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基于壳聚糖/羧甲基-β-环糊精水凝胶的盐酸小檗碱口服给药

Oral Administration of Berberine Hydrochloride Based on Chitosan/Carboxymethyl-β-Cyclodextrin Hydrogel.

作者信息

Clemence Bukatuka Futila, Xiao Lin, Yang Guang

机构信息

Department of Biomedical Engineering, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China.

School of Biomedical Engineering, Sun Yat-Set University, Shenzhen 518107, China.

出版信息

Polymers (Basel). 2024 Aug 21;16(16):2368. doi: 10.3390/polym16162368.

DOI:10.3390/polym16162368
PMID:39204588
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11360765/
Abstract

In this study, a novel oral formulation of berberine hydrochloride (BBH) hydrogel was successfully synthesized through physical cross-linking using chitosan (CS) and carboxymethyl-β-cyclodextrin (CMCD). The characterization results confirmed the successful synthesis of the CS/CMCD hydrogel and the subsequent loading of BBH into this composite (CS/CMCD/BBH) was effectively accomplished. The BBH was used as a model drug and the resulting hydrogel demonstrated a sustained drug release profile. In addition to its improved solubility and sustained release characteristics, the hydrogel exhibited excellent antibacterial activity against common pathogens such as (), (), and (). Additionally, in vitro studies indicated that the hydrogel was not cytotoxic to NIH3T3 and HaCaT cells, suggesting its safety for biomedical applications. This lack of cytotoxic effects, combined with the mechanical strength, solubility improvements, and antibacterial properties of the hydrogel, positions the CS/CMCD/BBH hydrogel as a promising candidate for the effective oral delivery of BBH. By addressing the solubility and delivery challenges of BBH, this hydrogel offers a viable solution for the oral administration of BBH, with potential applications in various biomedical fields.

摘要

在本研究中,通过使用壳聚糖(CS)和羧甲基-β-环糊精(CMCD)进行物理交联,成功合成了一种新型口服盐酸小檗碱(BBH)水凝胶制剂。表征结果证实了CS/CMCD水凝胶的成功合成,并且随后将BBH有效地负载到了该复合材料(CS/CMCD/BBH)中。将BBH用作模型药物,所得水凝胶呈现出药物缓释特性。除了其改善的溶解性和缓释特性外,该水凝胶对诸如()、()和()等常见病原体表现出优异的抗菌活性。此外,体外研究表明该水凝胶对NIH3T3和HaCaT细胞无细胞毒性,表明其在生物医学应用中的安全性。这种缺乏细胞毒性的作用,再加上水凝胶的机械强度、溶解性改善和抗菌性能,使得CS/CMCD/BBH水凝胶成为BBH有效口服给药的有前景的候选者。通过解决BBH的溶解性和给药挑战,这种水凝胶为BBH的口服给药提供了一种可行的解决方案,在各种生物医学领域具有潜在应用。

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