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

Wang, Hui, Yang, Ziming, He, Zuyu, Zhou, Chuang, Wang, Chao, Chen, Yu, Liu, Xianwu, Li, Sidong, Li, Puwang
Colloids and surfaces 2019 v.179 pp. 519-526
acetylcysteine, antioxidants, biocompatibility, chitosan, colloids, deoxycholic acid, drugs, encapsulation, hydrophilicity, hydrophobicity, micelles, quercetin, solvents, water solubility
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.