Abstract

Microspheres containing Pioglitazone hydrochloride were prepared by the ionotropic external gelation method, using sodium alginate with four mucoadhesive polymers namely sodium carboxy methyl cellulose, hydroxy propyl methyl cellulose, carbopol 934 P and cellulose acetate phthalate as coat materials. Ionotropic gelation is a method to prepare microspheres using combination of Ca2+ as cationic components and alginate as anion. The practical yield of prepared microspheres using the ionotropic gelation technique was between 172 mg and 604 mg. The result of the Chi-squared test carried out between the actual (practical) and expected (theoretical) yields showed no significant difference (P ex-vivo wash-off test shows the best mucoadhesive property. The in vitro drug release studies do up to 18 h. As observed from the various plots, most of the formulations followed the Korsmeyer-Peppas model.

Highlights

  • Microspheres are discrete particles that make up a multiple unit system

  • Mucoadhesive microspheres can provide the sustained release of drugs and advantage for pioglitazone HCl in the management of type-2 diabetes with a high margin of safety and reduced side effects

  • Pioglitazone hydrochloride a gift sample obtained from Torrent Pharmaceuticals, Ahmadabad, sodium alginate obtained from Loba chemie, mumbai, hydroxy propyl methyl cellulose, carbopol 934 P, cellulose acetate Phthalate from Glenmark Pharmaceuticals, and all chemicals used are of analytical grade

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Summary

Introduction

Microspheres are discrete particles that make up a multiple unit system. Recently, much emphasis has been laid on the development of microspheres dosage forms in preference to single unit systems because of their potential benefits such as increased bioavailability, reduced risk of systemic toxicity, reduced risk of local irritation and predictable gastric emptying. The incorporation of mucoadhesive polymers in the microspheres significantly increases the gastrointestinal transit time of microspheres [1]. It has the desired characteristics suitable for developing mucoadhesive extended release formulations, which include its solubility in acidic pH and a shorter half-life of 3 - 5 h. Mucoadhesive microspheres can provide the sustained release of drugs and advantage for pioglitazone HCl in the management of type-2 diabetes with a high margin of safety and reduced side effects. The present investigation has been carried out to prepare and evaluate mucoadhesive microspheres of pioglitazone HCl employing ionotropic external gelation method using sodium alginate in combination with four mucoadhesive polymers namely sodium carboxy methyl cellulose, carbopol 934 P, hydroxy propyl methyl cellulose, and cellulose acetate phthalate as coat materials

Materials
Preparation of Microspheres
Preformulation Studies
Evaluation of Formulated Microspheres
Morphological Study Using SEM
In-Vitro Dissolution Studies
Mechanism of Drug Release
Zero Order Kinetics
4.10. First Order Kinetics
4.11. Higuchi Model
4.12. Korsmeyer and Peppas Release Model
4.13. Stability Studies
Results and Discussion
Stability Studies
Mucoadhesive Studies
Conclusions
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