Abstract
Objective: The main objective of this study was to develop and evaluate the eudragit and HPMC coated metformin hydrochloride floating microspheres, in which HPMC helps in floating and eudragit as a coating material for a site-specific drug release in a controlled manner and the active moiety metformin used as anti-hyperglycemic agent.
 Methods: The floating microsphere was prepared by the solvent evaporation method incorporating metformin as a model drug. The prepared floating microsphere were characterized for particle size, %yield, drug loading and entrapment efficiency, compatibility study, %buoyancy, surface morphology and In vitro drug release and release kinetics.
 Results: The result metformin loaded floating microsphere was successfully prepared and the particle size range from 397±23.22 to 595±15.82 µm, the entrapment efficiency range from 83.49±1.33 to 60.02±1.65% and drug loading capacity range from 14.3±0.54 to 13.31±0.47% and %buoyancy range from 85.67±0.58 to 80.67±1.15%. The FT-IR and X-RD analysis confirmed that no any interaction between drug and excipient, and surface morphology confirmed those particles are sphere. The floating microsphere show maximum 96% drug release in pH 0.1N HCL and follow the Korsmeyer peppas model of the super case-2 transport mechanism.
 Conclusion: These results suggest that metformin loaded floating microspheres could be retain in stomach for long time and give site specific drug release in controlled manner.
Highlights
Most preferred route for drug delivery is the oral route due to its patient compliance and easiness of ingestion and cost-effectiveness
The metformin loaded lower density microsphere were prepared by emulsification (o/w) solvent evaporation method according to the above-described method by varying concentration of polymers (HPMC, eudragit) and metformin
The HPMC and eudragit S100 blend microspheres loaded with metformin hydrochloride were formulated successfully by using a modified solvent evaporation method and optimized the F8 formulation by different parameters like % yield, buoyancy, % drug loading, % entrapment efficiency and micrometric properties
Summary
Most preferred route for drug delivery is the oral route due to its patient compliance and easiness of ingestion and cost-effectiveness. Many different techniques have been developed like tablet capsule syrups etc for delivery of a significant amount of drug at a specific site and time prearranged and systematic manner but this route has numerous physiological problems, like- bypass through GIT at major absorption zone (stomach and upper part of intestine) due to high density and low density retention time resulting incomplete drug release and low efficacy of drug unpredictable absorption due to degradation of drug by stomach acid and enzyme [1], the site specific drug delivery for diabetic through oral route is most challenging task for researchers These difficulties provoked the investigators to develop a DDS known as gastro retentive floating microspheres which performs its actions i.e. its therapeutically active plasma concentration of drug for prolonged period of time, by minimizing the dosing criteria and minimizing the fluctuations in plasma concentration of drug by the pharmacological effect of the drug in a systemic and controlled way. The recent study describes the various Gastro-retentive approaches which are newly developed into leading methodologies in the field of site-specific orally controlled release drug delivery systems
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