title: Decreased Core Crystallinity Facilitated Drug Loading in Polymeric Micelles without Affecting Their Biological Performances.
abstract: Cargo-loading capacity of polymeric micelles could be improved by reducing the core crystallinity and the improvement in the amount of loaded cargo was cargo-polymer affinity dependent. The effect of medium chain triglyceride (MCT) in inhibiting PCL crystallization was confirmed by DSC and polarized microscope. When incorporating MCT into polymeric micelles, the maximum drug loading of disulfiram (DSF), cabazitaxel (CTX), and TM-2 (a taxane derivative) increased from 2.61 ± 0.100%, 13.5 ± 0.316%, and 20.9 ± 1.57% to 8.34 ± 0.197%, 21.7 ± 0.951%, and 28.0 ± 1.47%, respectively. Moreover, the prepared oil-containing micelles (OCMs) showed well-controlled particle size, good stability, and decreased drug release rate. MCT incorporation showed little influence on the performances of micelles in cell studies or pharmacokinetics. These results indicated that MCT incorporation could be a core construction module applied in the delivery of hydrophobic drugs.
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Jingxin
authors: J
authors: Gou
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Shuangshuang
authors: S
authors: Feng
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Helin
authors: H
authors: Xu
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Guihua
authors: G
authors: Fang
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Yanhui
authors: Y
authors: Chao
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Yu
authors: Y
authors: Zhang
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Hui
authors: H
authors: Xu
authors: School of Pharmacy, Shenyang Pharmaceutical University , 103 Wenhua Road, Shenyang 110016, China.
authors: Xing
authors: X
authors: Tang
mesh_terms: D000818:Animals; D002460:Cell Line; D004221:Disulfiram / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D008823:Micelles; D051381:Rats; D017207:Rats, Sprague-Dawley; D043823:Taxoids / Q000737:chemistry / Q000494:pharmacology; D014280:Triglycerides / Q000737:chemistry / Q000494:pharmacology
chemical_list: C000593048:13-(N-tert-butoxycarbonyl-3-isobutylisoserinoyl-4,10-diacetoxy-2-benzoyloxy-5-20-epoxy-1,13-dihydroxy-9-oxo-19-norcyclopropa(g)tax-11-ene; D004337:Drug Carriers; D008823:Micelles; D043823:Taxoids; D014280:Triglycerides; C552428:cabazitaxel; D004221:Disulfiram