Preparation and evaluation of zinc–pectin–chitosan composite particles for drug delivery to the colon: Role of chitosan in modifying in vitro and in vivo drug release

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• 作者：Surajit Das ; ^a ; ^{surajit_das@ices.a-star.edu.sg} ; ^{surajitdas1982@yahoo.com} ; Anumita Chaudhury^a ; Ka-Yun Ng^a
• 关键词：Pectin ; Chitosan ; Zinc ; Drug release ; Colon
• 刊名：International Journal of Pharmaceutics
• 出版年：2011
• 出版时间：15 March 2011
• 年：2011
• 卷：406
• 期：1-2
• 页码：11-20
• 全文大小：835 K

文摘

Zinc–pectin–chitosan composite microparticles were designed and developed as colon-specific carrier. Resveratrol was used as model drug due to its potential activity on colon diseases. Formulations were produced by varying different formulation parameters (cross-linking pH, chitosan concentration, cross-linking time, molecular weight of chitosan, and drug concentration). Single-step formulation technique was compared with multi-step technique. Effect of these parameters was investigated on shape, size, weight, weight loss (WL), moisture content (MC), encapsulation efficiency (EE), drug loading (L), and drug release pattern of the microparticles. The formulation conditions were optimized from the drug release study. In vivo pharmacokinetics of the zinc-pectinate particles was compared with the zinc–pectin–chitosan composite particles in rats. Formulations were spherical with 920.48–1107.56 μm size, 21.19–24.27 mg weight of 50 particles, 89.83–94.34 % WL, 8.31–13.25 % MC, 96.95–98.85 % EE, and 17.82–48.31 % L. Formulation parameters showed significant influence on drug release pattern from the formulations. Formulation prepared at pH 1.5, 1 % chitosan, 120 min cross-linking time, and pectin:drug at 3:1 ratio demonstrated colon-specific drug release. Microparticles were stable at 4 °C and room temperature. Pharmacokinetic study indicated in vivo colon-specific drug release from the zinc–pectin–chitosan composite particles only.