溴芬酸钠负载Pluronic纳米胶束的研制:表征及角膜渗透研究。

Miral Patel, Nithun Saha, Shruti Patel, Priyanka Ahlawat, Abhay Dharamsi, Asha Patel
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引用次数: 1

摘要

背景:白内障是世界范围内视力损害和可预防性失明的主要原因。白内障摘除手术涉及各种术后并发症,如疼痛和炎症。目的:本研究的目的是筛选聚合物的浓度和优化配方成分,以开发具有纳米级表征的pluronic胶束,并用于增强角膜渗透的研究。方法:为了优化,采用中心复合设计,研究Pluronic f127浓度(X1)和透明质酸浓度(X2)对选择响应(Y 1)胶束大小、(Y 2)包封效率、(Y 3)粘度的影响。冻干粉末用于物理表征。结果:以5%w/v Pluronic F127和0.2%w/v透明质酸为最优配方,胶束尺寸为38.74±4.12nm, zeta电位为-17.6±0.1 mV。8 h体外释药率为91.72±1.2 %。表面形貌显示胶束呈球形。眼部刺激试验表明,该制剂安全、无刺激性。通过切除的兔角膜进行的体外角膜渗透研究表明,与纳米胶束中含有相同量的药物的水悬浮液相比,在没有角膜损伤的情况下,眼可用性增加了1.5倍。结论:综上所述,Pluronic纳米胶束可作为溴芬酸钠的递送平台。
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Development of Bromfenac Sodium Loaded Pluronic Nanomicelles: Characterization and Corneal Permeation Study.

Background: The Cataract is the leading cause of visual impairment and preventable blindness worldwide. Cataract removal surgery involves various post-operative complications like pain and inflammation.

Objectives: The objective of this study is to screen the polymer concentration as well as optimize the formulation components to develop the pluronic micelles with nanosized characterization and for enhanced corneal permeation study.

Methodology: For optimization, Central Composite design was employed to study the effect of independent variables, concentration of Pluronic F 127 (X1) and the concentration of Hyaluronic acid (X2) on chosen responses (Y 1 ) Micelle size, (Y 2 ) Entrapment Efficiency, (Y 3 ) Viscosity. The lyophilised powder was used for physical characterisation.

Results: The formulation containing 5%w/v Pluronic F127 and 0.2%w/v Hyaluronic acid was the optimised composition with micelle size and zeta potential 38.74±4.12nm and -17.6±0.1 mV respectively. In-vitro drug release was found to be 91.72±1.2 percentage in 8 hours. Surface morphology revealed micelles were spherical in shape. Ocular irritancy study showed that formulation was safe and non-irritant. In vitro corneal permeation studies through excised rabbit cornea indicated 1.5 fold increase in ocular availability without corneal damage compared to an aqueous suspension containing the same amount of drug in nanomicelles.

Conclusion: In a nutshell, Pluronic Nanomicelles would be a platform for the delivery of Bromfenac Sodium.

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