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Molecules 2016, 21(12), 1641; doi:10.3390/molecules21121641

Docetaxel-Loaded Self-Assembly Stearic Acid-Modified Bletilla striata Polysaccharide Micelles and Their Anticancer Effect: Preparation, Characterization, Cellular Uptake and In Vitro Evaluation

1
Department of Pharmaceutics, School of Pharmacy, Jilin University, No. 1266, Fujin Road, Changchun 130021, China
2
Department of Neurology, Second Hospital of Jilin University, Changchun 130041, China
*
Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 18 October 2016 / Revised: 21 November 2016 / Accepted: 25 November 2016 / Published: 2 December 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [6244 KB, uploaded 2 December 2016]   |  

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)-modified Bletilla striata polysaccharides (BSPs) copolymers was successfully developed. Particle size, zeta potential, 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, zeta potential, 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. View Full-Text
Keywords: docetaxel; Bletilla striata polysaccharide; copolymer micelle; hemolysis assay; anticancer activity; apoptotic docetaxel; Bletilla striata polysaccharide; copolymer micelle; hemolysis assay; anticancer activity; apoptotic
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MDPI and ACS Style

Guan, Q.; Sun, D.; Zhang, G.; Sun, C.; Wang, M.; Ji, D.; Yang, W. Docetaxel-Loaded Self-Assembly Stearic Acid-Modified Bletilla striata Polysaccharide Micelles and Their Anticancer Effect: Preparation, Characterization, Cellular Uptake and In Vitro Evaluation. Molecules 2016, 21, 1641.

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