pH sensitive polyelectrolyte complex of O-carboxymethyl chitosan and poly (acrylic acid) cross-linked with calcium for sustained delivery of acid susceptible drugs

被引:47
作者
Gujarathi, Nayan A. [1 ]
Rane, Bhushan R. [2 ]
Patel, Jayvadan K. [3 ]
机构
[1] Jodhpur Natl Univ, Dept Pharmaceut Sci, Jodhpur 342003, Rajasthan, India
[2] N Maharashtra Univ, PSGVP Mandals Coll Pharm, Jalgaon, India
[3] N Gujarat Univ, Nootan Pharm Coll, Ahmadabad, India
关键词
O-Carboxymethyl chitosan; Carbopol; Rabeprazole sodium; Mucoadhesive; Ionic gelation method; Polyelectrolyte complex; IN-VITRO EVALUATION; MUCOADHESIVE PROPERTIES; POLY(ACRYLIC ACID); NANOPARTICLES; CARBOPOL; CHITIN; BEADS;
D O I
10.1016/j.ijpharm.2012.07.016
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The present study investigates the ability of a polyelectrolyte complex, composed of O-carboxymethyl chitosan (O-CMC) and carbopol cross linked with calcium, as a pH- sensitive carrier for acid susceptible drugs. DSC studies were performed to confirm the formation of O-CMC-carbopol complex. Double endothermic peaks in thermogram of polyelectrolyte beads reflect the molecular changes brought in after cross-linking. FT-IR spectroscopy was used to reveal peak variation of the carboxylic groups as a function of pH 1.2 and pH 6.8. The formation of polyelectrolyte complex, on account of electrostatic interactions between the -COO- group of carbopol and the -NH3+ group of O-CMC, was also confirmed by FT-IR studies. Swelling of the O-CMC-carbopol film showed a pH-dependent profile that was affected by calcium ion concentration. The swelling rate was more significant at intestinal pH because the ionization of carboxylic acid group on O-CMC and carbopol creates electrostatic repulsion. Release behavior of drug is relative to the viscosity of solution and the ionic interaction between O-CMC and carbopol. Mucous glycoprotein assay revealed that ionization of carboxylic group on the beads at intestinal pH formed a strong hydrogen bond with mucin, which was responsible for the prominent mucoadhesive property thus prolonging the intestinal residence time. (c) 2012 Elsevier B.V. All rights reserved.
引用
收藏
页码:418 / 425
页数:8
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