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Formulation and characterization of mucoadhesive microspheres of promethazine hydrochloride for nasal delivery

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Author(s): S.R.Iliger1* and T. Demappa2

Journal: Journal of Pharmacy Research
ISSN 0974-6943

Volume: 4;
Issue: 1;
Start page: 276;
Date: 2011;
Original page

Keywords: Promethazine hydrochloride | blend | hypercholesterolemia | crosslinking

ABSTRACT
Mucoadhesive microspheres of Promethazine hydrochloride in the blend of gelatin and chitosan were developed for intranasal systemic delivery with the aim to avoid first pass metabolism, to improve the patient compliance, to use an alternative therapy to conventional dosage form, to bypass hepatic first pass metabolism, and to increase the therapeutic efficacy of Promethazine hydrochloride in the treatment hypercholesterolemia. The microspheres of blends of gelatinand chitosan were prepared by emulsion crosslinking method using Glutaradehyde as a crosslinking agent. .All the prepared microspheres were evaluated for physical characteristics, such as particle size, incorporation efficiency, swelling index, in vitro bioadhesion using rat jejunum and in vitro drug release in pH 6.6 phosphate buffer. Average particle size of microspheres was found to be in the size range 1 – 50 mm. Increase in drug and polymer concentration in the formulation increased incorporation efficiency. All the microspheres showed good bioadhesive properties and swelling indices and good sustained release of drug. The data indicates the Promethazine hydrochloride release followed Higuchi’s matrix and Peppas model. Stability studies showed stability of formulation at all the conditions to which the formulations were subjected.
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