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Acta Pharmaceutica

The Journal of Croatian Pharmaceutical Society

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Swelling behavior and release properties of pH-sensitive hydrogels based on methacrylic derivatives

Tahar Bartil1 / Mahmoud Bounekhel1 / Calberg Cedric1 / Robert Jeerome1

Département de génie des procédés Faculté des sciences de l'ingénieur, Université ferhat Abbas, SETIF (19000), Algérie1

Centre de recherche et d'étude sur les macromolécules (CERM) B6 chimie, Université de Liège Sart-Tilman, 4000-Liege, Belgique2

This content is open access.

Citation Information: Acta Pharmaceutica. Volume 57, Issue 3, Pages 301–314, ISSN (Online) 1846-9558, ISSN (Print) 1330-0075, DOI: 10.2478/v10007-007-0024-6, September 2007

Publication History

Published Online:
2007-09-18

Swelling behavior and release properties of pH-sensitive hydrogels based on methacrylic derivatives

The purpose of this study is to develop novel intestinal-specific drug delivery systems with pH sensitive swelling and drug release properties. Methacrylic-type polymeric prodrugs were synthesized by free radical copolymerization of methacrylic acid, poly(ethyleneglycol monomethyl ether methacrylate) and a methacrylic derivative of N-(4-hydroxyphenyl)-2-(4-methoxyphenyl) acetamide in the presence of ethylene glycol dimethacrylate as crosslinking agent. The effect of copolymer composition on the swelling behavior and hydrolytic degradation were studied in simulated gastric (SGF, pH 1.2) and intestinal fluids (SIF, pH 7.0). The dynamic swelling behavior of these hydrogels was investigated to determine the mechanism of water transport through these hydrogels. The mechanism of water transport through the gels was significantly affected by the pH of the swelling medium and became more relaxation-controlled in a swelling medium of pH 7.0. The swelling and hydrolytic behaviors of hydrogels were dependent on the content of methacrylic acid (MAA) groups and caused a decrease and increase in gel swelling in SGF and SIF, respectively. Drug release studies showed that the increasing content of MAA in the copolymer enhances hydrolysis in SIF. These results suggest that pH-sensitive systems could be useful for preparation of a muccoadhesive system and controlled release of N-(4-hydroxyphenyl)-2-(4-methoxyphenyl) acetamide.

Oslobađanje ljekovite tvari i bubrenje pH-senzitivnih hidrogelova na bazi metakrilnih derivata

Cilj rada bio je razviti nove pH senzitivne sustave za isporuku lijekova u tankom crijevu te ispitati njihova svojstva bubrenja i oslobađanje ljekovite tvari. Metakrilni polimerni prolijekovi sintetizirani su kopolimerizacijom derivata metakrilne kiseline sa slobodnim radikalima, poli(etilenglikol monometil eter metakrilata) i metakrilnog derivata N-(4-hidroksifenil)-2-(4-metoksifenil) acetamida u prisutnosti etilenglikol dimetakrilata kao sredstva za umrežavanje. Učinak sastava kopolimera na svojstvo bubrenja i hidrolitički raspad proučavan je u simuliranoj želučanoj (SGF, pH 1,2) i crijevnoj tekućini (SIF, pH 7,0). Dinamičko svojstvo bubrenja hidrogelova ispitivano je da bi se odredio mehanizam transporta vode kroz hidrogelove. Mehanizam prijenosa vode značajno je ovisio o pH medija. Bubrenje i hidrolitičko ponašanje hidrogelova ovisilo je o udjelu metakrilne kiseline. U SGF se bubrenje smanjivalo, a u SIF povećavalo. Povećanje udjela metakrilne kiseline u kopolimeru povećavalo je hidrolizu u SIF. Ti rezultati sugeriraju da se pH-senzitivni sustavi mogu upotrijebiti u pripravi mukoadhezivnih sustava i za kontrolirano oslobađanje N-(4-hidroksifenil)-2-(4-metoksifenil) acetamida.

Keywords: pH-sensitive hydrogels; swelling; controlled release; poly(ethylene glycol); poly(methacrylic acid)

Keywords: pH-senzitivni hidrogelovi; bubrenje; kontrolirano oslobađanje; poli(etilenglikol); poli-(metakrilna kiselina)

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