Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles

Abstract

A folic acid (FA)-functionalized drug vehicle platform based on Pluronic 127 (P127)/D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) mixed micelles was orchestrated for an effective delivery of the model drug resveratrol in order to address the problem of poor water solubility and rapid metabolism of resveratrol and improve its targeted accumulation at tumor site. The FA-decorated mixed micelles were prepared using thin-film hydration method and optimized by central composite design approach. The micelles were also characterized in terms of size and morphology, drug entrapment efficiency and in vitro release profile. In addition, the cytotoxicity and cell uptake of the micelles were evaluated in folate receptor-overexpressing MCF-7 cell line. In vivo pharmacokinetic and biodistribution studies were also performed. The average size of the micelles was ~20 nm with a spherical shape and high encapsulation efficiency (99.67%). The results of fluorescence microscopy confirmed the targeting capability of FA-conjugated micelles in MCF-7 cells. FA-modified micelles exhibited superior pharmacokinetics in comparison with that of solution. Further, the low accumulation of resveratrol-loaded FA micelles formulation in the heart and kidney avoided toxicity of these vital organs. It could be concluded that folate-modified P127/TPGS mixed micelles might serve as a potential delivery platform for resveratrol.

Folate Conjugated Vs PEGylated Phytosomal Casein Nanocarriers for Codelivery of Fungal- and Herbal-Derived Anticancer Drugs

“…This result is in agreement with the previously reported higher uptake of covalent-conjugated FA-HSA NPs into cancer cells [51]. Recently, Hao et al reported the superior cytotoxicity of folate-targeted RSV-loaded Pluronic/TPGS- mixed MCs (IC 50 = 27.89 μg/ml) against folate receptor-overexpressing MCF-7 cells compared with free RSV (137.58 μg/ml) after 48 h [52]. Furthermore, the structure resemblance of phospholipid bilayer to the lipid content of the mammalian cellular membrane can increase membrane penetration.…”

Triphenylphosphonium and D-α-tocopheryl polyethylene glycol 1000 succinate-modified, tanshinone IIA-loaded lipid-polymeric nanocarriers for the targeted therapy of myocardial infarction

“…This phenomenon could be due to the ligands-mediated targeting of TPP-TPGS-modified LPNs. 45 In vivo infarct therapy effect was evaluated by measuring the infarct size. Infarct size is conceived as one of the critical indices for evaluating the cardiac damage in the generation of ischemic heart disease.…”

Functionalized Folic Acid-Chitosan Nanoparticles for Encapsulation of Dietary Polyphenols

“…Encapsulation of polyphenols enhances the bioavailability of these micronutrients in solution [1][2][3][4][5]34]. Folic acid functionalized drug delivery system based on resveratrol is known [35]. Resveratrol-folic acid-chitosan-100 5.9 (±0.9) 1.5 65…”