1. Folate-conjugated pluronic/polylactic acid polymersomes for oral delivery of paclitaxel.
- Author
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Pan XQ, Gong YC, Li ZL, Li YP, and Xiong XY
- Subjects
- Administration, Oral, Animals, Cell Line, Tumor, Drug Liberation, Humans, Kinetics, Nanoparticles, Paclitaxel pharmacokinetics, Rats, Reactive Oxygen Species, Drug Carriers, Folic Acid chemistry, Paclitaxel administration & dosage, Poloxamer chemistry, Polyesters chemistry
- Abstract
Cancer chemotherapy and the patient's life will be more convenient if oral administration of anti-cancer drugs can be achieved. The feasibility of folate-targeted Pluronic F127/polylactic acid (FA-F127-PLA) polymersomes as the oral delivery carriers of paclitaxel (PTX) has been explored in this study. PTX loaded in FA-F127-PLA and PLA-F127-PLA polymersomes showed biphasic release behaviors in simulated gastric and intestinal fluids. PTX loaded in FA-F127-PLA polymersomes exhibited higher cytotoxicity and cellular uptake than PTX loaded in PLA-F127-PLA polymersomes. In vivo pharmacokinetic studies in rats showed that oral PTX loaded in FA-F127-PLA polymersomes had a higher bioavailability than oral PTX loaded in PLA-F127-PLA polymersomes. D-α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS or Vitamin E TPGS) was also added to the FA-F127-PLA polymersomes as an optimization agent. Compared with PTX-loaded FA-F127-PLA polymersome, PTX-loaded FA-F127-PLA/TPGS mixed polymersomes showed even better cytotoxic ability, more cellular uptake and higher bioavailability. The above results indicate that FA-F127-PLA and FA-F127-PLA/TPGS mixed polymersomes could be good candidates for the oral delivery carrier of anti-cancer drugs., (Copyright © 2019 Elsevier B.V. All rights reserved.)
- Published
- 2019
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