Abstract
Objectives: The present study was aimed to develop Eudragit S100 coated colon-targeted sustained-release formulations of alginate-pectin and alginate-hydroxypropyl methylcellulose microbeads containing norfloxacin (NF) and tinidazole (TZ) for the treatment of amebiasis which was simultaneous estimated.
 Methods: Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for the preparation of formulations. Nine batches (P1-H5) were prepared by taking three independent variables (X1 – drug:polymer ratio, X2 – concentration of sodium alginate, and X3 – curing time) at three levels (1, 2, and 3). Response variables studied for batches (P1-H5) were mean particle size (μm) (Y1), drug entrapment efficiency (% w/w) (Y2), and drug loading (% w/w) (Y3). NF and TZ were simultaneous estimated by ultraviolet spectrophotometric method. Drug-polymer compatibility study was carried out by differential scanning calorimetry and Fourier-transform infrared spectroscopy and indicates no physicochemical interaction.
 Results: Microbeads were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading, and in vitro drug release. The average size of optimized alginate-pectin microbeads was found to be 881±0.05 μm with an entrapment efficiency of 78.50±0.28% (NF) and 86.50±0.32% (TZ) which was simultaneous estimated.
 Conclusion: The studies concluded that formulated enteric-coated alginate-pectin microbeads after enteric coating can be used effectively for the delivery of NF and TZ to colon.
Highlights
Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohn’s disease, amebiasis, colon cancer, and systemic delivery of proteins and peptide drugs [1]
Optimization of process parameters by Taguchi design is an effort to minimize the variation in quality as well as to attain the quality near to the intended value simultaneously [2]
Calcium chloride and HPMC were purchased from SD Fine-Chemicals Ltd., Mumbai, while pectin was procured from Thomas Baker Ltd., Mumbai
Summary
Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohn’s disease, amebiasis, colon cancer, and systemic delivery of proteins and peptide drugs [1].Optimization of process parameters by Taguchi design is an effort to minimize the variation in quality as well as to attain the quality near to the intended value simultaneously [2].Tinidazole (TZ) is the drug of choice in most forms of amebiasis. Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohn’s disease, amebiasis, colon cancer, and systemic delivery of proteins and peptide drugs [1]. Optimization of process parameters by Taguchi design is an effort to minimize the variation in quality as well as to attain the quality near to the intended value simultaneously [2]. Tinidazole (TZ) is the drug of choice in most forms of amebiasis. TZ provided significantly higher cure rates in the treatment of symptomatic intestinal amebiasis. Norfloxacin (NF) is effective orally and is rapidly bactericidal. It has relatively broad spectrum of action and is effective against Gram‐positive and Gram-negative organisms
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