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Preparation, Evaluation and Optimization of Antidiabetic in-situ gel of Pioglitazone

  • Unique Paper ID: 166222
  • Volume: 11
  • Issue: 2
  • PageNo: 2804-2813
  • Abstract:
  • This study investigates the formulation and evaluation of an in-situ gel of pioglitazone, a thiazolidinedione used in the management of type 2 diabetes mellitus. The objective is to develop a sustained release system that enhances pioglitazone's bioavailability and therapeutic efficacy while minimizing adverse effects. The in-situ gel is formulated using a thermosensitive polymer, Pluronic F127, which transitions from liquid at room temperature to gel at body temperature, and a pH-sensitive polymer, Carbopol 940, which enhances gel formation upon contact with physiological pH. This dual polymer system facilitates a controlled release of pioglitazone. The formulation process begins with creating a drug-polymer solution, which is characterized for gelation temperature, viscosity, and mechanical properties through rheological studies. Drug release studies are conducted using simulated body fluids to mimic physiological conditions, and the release kinetics are analyzed to understand the mechanisms of drug diffusion and polymer erosion. In vitro studies demonstrate that the in-situ gel formulation has an appropriate gelation temperature close to body temperature, ensuring easy administration and effective gel formation at the site of action. Viscosity measurements confirm the consistency necessary for the transition from liquid to gel under physiological conditions. The drug release profile shows a sustained release pattern with an initial burst followed by a steady release phase, conforming to the Higuchi model, indicative of diffusion-controlled release. Pharmacokinetic evaluation in diabetic animal models compares the bioavailability of the in-situ gel formulation with conventional oral pioglitazone formulations. Results indicate that the in-situ gel significantly enhances pioglitazone bioavailability, maintaining therapeutic plasma concentrations over an extended period, reducing administration frequency, and potentially minimizing side effects associated with peak plasma levels. In vivo efficacy studies in diabetic animal models demonstrate improved glycemic control with the in-situ gel formulation. The sustained release of pioglitazone results in consistent therapeutic effects, leading to better management of blood glucose levels and enhanced insulin sensitivity over time. Histopathological examinations show no significant tissue irritation or adverse reactions at the administration site, supporting the safety of the in-situ gel.
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Cite This Article

  • ISSN: 2349-6002
  • Volume: 11
  • Issue: 2
  • PageNo: 2804-2813

Preparation, Evaluation and Optimization of Antidiabetic in-situ gel of Pioglitazone

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