In-vitro and in-vivo evaluation of repaglinide loaded floating microspheres prepared from different viscosity grades of HPMC polymer

Abstract

During the study repaglinide encapsulated floating microspheres were formulated and characterized for enhancing residence time of drug in git and thereby increasing its bioavailability. Floating microspheres of ethylcellulose (EC) and hydroxypropyl methyl cellulose (HPMC) (5 and 100 cps) were prepared by emulsion solvent diffusion technique. During process optimization various parameters were studied such as: drug: polymer ratio, polymer ratio, concentration of emulsifier and stirring speed. Selected optimized formulations were studied for SEM, entrapment, floating behavior, drug release and kinetics. In-vivo floating ability (X-ray) study and in-vivo antidiabetic activity were performed on alloxan induced diabetic rats. Microspheres prepared with different viscosity grade HPMC were spherical shaped with smooth surface. Size of microspheres was in the range of 181.1-248 μm. Good entrapment and buoyancy were observed for 12 h. X-ray image showed that optimized formulation remained buoyant for more than 6 h. Optimized formulation treated group shows significant (p < 0.01) reduction in blood glucose level as compared to pure drug treated group. Repaglinide loaded floating microspheres expected to give new choice for safe, economical and increased bioavailable formulation for effective management of NIDDM.

Diabetes Mellitus: A Review on Pathophysiology, Current Status of Oral Pathophysiology, Current Status of Oral Medications and Future Perspectives

“…Nanoemulsion of repaglinide was characterized as a hopeful carrier for RPG for persistent hypoglycemic effect since showed better hypoglycemic effect in comparison to tablet formulation in experimental diabetic rats 56 Moreover, repaglinide encapsulated floating microspheres were investigated as safe, economical and improved bioavailable formulation showing important (p < 0.01) reduce in blood glucose in contrast to pure drug treated group 57 .Repaglinide-loaded solid lipid nanoparticles (SLNs) were manufactured with a variety of surfactants (Stearic acid and glyceryl mono stearate, phosphatidylcholin, Tween80, Pluronic F127, poly(vinyl alcohol) and poly(vinyl pyrrolidone) and characterized in vitro. It was resulted that the phosphatidylcholin-based SLNs reveal extended drug release time and the highest loading capacity.…”

Ethylcellulose Floating Microspheres of Antidiabetic Agent: In Vitro and in Vivo Evaluation

“…Tissues were fixed in paraffin blocks, sliced and placed onto glass slides. After staining slides were observed and photos were taken using topical microscope [17].…”

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“…[2,21,26] Drug and polymers were mixed in 1:1 mixture of dichloromethane and ethanol at room temperature. The slurry was slowly introduced into 200 ml of 0.25% w/v of polyvinyl alcohol as emulsifier.…”

“…[15,16] It has a half-life of 8-9 h with only 13% of bioavailability and is well absorbed in the upper part of gastrointestinal tract. [17][18][19][20][21] Hence, floating drug delivery system is preferred such that the dosage form can release drug in a controlled manner for a longer duration. By increasing the gastric residence time bioavailability of the drug can be enhanced.…”