Formulation and evaluation of anti-diabetic activity of repaglinide nanosuspension

Abstract

Diabetes is one of those metabolic disorders that are typically characterized by an increase in blood glucose level, glycosuria and ketonemia. This widely spread disease and its complications result in thickening of vascular tissue, PVD, neuropathy and retinopathy. Repaglinide is the first member of the newer class of drugs that are designed to lower the postprandial glucose. The most prevalent problem faced by those drugs are very low solubility and thereby causing the oral delivery very inefficient leading to low bioavailability and improper dose and release proportionality. Research attempts are being put towards enhancing the oral bioavailability of repaglinide kind of lipophilic drugs to improve the clinical effect. Out of those methods to improve the solubility and bioavailability, Nano suspensions have been a promising method to facilitate the above problem. Nano suspensions can be applied to enhance the solubility of Repaglinide too. So, in this research, Repaglinide particle size reduction has been performed, and nanosuspensions were tested for their clinical efficacy invivo. A nanoprecipitation method was developed to prepare Repaglinide nanosuspension using poloxamer as a stabilizer. The prepared formulations had been tested for the clinical efficacy invivo in albino Wistar rats. The results showed that the nanosuspensions have been very efficient in lowering the postprandial blood glucose levels and also facilitated the consistent release of the drug, which is evident from the constant lowering of glucose level. The prepared nanosuspensions showed a very potent and found to clinically efficient compared to the pure drug and drug suspensions.