Polymeric micelles with glycolipid-like structure and multiple hydrophobic domains for mediating molecular target delivery of paclitaxel.
Herein, polymeric micelles with glycolipid-like structure and about 40 nm diameter are prepared by self-aggregation from stearate-grafted chitosan oligosaccharides in aqueous medium. The micelles, with high degree of substitution (DS), present specific spatial structure with multiple hydrophobic "minor cores", and thus obtain excellent internalization into cancer cells and accumulation in cytoplasm. Furthermore, the micelles showed pH-sensitive properties, thus favoring intracellular delivery of encapsulated drug via endocytosis. The cell cytotoxicity of paclitaxel encapsulated in micelles was improved sharply and contributed to the increased intracellular delivery of the drug. The present micelles are a promising carrier candidate for targeting therapy of antitumor drugs with a cytoplasmic molecule target.
College of Pharmaceutical Sciences, Zhejiang University, Yuhangtang Road 388, Hangzhou 310058, People's Republic of China.
Jian
J
You
Fu-Qiang
FQ
Hu
Yong-Zhong
YZ
Du
Hong
H
Yuan
D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D004705:Endocytosis; D006017:Glycolipids / Q000737:chemistry* / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D015394:Molecular Structure; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D010316:Particle Size; D011108:Polymers / Q000737:chemistry* / Q000378:metabolism; D014867:Water / Q000737:chemistry
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D006017:Glycolipids; D008823:Micelles; D011108:Polymers; D014867:Water; D048271:Chitosan; D017239:Paclitaxel