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用于吲哚美辛递送的壳聚糖包被脂质囊泡的增强稳定性和体外生物相容性

Enhanced Stability and In Vitro Biocompatibility of Chitosan-Coated Lipid Vesicles for Indomethacin Delivery.

作者信息

Abu Koush Angy, Popa Eliza Gratiela, Pricop Daniela Angelica, Nita Loredana, Foia Cezar-Ilie, Pauna Ana-Maria Raluca, Buca Beatrice Rozalina, Pavel Liliana Lacramioara, Mititelu-Tartau Liliana

机构信息

Department of Pharmacology, Faculty of Medicine, 'Grigore T. Popa' University of Medicine and Pharmacy, 700115 Iasi, Romania.

Department of Pharmaceutical Technology, Faculty of Pharmacy, 'Grigore T. Popa' University of Medicine and Pharmacy, 700115 Iasi, Romania.

出版信息

Pharmaceutics. 2024 Dec 9;16(12):1574. doi: 10.3390/pharmaceutics16121574.

Abstract

BACKGROUND

Lipid vesicles, especially those utilizing biocompatible materials like chitosan (CHIT), hold significant promise for enhancing the stability and release characteristics of drugs such as indomethacin (IND), effectively overcoming the drawbacks associated with conventional drug formulations.

OBJECTIVES

This study seeks to develop and characterize novel lipid vesicles composed of phosphatidylcholine and CHIT that encapsulate indomethacin (IND-ves), as well as to evaluate their in vitro hemocompatibility.

METHODS

The systems encapsulating IND were prepared using a molecular droplet self-assembly technique, involving the dissolution of lipids, cholesterol, and indomethacin in ethanol, followed by sonication and the gradual incorporation of a CHIT solution to form stable vesicular structures. The vesicles were characterized in terms of size, morphology, Zeta potential, and encapsulation efficiency and the profile release of drug was assessd. In vitro hemocompatibility was evaluated by measuring erythrocyte lysis and quantifying hemolysis rates.

RESULTS

The IND-ves exhibited an entrapment efficiency of 85%, with vesicles averaging 317.6 nm in size, and a Zeta potential of 24 mV, indicating good stability in suspension. In vitro release kinetics demonstrated an extended release profile of IND from the vesicles over 8 h, contrasting with the immediate release observed from plain drug solutions. The hemocompatibility assessment revealed that IND-ves exhibited minimal hemolysis, comparable to control groups, indicating good compatibility with erythrocytes.

CONCLUSIONS

IND-ves provide a promising approach for modified indomethacin delivery, enhancing stability and hemocompatibility. These findings suggest their potential for effective NSAID delivery, with further in vivo studies required to explore clinical applications.

摘要

背景

脂质囊泡,尤其是那些利用壳聚糖(CHIT)等生物相容性材料制成的脂质囊泡,在提高药物如吲哚美辛(IND)的稳定性和释放特性方面具有巨大潜力,能有效克服传统药物制剂的缺点。

目的

本研究旨在开发并表征由磷脂酰胆碱和壳聚糖组成的新型脂质囊泡(IND-囊泡),该囊泡包裹吲哚美辛,并评估其体外血液相容性。

方法

采用分子滴自组装技术制备包裹IND的体系,即将脂质、胆固醇和吲哚美辛溶解于乙醇中,随后进行超声处理,并逐步加入壳聚糖溶液以形成稳定的囊泡结构。对囊泡的大小、形态、Zeta电位和包封率进行表征,并评估药物的释放曲线。通过测量红细胞裂解和定量溶血率来评估体外血液相容性。

结果

IND-囊泡的包封率为85%,囊泡平均大小为317.6 nm,Zeta电位为24 mV,表明其在悬浮液中具有良好的稳定性。体外释放动力学表明,IND从囊泡中的释放曲线在8小时内呈缓释状态,这与普通药物溶液的即时释放形成对比。血液相容性评估显示,IND-囊泡的溶血作用极小,与对照组相当,表明其与红细胞具有良好的相容性。

结论

IND-囊泡为改进吲哚美辛的递送提供了一种有前景的方法,提高了稳定性和血液相容性。这些发现表明其在有效递送非甾体抗炎药方面的潜力,需要进一步的体内研究来探索其临床应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/484b/11676990/28cf499238ee/pharmaceutics-16-01574-g001.jpg

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