title: Self-assembled methoxy poly(ethylene glycol)-cholesterol micelles for hydrophobic drug delivery.
abstract: To promote the application of methoxy poly(ethylene glycol)-cholesterol (mPEG-Chol), mPEG-Chol was used to prepare core-shell micelles encapsulating poorly water-soluble docetaxel (DTX-PM) by modified cosolvent evaporation method. Approaches to enhance DTX entrapment efficiency (EE) and minimize particle size were investigated in detail, including organic and aqueous phase composition, organic/aqueous phase ratio, and polymer concentration. In optimal formulation, micelles had higher EE (97.6%) and drug loading (4.76%) with the diameter of 13.76 ± 0.68 nm and polydispersity index of 0.213 ± 0.006. Transmission electron microscopy (TEM) showed that the micelles were spherical, and differential scanning calorimetry (DSC) analysis proved that DTX was successfully entrapped into mPEG-Chol micelles. The in vitro cytotoxicity experiments displayed that blank micelles had no effect on the growth of SKOV-3, BXPC-3, A549, and HepG-2 cells, demonstrating that mPEG-Chol was one of the biocompatible biomaterials. The half inhibition concentration of DTX-PM on SKOV-3, BXPC-3, A549, and HepG-2 cells were 10.08, 7.6, 28.37, and 125.75 ng/mL, respectively. DTX-PM had the similar antitumor activity to free DTX, indicating that mPEG-Chol was a promising micellar vector for hydrophobic drug delivery. In addition, this work provided a new and facile approach to prepare drug-loaded micelles with controllable performances.
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.
authors.forename: Yiyi
authors.initials: Y
authors.lastname: Yu
authors.forename: Yingju
authors.initials: Y
authors.lastname: He
authors.forename: Bei
authors.initials: B
authors.lastname: Xu
authors.forename: Zhiyao
authors.initials: Z
authors.lastname: He
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhang
authors.forename: Yan
authors.initials: Y
authors.lastname: Chen
authors.forename: Yang
authors.initials: Y
authors.lastname: Yang
authors.forename: Yongmei
authors.initials: Y
authors.lastname: Xie
authors.forename: Yu
authors.initials: Y
authors.lastname: Zheng
authors.forename: Gu
authors.initials: G
authors.lastname: He
authors.forename: Jun
authors.initials: J
authors.lastname: He
authors.forename: Xiangrong
authors.initials: X
authors.lastname: Song
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002784:Cholesterol / Q000737:chemistry*; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D009369:Neoplasms / Q000188:drug therapy; D011092:Polyethylene Glycols / Q000737:chemistry*; D043823:Taxoids / Q000008:administration & dosage* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D043823:Taxoids; D000077143:Docetaxel; D011092:Polyethylene Glycols; C028210:monomethoxypolyethylene glycol; D002784:Cholesterol