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5-氟尿嘧啶与β-环糊精、碳酸盐及二酐交联β-环糊精的弱络合作用及研究

Weak complexation of 5-fluorouracil with β-cyclodextrin, carbonate, and dianhydride crosslinked β-cyclodextrin: and studies.

作者信息

Mashaqbeh Hadeia, Obaidat Rana, Al-Shar'i Nizar A, El-Elimat Tamam, Alnabulsi Soraya

机构信息

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

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

出版信息

Res Pharm Sci. 2022 Jul 14;17(4):334-349. doi: 10.4103/1735-5362.350235. eCollection 2022 Aug.

DOI:10.4103/1735-5362.350235
PMID:36034082
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9400465/
Abstract

BACKGROUND AND PURPOSE

Several pharmaceutical formulations were investigated to improve the solubility of 5-fluorouracil to enhance bioavailability and therapeutic efficacy. This study aimed to examine the potential use of cyclodextrin-based nanosponges for the incorporation of 5-fluorouracil and to investigate the use of different crosslinking agents on the properties of the resulting drug carrier. 5-Fluorouracil complexation with β-cyclodextrin was also studied to explain the unexpected results of weak 5-fluorouracil incorporation in nanosponge.

EXPERIMENTAL APPROACH

Nanosponges were synthesized by crosslinking β-cyclodextrin with two different crosslinkers; diphenyl carbonate and ethylenediaminetetraacetic dianhydride. The incorporation of 5-fluorouracil into β-cyclodextrin and the prepared nanosponges were assessed by NMR, FTIR, PXRD, DSC, and TGA. In addition, an release study was carried out to evaluate the potential use of β-cyclodextrin- based nanosponges as pharmaceutical formulations for 5-fluorouracil.

FINDINGS / RESULTS: Physicochemical characterization of the dried formulations indicated the complexation of 5-fluorouracil with the β-cyclodextrin polymer. Despite that, no clear manifestation of 5-fluorouracil encapsulation in the prepared β-cyclodextrin-based nanosponge was detected. Furthermore, no significant differences were observed in the release profiles of 5-fluorouracil, β-cyclodextrin complex, and β- cyclodextrin-based nanosponge, suggesting weak complexation and instability in aqueous solutions. EDTA- crosslinked β-cyclodextrin-based nanosponge showed a slight improvement in 5-fluorouracil solubility with a faster initial rate of 5-fluorouracil release.

CONCLUSION AND IMPLICATIONS

This study suggested weak complexation between 5-fluorouracil and the β- cyclodextrin polymer or nanosponges. Crosslinking of β-cyclodextrin with EDTA dianhydride crosslinker showed an enhancement in 5-fluorouracil saturation solubility combined with a faster initial rate of drug release.

摘要

背景与目的

研究了几种药物制剂以提高5-氟尿嘧啶的溶解度，从而增强其生物利用度和治疗效果。本研究旨在考察基于环糊精的纳米海绵对5-氟尿嘧啶的包载潜力，并研究不同交联剂对所得药物载体性质的影响。还研究了5-氟尿嘧啶与β-环糊精的络合作用，以解释纳米海绵中5-氟尿嘧啶包载量低这一意外结果。

实验方法

用两种不同的交联剂——碳酸二苯酯和乙二胺四乙酸二酐——使β-环糊精交联，合成纳米海绵。通过核磁共振（NMR）、傅里叶变换红外光谱（FTIR）、粉末X射线衍射（PXRD）、差示扫描量热法（DSC）和热重分析法（TGA）评估5-氟尿嘧啶在β-环糊精及所制备纳米海绵中的包载情况。此外，进行了释放研究，以评估基于β-环糊精的纳米海绵作为5-氟尿嘧啶药物制剂的潜在用途。

研究结果

干燥制剂的物理化学表征表明5-氟尿嘧啶与β-环糊精聚合物发生了络合。尽管如此，在所制备的基于β-环糊精的纳米海绵中未检测到5-氟尿嘧啶包封的明显迹象。此外，5-氟尿嘧啶、β-环糊精络合物和基于β-环糊精的纳米海绵的释放曲线未观察到显著差异，表明在水溶液中络合作用较弱且不稳定。乙二胺四乙酸（EDTA）交联的基于β-环糊精的纳米海绵在5-氟尿嘧啶溶解度方面有轻微改善，5-氟尿嘧啶释放的初始速率更快。

结论与意义

本研究表明5-氟尿嘧啶与β-环糊精聚合物或纳米海绵之间的络合作用较弱。用乙二胺四乙酸二酐交联剂使β-环糊精交联，显示出5-氟尿嘧啶饱和溶解度提高，同时药物释放的初始速率更快。

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