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Formulation and evaluation of mucoadhesive glipizide microspheres

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Abstract

The purpose of this research was to formulate and system-atically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a cross-linking agent. Results of preliminary trials indicate that volume of cross-linking agent, time for cross-linking, polymer-to-drug ratio, and speed of rotation affected characteristics of microspheres. Microspheres were discrete, spherical, and free flowing. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test and also showed a high percentage drug entrapment efficiency. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X 1), and stirring speed (X 2) on dependent variables percentage mucoadhesion, t80, drug entrapment efficiency, and swelling index. The best batch exhibited a high drug entrapment efficiency of 75% and a swelling index of 1.42; percentage mucoadhesion after 1 hour was 78%. The drug release was also sustained for more than 12 hours. The polymer-to-drug ratio had a more significant effect on the dependent variables. In vivo testing of the mucoadhesive microspheres to albino Wistar rats demonstrated significant hypoglycemic effect of glipizide.

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Authors and Affiliations

  1. Shree S.K. Patel College of Pharmaceutical Education and Research, Ganpat Vidyanagar, Mehsana-Gozaria Highway, 382711, Kherva, India

    Jayvadan K. Patel, Rakesh P. Patel & Madhabhai M. Patel

  2. Nirma Institute of Pharmacy, Nirma University of Science and Technology, Sarkhej-Gandhinagar Highway, 380061, Ahmedabad, India

    Avani F Amin

Authors
  1. Jayvadan K. Patel
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  2. Rakesh P. Patel
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  3. Avani F Amin
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  4. Madhabhai M. Patel
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Correspondence to Jayvadan K. Patel.

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Published: September 20, 2005

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Patel, J.K., Patel, R.P., Amin, A.F. et al. Formulation and evaluation of mucoadhesive glipizide microspheres. AAPS PharmSciTech 6, 10 (2005). https://doi.org/10.1208/pt060110

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