A Nanomicelles Platform Delivery System for Water-Insoluble Corticosteroid to Treat Anterior Uveitis.

IF 5 3区医学 Q1 PHARMACOLOGY & PHARMACY

AAPS Journal Pub Date : 2025-07-22 DOI:10.1208/s12248-025-01103-z

Priyadarshini Sathe, Srujana Mosalikanti Sai Kameshwari, Jayabalan Nirmal

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引用次数: 0

Abstract

Difluprednate is marketed as an emulsion due to its poor aqueous solubility. Emulsions are known to cause ocular discomfort and require frequent dosing to show therapeutic activity. Nanomicelles are well known to improve the solubility and permeation of water-insoluble drugs. Therefore, to enhance the water solubility and reduce the dosing frequency by improving difluprednate permeation across the cornea, we formulated nanomicelles. Difluprednate loaded nanomicelles (Dicel) was prepared by thin film hydration method and optimized using Box-Behnken design. The Dicel formulated had a particle size, polydispersity index, zeta potential and entrapment efficiency of 21.9 nm, 0.15, -7.55 mV and 75.4%, respectively. Transmission electron microscopy analysis showed spherical nanomicelles. The Dicel showed a sustained release profile for 48 h. The difluprednate permeation across the cornea from Dicel was enhanced by twofold compared to commercially available emulsion. Also, it was found to be stable upon dilution with simulated tear fluid and was biocompatible. Further, Dicel improved the anti-inflammatory activity of difluprednate at one and two times a day administration compared to four times a day administration of difluprednate emulsion. The present study highlights the role of topical nanomicelles in delivering difluprednate, which is better than the existing marketed emulsion in the management of ocular inflammation.

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水不溶性皮质类固醇纳米胶束平台递送系统治疗葡萄膜前炎。

由于其水溶性差，二氟泼尼酯作为乳剂销售。乳剂会引起眼部不适，需要经常给药才能显示治疗效果。众所周知，纳米胶束可以提高水不溶性药物的溶解度和渗透性。因此，为了通过改善二氟泼尼酯在角膜中的渗透来提高水溶性并减少给药频率，我们配制了纳米胶束。采用薄膜水化法制备了负载双氟乙酸酯的纳米胶束（Dicel），并采用Box-Behnken设计对其进行了优化。Dicel的粒径为21.9 nm，多分散性指数为0.15，zeta电位为-7.55 mV，包封效率为75.4%。透射电镜分析显示为球形纳米胶束。Dicel显示了48小时的缓释特性。与市售的乳剂相比，Dicel的二氟泼尼酯在角膜中的渗透增强了两倍。此外，用模拟泪液稀释后发现它是稳定的，并且具有生物相容性。此外，与每天给药四次的二氟泼尼酯乳剂相比，每天给药一次和两次的Dicel提高了二氟泼尼酯的抗炎活性。本研究强调了局部纳米胶束在传递二氟泼尼酯方面的作用，它比现有的市场上销售的乳剂在治疗眼部炎症方面更好。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

AAPS Journal 医学-药学

CiteScore

7.80

自引率

4.40%

发文量

109

审稿时长

1 months

期刊介绍： The AAPS Journal, an official journal of the American Association of Pharmaceutical Scientists (AAPS), publishes novel and significant findings in the various areas of pharmaceutical sciences impacting human and veterinary therapeutics, including: · Drug Design and Discovery · Pharmaceutical Biotechnology · Biopharmaceutics, Formulation, and Drug Delivery · Metabolism and Transport · Pharmacokinetics, Pharmacodynamics, and Pharmacometrics · Translational Research · Clinical Evaluations and Therapeutic Outcomes · Regulatory Science We invite submissions under the following article types: · Original Research Articles · Reviews and Mini-reviews · White Papers, Commentaries, and Editorials · Meeting Reports · Brief/Technical Reports and Rapid Communications · Regulatory Notes · Tutorials · Protocols in the Pharmaceutical Sciences In addition, The AAPS Journal publishes themes, organized by guest editors, which are focused on particular areas of current interest to our field.