Journal
MOLECULAR PHARMACEUTICS
Volume 14, Issue 4, Pages 1190-1203Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.6b01068
Keywords
VES-grafted-CSO; TPGS-RGD; PTX; mixed micelles; U87MG tumor inhibition
Funding
- National Natural Science Foundation of China [81503021, 81603502]
- Fundamental Research Funds for the Central Universities [22A201514055 ECUST]
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The poor therapeutic efficacy of hydrophobic chemotherapeutic drugs is an intrinsic limitation to successful chemotherapy. In the present study, a multitask delivery system based on arginine-glycine-aspartic acid peptide (RGD) decorated vitamin E succinate (VES)-grafted-chitosan oligosaccharide (CSO)/ RGD-conjugated D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS-RGD) mixed micelles (VeC/T-RGD MM) was first prepared for targeted delivery of a hydrophobic anticancer drug, paclitaxel (PTX), to improve the efficacy of U87MG tumor therapy. VES grafted CSO (VES-g-CSO) and TPGS-RGD were synthesized as nanocarriers, and PTX loaded VeC/T-RGD MM (PTX@VeC/TRGD MM) was prepared via the organic solvent emulsification evaporation method. The PTX@VeC/T-RGD MM was 150.2 um in diameter with uniform size distribution, 5.92% drug loading coefficient, and no obvious particle size changes within 7 days. The PTX@VeC/T-RGD, MM showed sustained-release properties in vitro and high cytotoxicity, and could be efficiently taken up by human glioma U87MG cells. The tumor inhibitory rate of PTX@VeC/T-RGD MM treatment in U87MG tumor spheroids and U87MG tumor bearing mice was 49.3% and 88.4%, respectively, which indicated a superior therapeutic effect. PTX@VeC/T-RGD MM did not damage normal tissues in safety evaluations. These findings suggested that PTX@VeC/T-RGD MM could be developed for the delivery of hydrophobic drugs to U87MG tumors.
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