Abstract

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

Highlights

  • The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy

  • There are two types of diabetes [3]: (1) diabetes insipidus (DI) and (2) diabetes mellitus (DM); it is a disorder that is characterized by the excretion of large amounts of severely diluted urine and excessive thirst with reduction of fluid intake having no effect on the concentration of the urine

  • Diabetes mellitus (DM) is a group of metabolic disorder in that the person has high blood sugar, either because cells do not respond to the insulin that is produced by the body or body does not produce enough insulinIt has several types of various symptoms of diabetes which are as follows: polyphagia, blurred vision, loss of weight, and polyuria

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Summary

Introduction

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Stability study was carried out for 3 months It indicated no significant change in particle size and zeta potential. Repaglinide depresses blood glucose concentrations by stimulating the release of insulin from beta cells of pancreatic islet tissue. This is done by a selective ion channel mechanism. Decreasing the particle size by formulating nanocrystal may increase the surface area. The decreased size increases the surface area and solubility of drug and there is proportionate increase in the bioavailability of poorly soluble drugs

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