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评价乙二醛二酐与二苯碳酸纳米海绵负载姜黄素。

Evaluation of EDTA Dianhydride Versus Diphenyl Carbonate Nanosponges for Curcumin.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Ar-Ramtha, Jordan.

Department of Medicinal Chemistry, Faculty of Pharmacy, Jordan University of Science and Technology, Ar-Ramtha, Jordan.

出版信息

AAPS PharmSciTech. 2022 Aug 17;23(7):229. doi: 10.1208/s12249-022-02372-z.

Abstract

Cyclodextrin-based nanosponges are widely investigated for several applications and are considered potential drug carriers. The method of nanosponges preparation involves the use of chemical cross-linking agents where the properties of Nanosponges can be affected. This study compared the resulting differences in the final nanosponges' properties using carbonate and dianhydride crosslinkers. Diphenyl carbonate and EDTA dianhydride were used for the synthesis of nanosponges. Both types of nanosponges were loaded with curcumin as a model drug. Physicochemical characterizations, including PXRD, DSC, FTIR, scanning electron microscopy, AFM, particle size, zeta potential, and surface area analysis, were carried out for the prepared nanosponges. Curcumin release and drug content were also evaluated. Nanosponges prepared by Diphenyl carbonate crosslinker resulted in an amorphous form compared to crystalline EDTA-nanosponges. This study reported the successful inclusion and complexation of curcumin inside carbonate cross-linked cyclodextrin-based nanosponges and suggested the physical entrapment of crystalline curcumin in EDTA dianhydride. These findings were further investigated and supported by computational modeling.

摘要

环糊精纳米海绵因其在多种应用中的广泛研究而备受关注,并被认为是有潜力的药物载体。纳米海绵的制备方法涉及使用化学交联剂,这可能会影响纳米海绵的性质。本研究使用碳酸酯和二酐交联剂比较了最终纳米海绵性质的差异。二苯甲碳酸酯和 EDTA 二酐用于纳米海绵的合成。这两种类型的纳米海绵都负载了姜黄素作为模型药物。对制备的纳米海绵进行了包括 PXRD、DSC、FTIR、扫描电子显微镜、原子力显微镜、粒径、Zeta 电位和表面积分析在内的物理化学特性分析。还评估了姜黄素的释放和药物含量。与结晶的 EDTA 纳米海绵相比,二苯甲碳酸酯交联剂制备的纳米海绵呈无定形形式。本研究报告了姜黄素成功地被包合和络合在碳酸酯交联的环糊精纳米海绵内,并提出了结晶姜黄素在 EDTA 二酐中的物理包埋。这些发现通过计算建模得到了进一步的研究和支持。

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