Polycaprolactone-Vitamin E TPGS Micellar Formulation for Oral Delivery of Paclitaxel

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 prepar...

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Bibliographic Details
Published in:Polymers 2024-08, Vol.16 (15), p.2232
Main Authors: Binkhathlan, Ziyad, Ali, Raisuddin, Yusuf, Osman, Alomrani, Abdullah H, Badran, Mohamed M, Alshememry, Abdullah K, Alshamsan, Aws, Alqahtani, Faleh, Qamar, Wajhul, Attwa, Mohamed W
Format: Article
Language:English
Subjects:
Bioavailability
Cancer
Chemotherapy
Copolymers
Fluorescent indicators
Laboratories
Micelles
Oral administration
Paclitaxel
Permeability
Pharmaceutical industry
Polycaprolactone
Polydispersity
Polyethylene glycol
Polymerization
Rhodamine
Ring opening polymerization
Solvents
Tocopherol
Vitamin E
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Summary: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 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 (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 . 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 -TPGS micelles exhibit potential as an effective oral delivery system for PTX.
ISSN:2073-4360
2073-4360
DOI:10.3390/polym16152232