Abstract
Bletilla striata polysaccharides (BSPs) have been used in pharmaceutical and biomedical industry, the aim of the present study was to explore a BSPs amphiphilic derivative to overcome its application limit as poorly water-soluble drug carriers due to water-soluble polymers. Stearic acid (SA) was selected as a hydrophobic block to modify B. striata polysaccharides (SA-BSPs). Docetaxel (DTX)-loaded SA-BSPs (DTX-SA-BSPs) copolymer micelles were prepared and characterized. The DTX release percentage in vitro and DTX concentration in vivo was carried out by using high performance liquid chromatography. HepG2 and HeLa cells were subjected to MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazonium bromide) assay to evaluate the cell viability. In vitro evaluation of copolymer micelles showed higher drug encapsulation and loading capacity. The release percentage of DTX from DTX-SA-BSPs copolymer micelles and docetaxel injection was 66.93 ± 1.79% and 97.06 ± 1.56% in 2 days, respectively. The DTX-SA-BSPs copolymer micelles exhibited a sustained release of DTX. A 50% increase in growth inhibition was observed for HepG2 cells treated with DTX-SA-BSPs copolymer micelles as compared to those treated with docetaxel injection for 72 h. DTX-SA-BSPs copolymer micelles presented a similar growth inhibition effect on Hela cells. Furthermore, absolute bioavailability of DTX-SA-BSPs copolymer micelles was shown to be 1.39-fold higher than that of docetaxel injection. Therefore, SA-BSPs copolymer micelles may be used as potential biocompatible polymers for cancer chemotherapy.
Highlights
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]
Compared to the standard spectrum of Bletilla striata polysaccharides (BSPs), a new peak showing the characteristic absorption at 1730 cm-1 was observed for Stearic acid (SA)-BSPs
The present study was an effort to deliver DTX using nanoparticulate drug delivery system in order to minimize the toxicity associated with its use and improve its therapeutic efficacy
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]. Docetaxel-loaded stearic acid-modified Bletilla striata polysaccharide copolymer micelles incorporated into the hydrophobic core of copolymer micelles, whereas the hydrophilic shell can stabilize and protect the drug in the aqueous medium. The hydrophilic shell can prolong the blood circulation time of micelles as a result of steric stabilization, which helps micelles escape mononuclear phagocyte system uptake after intravenous administration[5, 6]. These self-assemblies have potential uses in medicine and biotechnology because of their unique core—shell backbone[7], various amphiphilic block copolymers have been synthesized and their characteristics have been investigated widely[8, 9]. Many efforts have been performed to prepare non-toxic and biocompatibility amphiphilic block copolymers on the basis of natural polysaccharides[10]
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