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New amphiphilic and pH-sensitive hydrogel for controlled release of a model poorly water-soluble drug.
Eur J Pharm Biopharm. 2009 Nov; 73(3):345-50.EJ

Abstract

This paper presents the development of new pH-sensitive, amphiphilic and biocompatible hydrogels based on alginate-g-PCL, cross-linked with calcium ions to form beads, prepared for controlled delivery of poorly water-soluble drug. We have focused our study on the effect of the length of PCL chains (530 and 1250 g mol(-1)). Swelling profiles obtained clearly indicated that these hydrogels swell slightly (10-14%) in a simulated gastric fluid (pH 1.2), and strongly (700-1300% before disintegration) in a simulated intestinal fluid (pH 6.8). In both media, rates of swelling were lower for beads based on amphiphilic derivatives than for alginate/Ca2+ ones due to the hydrophobic PCL grafts, and decreased when hydrophobic character increased. A model drug, theophylline, was entrapped into these hydrogels and release studies were carried out. The drug was protected in acidic fluid (only 14-20% of release for alginate-g-PCL hydrogel against 35% of release for alginate hydrogel during 350 min). The drug is released completely in neutral fluid due to ion exchanges and disintegration of the hydrogel. PCL leads to decrease in the release kinetics in SIF (2h for alginate-g-PCL/Ca2+ beads against 1h for alginate/Ca2+ beads). It was demonstrated that the establishment of clusters inside beads by intramolecular interactions between PCL grafts of 530 g mol(-1) in salt media allowed to retain the drug and to slow down its release considerably.

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Authors+Show Affiliations

Colinet I
University of Rouen, Mont Saint Aignan, France.
Dulong V
No affiliation info available
Mocanu G
No affiliation info available
Picton L
No affiliation info available
Le Cerf D
No affiliation info available

MeSH

AlginatesCalciumChemistry, PharmaceuticalCross-Linking ReagentsDelayed-Action PreparationsDrug CarriersGlucuronic AcidHexuronic AcidsHydrogelsHydrogen-Ion ConcentrationPolyestersSolubilityTheophylline

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19631739

Citation

Colinet, I, et al. "New Amphiphilic and pH-sensitive Hydrogel for Controlled Release of a Model Poorly Water-soluble Drug." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 73, no. 3, 2009, pp. 345-50.
Colinet I, Dulong V, Mocanu G, et al. New amphiphilic and pH-sensitive hydrogel for controlled release of a model poorly water-soluble drug. Eur J Pharm Biopharm. 2009;73(3):345-50.
Colinet, I., Dulong, V., Mocanu, G., Picton, L., & Le Cerf, D. (2009). New amphiphilic and pH-sensitive hydrogel for controlled release of a model poorly water-soluble drug. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 73(3), 345-50. https://doi.org/10.1016/j.ejpb.2009.07.008
Colinet I, et al. New Amphiphilic and pH-sensitive Hydrogel for Controlled Release of a Model Poorly Water-soluble Drug. Eur J Pharm Biopharm. 2009;73(3):345-50. PubMed PMID: 19631739.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - New amphiphilic and pH-sensitive hydrogel for controlled release of a model poorly water-soluble drug. AU - Colinet,I, AU - Dulong,V, AU - Mocanu,G, AU - Picton,L, AU - Le Cerf,D, Y1 - 2009/07/23/ PY - 2009/05/12/received PY - 2009/07/15/revised PY - 2009/07/17/accepted PY - 2009/7/28/entrez PY - 2009/7/28/pubmed PY - 2010/1/7/medline SP - 345 EP - 50 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 73 IS - 3 N2 - This paper presents the development of new pH-sensitive, amphiphilic and biocompatible hydrogels based on alginate-g-PCL, cross-linked with calcium ions to form beads, prepared for controlled delivery of poorly water-soluble drug. We have focused our study on the effect of the length of PCL chains (530 and 1250 g mol(-1)). Swelling profiles obtained clearly indicated that these hydrogels swell slightly (10-14%) in a simulated gastric fluid (pH 1.2), and strongly (700-1300% before disintegration) in a simulated intestinal fluid (pH 6.8). In both media, rates of swelling were lower for beads based on amphiphilic derivatives than for alginate/Ca2+ ones due to the hydrophobic PCL grafts, and decreased when hydrophobic character increased. A model drug, theophylline, was entrapped into these hydrogels and release studies were carried out. The drug was protected in acidic fluid (only 14-20% of release for alginate-g-PCL hydrogel against 35% of release for alginate hydrogel during 350 min). The drug is released completely in neutral fluid due to ion exchanges and disintegration of the hydrogel. PCL leads to decrease in the release kinetics in SIF (2h for alginate-g-PCL/Ca2+ beads against 1h for alginate/Ca2+ beads). It was demonstrated that the establishment of clusters inside beads by intramolecular interactions between PCL grafts of 530 g mol(-1) in salt media allowed to retain the drug and to slow down its release considerably. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/19631739/New_amphiphilic_and_pH_sensitive_hydrogel_for_controlled_release_of_a_model_poorly_water_soluble_drug_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(09)00216-1 DB - PRIME DP - Unbound Medicine ER -