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Physicochemical principles of controlled release solid dispersion containing a poorly water-soluble drug

Version 2 2024-06-04, 06:09
Version 1 2019-03-08, 11:30
journal contribution
posted on 2024-06-04, 06:09 authored by Thao Truong-Dinh Tran, Phuong Ha-Lien Tran, Jisung Lim, Jun Bom Park, Soon-Kuk Choi, Beom-Jin Lee
BACKGROUND: The aim of this study was to investigate the physicochemical properties of polyethylene oxide (PEO)-based controlled release solid dispersions (CR-SDs) containing aceclofenac, Gelucire 44/14, poloxamer 407 and pH modifier (Na2CO3). RESULTS: The immediate release solid dispersions containing the pH modifier greatly enhanced the drug dissolution rate to approximately 100%, while the CR-SDs with PEO showed controlled release. A bigger droplet size and a higher surface charge for the CR-SDs were observed compared with the immediate release solid dispersions. The pH modifier played an important role in modulating the release rate of the drug through changes in the drug crystallinity and the hydrogen-bonding interaction, as well as the microenvironmental pH. Near-infrared images revealed a modulation of the PEO concentration to preserve the pH modifier within the system for controlled release of the drug. CONCLUSION: The dissolution process of PEO-based solid dispersions containing a water-insoluble drug was governed by the changing net effect of the microenvironmental pH, the surface charge, the particle size and the release rate of the pH modifier, as well as the function of PEO in controlling drug release.

History

Journal

Therapeutic delivery

Volume

1

Pagination

51-62

Location

London, Eng.

ISSN

2041-5990

Language

eng

Publication classification

C1.1 Refereed article in a scholarly journal

Copyright notice

2010, Future Science Ltd

Issue

1

Publisher

Future Science