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Self-assembled amphiphilic chitosan nanomicelles to enhance the solubility of quercetin for efficient delivery

Author:
Wang, Hui, Yang, Ziming, He, Zuyu, Zhou, Chuang, Wang, Chao, Chen, Yu, Liu, Xianwu, Li, Sidong, Li, Puwang
Source:
Colloids and surfaces 2019 v.179 pp. 519-526
ISSN:
0927-7765
Subject:
acetylcysteine, antioxidants, biocompatibility, chitosan, colloids, deoxycholic acid, drugs, encapsulation, hydrophilicity, hydrophobicity, micelles, quercetin, solvents, water solubility
Abstract:
Quercetin (QCT) has important functions such as antioxidant, anti-inflammatory and anticancer. However, its applications in food and in drug are restricted owing to its poor water solubility. In this work, a novel amphiphilic wall-material chitosan was synthesized via grafting of chitosan with deoxycholic acid (DA) as hydrophobic group and modified N-acetyl-L-cysteine (NAC) as hydrophilic group. Amphiphilic chitosan was self-assembled to load QCT as nanomicelles by a low-cost and inorganic solvent procedure. Both the encapsulation efficiencies (EE) and drug-loading rates (DL) increased when increasing the grafting rate of DA. There was a bursting release of QCT for the QCT-loaded nanomicelles (CS-DA-NAC-QNMs) from 0 to 8 h, and then the release rate decreased gradually. After releasing for 72 h, the final cumulative release percentages were more than 40%. All the QCT-loaded nanomicelles samples showed good hemocompatibility, and their water solubility and biocompatibility increased evidently. What’s more, they exhibited an obvious inhibition rate of A549 cells.
Agid:
6367063