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Investigation of cationized triblock and diblock poly( ε -caprolactone)-co-poly(ethylene glycol) copolymers for oral delivery of enoxaparin: In vitro approach

Abstract : In this study, poly(ε-caprolactone)-co-poly(ethylene glycol) copolymers grafted with a cationic ligand, propargyltrimethyl ammonium iodide (PTA), to fabricate the cationized triblock (P(CatCLCL)2-PEG) and diblock (P(CatCLCL)-mPEG) copolymers were investigated their potential use for oral delivery of enoxaparin (ENX). Influences of various PTA contents and different structures of the copolymers on molecular characteristics, ENX encapsulation, particle characteristics, and capability of drug transport across Caco-2 cells were elucidated. The results showed that P(CatCLCL)2-PEG and P(CatCLCL)-mPEG copolymers self-aggregated and encapsulated ENX into spherical particles of ∼200-450nm. The increasing amount of PTA on the copolymers increased encapsulation efficiency of over 90%. The ENX release from both types of the cationized copolymer particles was pH-dependent which was retarded at pH 1.2 and accelerated at pH 7.4, supporting the drug protection in the acidic environment and possible release in the blood circulation. The toxicity of ENX-loaded particles on Caco-2 cells decreased when decreasing the amount of PTA. The triblock and diblock particles dramatically enhanced ENX uptake and transport across Caco-2 cells as compared to the ENX solution. However, the different structures of the copolymers slightly affected ENX transport. These results suggested that P(CatCLCL)2-PEG and P(CatCLCL)-mPEG copolymers would be potential carriers for oral delivery of ENX.
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https://hal.univ-lorraine.fr/hal-02923630
Contributor : Thomas Chaigneau <>
Submitted on : Thursday, August 27, 2020 - 12:05:06 PM
Last modification on : Tuesday, October 13, 2020 - 10:46:52 AM

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Pimchanok Charoongchit, Jiraphong Suksiriworapong, Shirui Mao, Anne Sapin-Minet, Philippe Maincent, et al.. Investigation of cationized triblock and diblock poly( ε -caprolactone)-co-poly(ethylene glycol) copolymers for oral delivery of enoxaparin: In vitro approach. Acta Biomaterialia, Elsevier, 2017, 61, pp.180-192. ⟨10.1016/j.actbio.2017.08.006⟩. ⟨hal-02923630⟩

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