Core-modified chitosan-based polymeric micelles for controlled release of doxorubicin.
Amphiphilic stearic acid-grafted chitosan oligosaccharide (CSO-SA) micelles have been shown a good drug delivery system by incorporating hydrophobic drugs into the core of the micelles. One of the problems associated with the use of CSO-SA micelles is disassociation or the initial burst drug release during the dilution of drug delivery system by body fluid. Herein, the core of CSO-SA micelles was modified by the physical solubilization of stearic acid (SA) to reduce the burst drug release and enhance the physical stability of CSO-SA micelles. The CSO-SA micelles had 27.4+/-2.4 nm number average diameter, and indicated pH-sensitive properties. The micelle size and drug release rate from micelles increased with the decrease of pH value. After the incorporation of SA into CSO-SA micelles, the micelle size was increased, and the zeta potential was decreased. The extents of the increase in micelle size and the decrease of zeta potential related with the incorporated amount of SA. The in vitro drug release tests displayed the incorporation of SA into CSO-SA micelles could reduce the drug release from the micelles due to the enhanced hydrophobic interaction among SA, hydrophobic drug and hydrophobic segments of CSO-SA.
Ye
Yi-Qing
YQ
Women Hospital, School of Medicine, Zhejiang University, 2 Xueshi Road, Hangzhou 310006, PR China.
Yang
Feng-Liang
FL
Hu
Fu-Qiang
FQ
Du
Yong-Zhong
YZ
Yuan
Hong
H
Yu
He-Yong
HY
D000903:Antibiotics, Antineoplastic / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004317:Doxorubicin / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D008823:Micelles; D010316:Particle Size; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods
D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008823:Micelles; D013229:Stearic Acids; C031183:stearic acid; D004317:Doxorubicin; D048271:Chitosan