title: Docetaxel-Loaded Self-Assembly Stearic Acid-Modified Bletilla striata Polysaccharide Micelles and Their Anticancer Effect: Preparation, Characterization, Cellular Uptake and In Vitro Evaluation.
abstract: Poorly soluble drugs have low bioavailability after oral administration, thereby hindering effective drug delivery. A novel drug-delivery system of docetaxel (DTX)-based stearic acid (SA)-modifiedBletilla striatapolysaccharides (BSPs) copolymers was successfully developed. Particle size,zetapotential, encapsulation efficiency (EE), and loading capacity (LC) were determined. The DTX release percentage in vitro was determined using high performance liquid chromatography (HPLC). The hemolysis and in vitro anticancer activity were studied. Cellular uptake and apoptotic rate were measured using flow cytometry assay. Particle size,zetapotential, EE and LC were 125.30 ± 1.89 nm, -26.92 ± 0.18 mV, 86.6% ± 0.17%, and 14.8% ± 0.13%, respectively. The anticancer activities of DTX-SA-BSPs copolymer micelles against HepG2, HeLa, SW480, and MCF-7 (83.7% ± 1.0%, 54.5% ± 4.2%, 48.5% ± 4.2%, and 59.8% ± 1.4%, respectively) were superior to that of docetaxel injection (39.2% ± 1.1%, 44.5% ± 5.3%, 38.5% ± 5.4%, and 49.8% ± 2.9%, respectively) at 0.5 μg/mL drug concentration. The DTX release percentage of DTX-SA-BSPs copolymer micelles and docetaxel injection were 66.93% ± 1.79% and 97.06% ± 1.56% in two days, respectively. Cellular uptake of DTX-FITC-SA-BSPs copolymer micelles in cells had a time-dependent relation. Apoptotic rate of DTX-SA-BSPs copolymer micelles and docetaxel injection were 73.48% and 69.64%, respectively. The SA-BSPs copolymer showed good hemocompatibility. Therefore, SA-BSPs copolymer can be used as a carrier for delivering hydrophobic drugs.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China. guanqx@jlu.edu.cn.
authors.forename: Qingxiang
authors.initials: Q
authors.lastname: Guan
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China. sundd15@mails.jlu.edu.cn.
authors.forename: Dandan
authors.initials: D
authors.lastname: Sun
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China. zhangguangyuan11@126.com.
authors.forename: Guangyuan
authors.initials: G
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China. suncheng15@mails.jlu.edu.cn.
authors.forename: Cheng
authors.initials: C
authors.lastname: Sun
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China. wangmiao15@mails.jlu.edu.cn.
authors.forename: Miao
authors.initials: M
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China. jidy16@mails.jlu.edu.cn.
authors.forename: Danyang
authors.initials: D
authors.lastname: Ji
authors.affiliation: Department of Neurology, Second Hospital of Jilin University, Changchun 130041, China. wei88linda@yahoo.com.
authors.forename: Wei
authors.initials: W
authors.lastname: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D000077143:Docetaxel; D004337:Drug Carriers / Q000494:pharmacology*; D065546:Drug Liberation; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D061986:MCF-7 Cells; D008823:Micelles; D009369:Neoplasms / Q000188:drug therapy*; D019906:Nuclear Magnetic Resonance, Biomolecular; D010316:Particle Size; D018517:Plant Roots / Q000737:chemistry; D011134:Polysaccharides / Q000494:pharmacology*; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry; D043823:Taxoids / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D011134:Polysaccharides; D013229:Stearic Acids; D043823:Taxoids; C000591471:polysaccharide b, Bletilla striata; D000077143:Docetaxel; C031183:stearic acid
keywords: Bletilla striata polysaccharide; anticancer activity; apoptotic; copolymer micelle; docetaxel; hemolysis assay