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Preparation and In Vitro/Vivo Evaluation of Folate-conjugated Pluronic F87-PLGA/TPGS Mixed Nanoparticles for Targeted Drug Delivery

Author(s):

Tianyi Wu, Yanchun Gong, Ziling Li, Yuping Li and Xiangyuan Xiong*   Pages 1 - 10 ( 10 )

Abstract:


Aim: Folate-conjugated Pluronic F87-poly(lactic-co-glycolic acid) block copolymer (FA-F87-PLGA) was synthesized to encapsulate anticancer drug Paclitaxel (PTX) for targeted drug delivery. To further improve the curative effect, D-α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS or Vitamin E TPGS) was added to form FA-F87-PLGA/TPGS mixed NPs.

Methods: FA-F87-PLGA was synthesized by the ring-opening polymerization, and the structure was characterized. PTX-loaded nanoparticles were prepared with the nanoprecipitation method. The physicochemical characteristics were studied to determine the appropriate dose ratio of the FA-F87-PLGA to TPGS. The cytotoxicity against Ovarian Cancer Cells (OVCAR-3) was determined by MTT assay. The Area Under the Curve (AUC) and half-life were measured in the in vivo pharmacokinetic studies.

Results: Based on the optimization of particle size and embedding rate of PTX-loaded mixed NPs, the appropriate dosage ratio of FA-F87-PLGA to TPGS was finally determined to be 5:3. According to in vitro release studies, the cumulative release rate of PTX-loaded FA-F87-PLGA/TPGS mixed NPs was 92.04%, which was higher than that of nanoparticles without TPGS. The cytotoxicity studies showed that the IC50 value of PTX-loaded FA-F87-PLGA/TPGS decreased by 75.4 times and 19.7 times after 72 h treatment compared with free PTX injections and PTX-loaded FA-F87- PLGA NPs, respectively. In vivo pharmacokinetic studies indicated that FA-F87-PLGA/TPGS mixed NPs had a longer drug metabolism time and a larger Area Under the Curve (AUC) compared with free PTX injections.

Conclusion: FA-F87-PLGA/TPGS mixed NPs are potential candidates for targeted drug delivery systems.

Keywords:

Pluronic F87, TPGS, PLGA, nanoparticles, targeted drug delivery systems, paclitaxel.

Affiliation:

School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi, School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi, School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi, School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi, School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi



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