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Polycaprolactone—Vitamin E TPGS Micellar Formulation for Oral Delivery of Paclitaxel.
- Source :
- Polymers (20734360); Aug2024, Vol. 16 Issue 15, p2232, 18p
- Publication Year :
- 2024
-
Abstract
- This study aimed to investigate the potential of polycaprolactone–vitamin E TPGS (PCL-TPGS) micelles as a delivery system for oral administration of paclitaxel (PTX). The PCL-TPGS copolymer was synthesized using ring opening polymerization, and PTX-loaded PCL-TPGS micelles (PTX micelles) were prepared via a co-solvent evaporation method. Characterization of these micelles included measurements of size, polydispersity, and encapsulation efficiency. The cellular uptake of PTX micelles was evaluated in Caco-2 cells using rhodamine 123 (Rh123) as a fluorescent probe. Moreover, an everted rat sac study was conducted to evaluate the ex vivo permeability of PTX micelles. Additionally, a comparative pharmacokinetic study of PTX micelles versus the marketed formulation, Ebetaxel<superscript>®</superscript> (a Taxol generic), was performed after a single oral administration to rats. The results demonstrated that the micellar formulation significantly improved PTX solubility (nearly 1 mg/mL). The in vitro stability and release of PTX micelles in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) demonstrated that PTX micelles remained stable for up to 24 h and significantly slowed the release of PTX in both media compared to Ebetaxel<superscript>®</superscript>. The in vitro cellular uptake, ex vivo intestinal permeability, and in vivo pharmacokinetic profile demonstrated that PTX micelles enhanced the permeability and facilitated a rapid absorption of the drug. Conclusively, the PCL<subscript>7000</subscript>-TPGS<subscript>3500</subscript> micelles exhibit potential as an effective oral delivery system for PTX. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 20734360
- Volume :
- 16
- Issue :
- 15
- Database :
- Complementary Index
- Journal :
- Polymers (20734360)
- Publication Type :
- Academic Journal
- Accession number :
- 178952931
- Full Text :
- https://doi.org/10.3390/polym16152232