Abstract

Pioglitazone HCl is an oral anti-diabetic agent used for the treatment of diabetes mellitus type II. The aim of the present work is to evaluate the pharmacodynamic activity of solid lipid nanoparticles of pioglitazone HCL prepared by using solvent injection technique and to compare with the control and test group. Among all the formulations, F5 was found to possess highest in-vitro drug release within 24 hrs i.e., 95.02±1.26%. The in vivo studies were performed using male albino rats of wistar strain (150-200g). Rats were divided in to five groups (n=6), group-I normal, group-II diabetes control, group-III placebo control, group-IV reference, group-V test group. Diabetes was induced by streptazocin (60 mg/kg) by intraperitonial route. The reference group was treated with marketed tablet of pioglitazone HCL, test groups were treated with SLNs suspended in 0.1% Tween 80 and given to animals through oral gavages. Blood samples were collected by retro-orbital puncture before treatment, and after treatment at time intervals 0, 2, 4, 6, 8, 10, 12 and 24h in anti-coagulated vials. Parameters like glucose, tri glycerides (TG), total cholesterol (TC) and HDL-C were estimated by calorimetric method. Diabetes induced rats showed elevated levels of glucose, TG, TC and reduced HDL. The oral administration of drug loaded SLNs in 0.1% Tween 80 solution showed reduced levels of glucose, TG and elevated levels of HDL-C and slightly reduced levels of TG in 24 h where as the marketed tablet showed reduced levels of glucose, TG and TC up-to 12 h and in 24thh the glucose levels get elevated. Thus the optimized SLNs showed prolonged activity.

Highlights

  • Carrier based delivery of a drug molecule to specific organ sites is one of the major thrust area in pharmaceutical sciences

  • These results indicated that the optimized formulation (F5) could function as a prolonged release hypoglycemic drug delivery system to prevent hyperglycemia by lowering the plasma glucose levels for extended period of time without maintenance dose

  • The in-vivo studies showed the significant decrease in glucose levels on oral administration of Pioglitazone HCl SLNs for 24 hrs

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Summary

Introduction

Carrier based delivery of a drug molecule to specific organ sites is one of the major thrust area in pharmaceutical sciences. The scarcity of biocompatible polymers with regulatory approval and their high cost have limited the wide spread application of nanoparticles to clinical medicine [3].To overcome these limitations of polymeric nanoparticles, lipids have been put forward as an alternative carrier, for lipophilic pharmaceuticals. These lipid nanoparticles are known as Solid Lipid Nanoparticles(SLNs) [4]. Pioglitazone HCl is an oral anti-diabetic agent used for the treatment of diabetes mellitus type II [5] It is the drug of choice for the preparation of SLNs since it is highly lipophilic in nature. It is formulated in the form of SLNs to increase the aqueous solubility and for sustained release over a prolonged period of time to maintain the glucose levels by preventing the hyperglycemia [6]

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