据 2 1 .4 1全因子设计，使用两种类型的聚乳酸-乙醇酸 (PLGA) 聚合物和四种（药物：聚合物），通过双乳液/溶剂蒸发技术开发负载 NFX 的纳米颗粒。比率。对纳米颗粒的粒径 (PS)、多分散指数 (PDI)、zeta 电位 (ZP)、药物包封率 (EE%)、30 分钟 (Q 30min ) 和 12 小时 (Q 12h ) 后释放的药物百分比进行评估)、30 分钟 (P 30min ) 和 12 小时 (P 12h )后通过山羊角膜渗透的药物百分比和形态。统计选择了两个配方并将其纳入基于羟丙基甲基纤维素 (HPMC) 的水凝胶中；G1 - G4。评估后一种系统的外观、透明度、pH、铺展性、流变学、释放的药物百分比、渗透的药物百分比、对铜绿假单胞菌的抗菌活性和组织病理学变化。
结果：所选纳米颗粒（NP2 和 NP6）呈球形，具有合适的 PS（392.02 nm 和 190.51 nm）和 PDI（0.17 和 0.18），高 ZP 幅度（- 30.43 mV 和 - 33.62 mV），高 EE% （79.24% 和 91.72%），低 Q 30min(10.96% 和 16.65%) 和 P 30min (17.39% 和 21.05%) 和有希望的 Q 12h (58.23% 和 71.20%) 和 P 12h (53.31% 和 65.01%)，分别。开发了基于透明、可涂抹、可耐受、假塑性和触变性 HPMC 的水凝胶。它们显示出更长的药物释放和药物渗透曲线。载有 NP2 和 NP6 的水凝胶（分别为 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。
结论： G3 和 G4 是 NFX 潜在的眼部传递系统。
关键词：诺氟沙星，纳米颗粒，PLGA，眼部给药，假单胞菌角膜炎
更新日期：2021-02-05
Methods: NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 21 .41 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 (Q30min) and 12 hours (Q12h), drug percentage permeated through goat corneas after 30 min (P30min) and 12 hours (P12h) 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 Pseudomonas aeruginosa, and histopathological changes.
Results: 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 Q30min (10.96% and 16.65%) and P30min (17.39% and 21.05%) and promising Q12h (58.23% and 71.20%) and P12h (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.
Conclusion: G3 and G4 are potential ocular delivery systems for NFX.
Keywords: norfloxacin, nanoparticles, PLGA, ocular delivery, Pseudomonas keratitis
中文翻译：
PLGA 纳米颗粒载水凝胶的开发和表征，用于诺氟沙星在治疗假单胞菌角膜炎中的持续眼部给药：一项实验研究
目的：诺氟沙星 (NFX) 的眼部生物利用度较低。目前的工作旨在开发负载 NFX 的纳米颗粒 (NP) 水凝胶，以提高 NFX 的眼部潜力，最大限度地减少频繁滴注的需要并降低不良副作用。
方法：根据 2 1 .4 1全因子设计，使用两种类型的聚乳酸-乙醇酸 (PLGA) 聚合物和四种（药物：聚合物），通过双乳液/溶剂蒸发技术开发负载 NFX 的纳米颗粒。比率。对纳米颗粒的粒径 (PS)、多分散指数 (PDI)、zeta 电位 (ZP)、药物包封率 (EE%)、30 分钟 (Q 30min ) 和 12 小时 (Q 12h ) 后释放的药物百分比进行评估)、30 分钟 (P 30min ) 和 12 小时 (P 12h )后通过山羊角膜渗透的药物百分比和形态。统计选择了两个配方并将其纳入基于羟丙基甲基纤维素 (HPMC) 的水凝胶中；G1 - G4。评估后一种系统的外观、透明度、pH、铺展性、流变学、释放的药物百分比、渗透的药物百分比、对铜绿假单胞菌的抗菌活性和组织病理学变化。
结果：所选纳米颗粒（NP2 和 NP6）呈球形，具有合适的 PS（392.02 nm 和 190.51 nm）和 PDI（0.17 和 0.18），高 ZP 幅度（- 30.43 mV 和 - 33.62 mV），高 EE% （79.24% 和 91.72%），低 Q 30min(10.96% 和 16.65%) 和 P 30min (17.39% 和 21.05%) 和有希望的 Q 12h (58.23% 和 71.20%) 和 P 12h (53.31% 和 65.01%)，分别。开发了基于透明、可涂抹、可耐受、假塑性和触变性 HPMC 的水凝胶。它们显示出更长的药物释放和药物渗透曲线。载有 NP2 和 NP6 的水凝胶（分别为 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。
结论： G3 和 G4 是 NFX 潜在的眼部传递系统。
关键词：诺氟沙星，纳米颗粒，PLGA，眼部给药，假单胞菌角膜炎
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