Encapsulation of paclitaxel into lauric acid-O-carboxymethyl chitosan-transferrin micelles for hydrophobic drug delivery and site-specific targeted delivery.
Transferrin/PEG/O-carboxymethyl chitosan/fatty acid/paclitaxel (TPOCFP) micelles were tested for suitability as a drug carrier characterized by low cytotoxicity, sustained release, high cellular uptake, and site-specific targeted delivery of hydrophobic drugs. Characterization, drug content, encapsulation efficiency, and in vitro drug release were investigated. When the feeding amount of paclitaxel (PTX) was increased, the drug content increased, but loading efficiency decreased. TPOCFP micelles had a spherical shape, with a particle size of approximately 140-649 nm. In vitro cell cytotoxicity and hemolysis assays were conducted to confirm the safety of the micelles. Anticancer activity and confocal laser scanning microscopy (CLSM) were used to confirm the targeting efficiency of target ligand-modified TPOCFP micelles. Anticancer activity and CLSM results clearly demonstrated that transferrin-modified TPOCFP micelles were quickly taken up by the cell. The endocytic pathway of TPOCFP micelles was analyzed by flow cytometry, revealing transfection via receptor-mediated endocytosis. These results suggest that PTX-encapsulated TPOCFP micelles may be used as an effective cancer-targeting drug delivery system for chemotherapy.
Department of Polymer Science and Engineering, Sunchon National University, 255 Jungang-ro, Suncheon, Jeollanam-do, Republic of Korea.
Joung-Pyo
JP
Nam
Seong-Cheol
SC
Park
Tae-Hun
TH
Kim
Jae-Yeang
JY
Jang
Changyong
C
Choi
Mi-Kyeong
MK
Jang
Jae-Woon
JW
Nah
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000031:analogs & derivatives* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D007850:Lauric Acids / Q000737:chemistry*; D008823:Micelles; D017239:Paclitaxel / Q000008:administration & dosage / Q000737:chemistry*; D051381:Rats; D014168:Transferrin / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D007850:Lauric Acids; D008823:Micelles; C504164:O-carboxymethylchitosan; D014168:Transferrin; C030358:lauric acid; D048271:Chitosan; D017239:Paclitaxel
Micelle; O-carboxymethyl chitosan; PEG; Paclitaxel; Transferrin