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Published on:1 January, 2012
Indian Journal of Pharmaceutical Education and Research, 2012; 46(1):52-58
Research Article | doi:NILL

Preparation and In Vitro Characterization of Mucoadhesive Polyvinyl Alcohol Microspheres Containing Amlodipine Besylate for Nasal Administration


Authors and affiliation (s):

N.G.N. Swamy* and Z. Abbas

Department of Pharmaceutics, Government College of Pharmacy, Subbaiah Circle, Bangalore – 560027, India

Abstract:

Amlodipine Besylate microspheres for intranasal administration were prepared with an aim to avoid first-pass metabolism, to achieve controlled blood level profiles and to improve therapeutic efficacy. Polyvinyl Alcohol, a water soluble synthetic polymer, was used in the preparation of microspheres by employing phase separation emulsification technique. The formulation variables were drug concentration, emulsifier concentration, temperature, agitation speed and polymer concentration. All the formulations were evaluated for particle size, particle shape and surface morphology by Scanning Electron Microscopy, percentage yield, drug entrapment efficiency, in vitro mucoadhesion test, degree of swelling and in vitro drug diffusion through sheep nasal mucosa. The microspheres obtained were free flowing, spherical and had a mean particle size of 10.2 ± 3.08 μm to 37.2 ± 1.52 μm very much suitable for nasal delivery. Increasing the polymer concentration resulted in increased drug entrapment efficiency and increased particle size. Amlodipine Besylate was entrapped into the microspheres with an efficiency of 64.5 ± 2.08 % to 83.6 ± 1.05 %. The prepared microspheres revealed good mucoadhesion properties, swellability and sustained the release of the drug over a period of 8 h. The data obtained were analysed by fitment into various kinetic models; it was observed that the drug release was matrix diffusion controlled and the release mechanism was found to be non-Fickian. Stability studies were carried out on select formulations at 50C ± 30C, 250C ± 20C / 60% RH ± 5% RH and 400C ± 20C / 75% RH ± 5% RH for 90 days. The drug content was observed to be within permissible limits and there were no significant deviations in the in vitro mucoadhesion and in vitro drug diffusion characteristics.

Keywords: Mucoadhesive microspheres, Amlodipine Besylate, Phase separation emulsification technique, Drug entrapment efficiency, Degree of swelling, In vitro mucoadhesion studies, Nasal drug delivery

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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