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Enhanced effect of folated pluronic F87-PLA/TPGS mixed micelles on targeted delivery of paclitaxel.
Xiong, Xiang Yuan; Pan, Xiaoqian; Tao, Long; Cheng, Feng; Li, Zi Ling; Gong, Yan Chun; Li, Yu Ping.
Afiliación
  • Xiong XY; School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, China; School of Life Science, Jiangxi Science and Technology Normal University, Nanchang 330013, China. Electronic address: xyxiong@gmail.com.
  • Pan X; School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, China.
  • Tao L; School of Life Science, Jiangxi Science and Technology Normal University, Nanchang 330013, China.
  • Cheng F; Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA.
  • Li ZL; School of Life Science, Jiangxi Science and Technology Normal University, Nanchang 330013, China.
  • Gong YC; School of Life Science, Jiangxi Science and Technology Normal University, Nanchang 330013, China.
  • Li YP; School of Life Science, Jiangxi Science and Technology Normal University, Nanchang 330013, China.
Int J Biol Macromol ; 103: 1011-1018, 2017 Oct.
Article en En | MEDLINE | ID: mdl-28552723
Targeted drug delivery systems have great potential to overcome the side effect and improve the bioavailability of conventional anticancer drugs. In order to further improve the antitumor efficacy of paclitaxel (PTX) loaded in folated Pluronic F87/poly(lactic acid) (FA-F87-PLA) micelles, D-α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS or Vitamin E TPGS) were added into FA-F87-PLA to form FA-F87-PLA/TPGS mixed micelles. The LE of PTX-loaded mixed micelles (13.5%) was highest in the mass ratio 5 to 3 of FA-F87-PLA to TPGS. The in vitro cytotoxicity assays indicated that the IC50 values for free PTX injections, PTX-loaded FA-F87-PLA micelles and PTX-loaded FA-F87-PLA/TPGS mixed micelles after 72h of incubation were 1.52, 0.42 and 0.037mg/L, respectively. The quantitative cellular uptake of coumarin 6-loaded FA-F87-PLA/TPGS and FA-F87-PLA micelles showed that the cellular uptake efficiency of mixed micelles was higher for 2 and 4h incubation, respectively. In vivo pharmacokinetic studies found that the AUC of PTX-loaded FA-F87-PLA/TPGS mixed micelles is almost 1.4 times of that of PTX-loaded FA-F87-PLA micelles. The decreased particle size and inhibition of P-glycoprotein effect induced by the addition of TPGS could result in enhancing the cellular uptake and improving the antitumor efficiency of PTX-loaded FA-F87-PLA/TPGS mixed micelles.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Polietilenglicoles / Succinatos / Portadores de Fármacos / Paclitaxel / Poloxámero / Ácido Fólico / Micelas Límite: Animals / Humans / Male Idioma: En Revista: Int J Biol Macromol Año: 2017 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Polietilenglicoles / Succinatos / Portadores de Fármacos / Paclitaxel / Poloxámero / Ácido Fólico / Micelas Límite: Animals / Humans / Male Idioma: En Revista: Int J Biol Macromol Año: 2017 Tipo del documento: Article Pais de publicación: Países Bajos