Abstract

Lipospheres which represent novel drug delivery vehicles are water-insoluble lipid spheres forming a solid hydrophobic core, with a layer of phospholipids embedded on the surface of the core. Drugs or other biologically active agents may be contained in the hydrophobic core, adhered to the phospholipids, or a combination thereof. Lipid based carrier system (lipospheres) was adopted to eliminate the toxic effects associated with the use of polymers as carrier and entrapment of high amount of poorly bioavailable lipophilic compound. Due to its poor aqueous solubility of Pioglitazone HCl, was selected as drug candidate to develop lipospheres employing the melt dispersion technique. The Pioglitazone HCl - loaded lipospheres were found to be an effective natural carrier in terms of discrete particle size, encapsulation efficiency, and satisfactory in vitro release characteristics. In the presence of cetyl alcohol, the incorporated phospholipid could combine with drug by hydrophilic and hydrophobic interactions, consequently improved the drug entrapment efficiency and produced the sustained release rate.

Highlights

  • Due to several limitations with polymeric delivery systems, extensive attempts are being made to develop alternate carriers

  • The aim of the present study was to assess the feasibility of formulating lipospheres of Pioglitazone HCl by melt dispersion technique and obtaining a suitable release pattern.[1,2,3,4,5]

  • Owing to the finer particle size of lipospheres and presence of a surface stabilized by emulsifier particles, bioavailability of several problematic drugs was found to increase

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Summary

Introduction

Due to several limitations with polymeric delivery systems, extensive attempts are being made to develop alternate carriers. Pioglitazone HCl (PZ), an oral hypoglycemic agent, is one of the most commonly prescribed drugs for the treatment of patients with diabetes mellitus type II. Pioglitazone HCl having Short half-life (3-7 hr) and practically insoluble in water and potent drug, Pioglitazone hydrochloride to be administered in 2 to 3 doses of 15 to 45 mg per day So the strong clinical need of Pioglitazone HCl as develop prolonged and controlled release formulation of this drug for better control on type II diabetes and increase in bioavailability. The aim of the present study was to assess the feasibility of formulating lipospheres of Pioglitazone HCl by melt dispersion technique and obtaining a suitable release pattern.[1,2,3,4,5]

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