Abstract
Purpose: To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence and to study their effect on alloxan-induced diabetic rats. Methods: Floating microsphere were prepared by emulsion-solvent diffusion method, using hydroxylpropyl methylcellulose, chitosan and Eudragit S 100 polymer in varying proportions. Ethanol/dichloromethane blend was used as solvent in a ratio of 1:1. The floating microspheres were evaluated for flow properties, particle size, incorporation efficiency, as well as in-vitro floatability and drug release. The anti-diabetic activity of the floating microspheres of batch FM4 was performed on alloxaninduced diabetic rats. Result: The floating microspheres had particle size, buoyancy, drug entrapment efficiency and yield in the ranges of 255.32 - 365.65 μm, 75.58 - 89.59, 72.6 - 83.5, and 60.46 - 80.02 %, respectively. Maximum drug release after 24 h was 82.62 % for formulation FM4 and 73.879, 58.613 and 46.106 % for formulations FM1, FM2, and FM3 respectively. In-vivo data obtained over a 120-h period indicate that curcumin floating microspheres from batch FM4 showed the better glycemic control than control and a commercial brand of the drug. Conclusion: The developed floating curcumin delivery system seems economical and effective in diabetes management in rats, and enhances the bioavailability of the drug. Keywords: Gastro-retentive, Sustained release, Bioavailability, Curcumin, Floating microspheres, Diabetes
Highlights
Glucose is necessary for health because it's an important source of energy for the cells that make muscles and tissues
When the blood glucose increases for example, after eating food material, insulin is released from the pancreas to normalize the glucose level [1]
Mean particle size significantly increased with increasing polymer concentration this was due to high viscosity of polymer concentration require high energy for breaking of droplets
Summary
Glucose is necessary for health because it's an important source of energy for the cells that make muscles and tissues. When the blood glucose increases for example, after eating food material, insulin is released from the pancreas to normalize the glucose level [1]. Curcumin could attenuate tumor necrosis factor- (TNF-α) levels and plasma free fatty acids. It inhibits nuclear factor-kappa β (NF- β) activation and protein carbonyl [5] lipid peroxidation. Floating microspheres are gastroretentive drug delivery systems based on a non-effervescent approach. These microspheres are characteristically free-flowing powders having a size < 199 μm and remain buoyant over gastric contents for a prolonged period. The objective of present study was to develop a floating drug delivery system of Curcumin and to study their therapeutic effectiveness on alloxan induced diabetic rats. Ingredient Curcumin (mg) Eudragit S100 (mg) Chitosan (mg) HPMC (mg) Dichloromethane:ethanol 1:1 (ml) Tween 80 (ml)
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