Development of transferosomes for topical ocular drug delivery of curcumin

IF 4.4 2区医学 Q1 PHARMACOLOGY & PHARMACY European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2024-10-18 DOI:10.1016/j.ejpb.2024.114535

Geisa Nascimento Barbalho , Stefan Brugger , Christian Raab , Jara-Sophie Lechner , Taís Gratieri , Cornelia M. Keck , Ilva D. Rupenthal , Priyanka Agarwal

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Abstract

Background

Transferosomes (TFS) are ultra-deformable elastic bilayer vesicles that have previously been used to enhance gradient driven penetration through the skin. This study aimed to evaluate the potential of TFS for topical ocular drug delivery and to compare their penetration enhancing properties in different ocular tissues.

Methods

Curcumin-loaded TFS were prepared using Tween 80 as the edge activator. Drug release and precorneal retention of the TFS were evaluated in vitro, while their ocular biocompatibility and bioavailability were evaluated ex vivo using a curcumin solution in medium chain triglycerides as the oily control.

Results

The TFS had a narrow size distribution with a particle size less than 150 nm and an entrapment efficiency greater than 99.96 %. Burst release from the TFS was minimal and the formulation showed good corneal biocompatibility. Moreover, enhanced corneal and conjunctival drug penetration with significantly greater and deeper drug delivery was observed with TFS.

Conclusion

TFS offer a promising platform for ocular delivery of hydrophobic drugs. This study, for the first time, elucidates the effect of tissue morphology and osmotic gradients on drug penetration in different ocular tissues.

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开发用于姜黄素局部眼部给药的转移体。

背景：转运体（TFS）是一种超可变形的弹性双层囊泡，以前曾被用于增强皮肤的梯度渗透。本研究旨在评估 TFS 用于眼部局部给药的潜力，并比较其在不同眼部组织中的渗透增强特性：方法：使用吐温 80 作为边缘活化剂制备了姜黄素负载 TFS。方法：使用吐温 80 作为边缘活化剂制备姜黄素负载 TFS，在体外对 TFS 的药物释放和角膜前保留进行了评估，同时使用中链甘油三酯中的姜黄素溶液作为油性对照，在体外对 TFS 的眼部生物相容性和生物利用度进行了评估：TFS 的粒度分布较窄，粒径小于 150 nm，截留效率大于 99.96%。TFS 的迸发释放量极低，配方具有良好的角膜生物相容性。此外，TFS 还增强了角膜和结膜的药物渗透性，在所有眼部组织中的给药量和给药深度都明显增加：结论：TFS 为疏水性药物的眼部给药提供了一个前景广阔的平台。本研究首次阐明了组织形态和渗透梯度对药物在不同眼组织中渗透的影响。

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来源期刊

European Journal of Pharmaceutics and Biopharmaceutics 医学-药学

CiteScore

8.80

自引率

4.10%

发文量

211

审稿时长

36 days

期刊介绍： The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.