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.
Highlights
Over the past decades, self-assembled copolymer micelles consisting of amphiphilic block copolymer in aqueous medium are receiving considerable attention as gene and drug nanocarriers because of their particular characteristics [1,2,3,4]
The results indicated that DTX-stearic acid (SA)-B. striata polysaccharides (BSPs) copolymer micellescopolymer were micelles theagainst four cancer to that of DTX-SA-BSPs docetaxel injection
The results indicated that DTX-SA-BSPs copolymer micelles the particles have a large surface energy and chemical activity, which are beneficial to had more effective against tumor cells
Summary
Self-assembled copolymer micelles consisting of amphiphilic block copolymer in aqueous medium are receiving considerable attention as gene and drug nanocarriers because of their particular characteristics [1,2,3,4]. Natural polysaccharides (SA)-modified chitosan drug-loaded micelles showed significantly higher tumor cell inhibition in vitro have good biocompatibility, biodegradability, and negative immunogenicity. BSPs have micelles showed higher stability in acidic medium and sustained drug release up to 100 h in the been extensivelysmall used in chemical industries as gels, suspension solutions, and binders as well as in intestine, which enhanced the interaction of copolymer micelles with the intestinal membrane and facilitated superoxide cellularBSPs uptake [18]. Have excellent candidate for various drug-loaded micelles showed significantly higher tumor cell inhibition in vitro compared with free pharmaceutical applications, such as drug-delivery systems [23]. BSPs have become an excellent candidate for various this problem, alkyl, aralkyl, and deoxycholic acid were used to modify water-soluble copolymer to pharmaceutical applications, such as drug-delivery systems [23]. Synthetic route of stearic acid conjugated B. striata polysaccharides (SA-BSPs)
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