Authors: Patil, Sanjay; Sawant, Krutika

Source: Journal of Microencapsulation, Volume 26, Number 5, August 2009 , pp. 432-443(12)

Publisher: Informa Healthcare

Abstract:

The present research work was aimed at development and optimization of alginate mucoadhesive microspheres of carvedilol for nasal delivery to avoid first pass metabolism and to improve the therapeutic efficacy in the treatment of hypertension and angina pectoris. The microspheres were prepared by a water-in-oil (w/o) emulsification technique. A 23 factorial design was employed with drug : polymer ratio, calcium chloride concentration and cross-linking time as independent variables while particle size of the microspheres and in vitro mucoadhesion were the dependent variables. Regression analysis was performed to identify the best formulation conditions. Particle size was analysed by dynamic laser light diffraction technique and found to be in the range of 26.36-54.32 µm, which is favourable for intranasal absorption. The shape and surface characteristics were determined by scanning electron microscopy (SEM) which depicted the spherical nature and nearly smooth surfaces of the microspheres. The percentage encapsulation efficiency was found to be in the range between 36.62-56.18. In vitro mucoadhesion was performed by adhesion number using sheep nasal mucosa and was observed in a range from 69.25-85.28. Differential scanning calorimetry and X-ray diffraction results indicated a molecular level dispersion of carvedilol in the microspheres. In vitro release studies in pH 6.2 phosphate buffer indicated non-Fickian or anomalous type of transport for the release of carvedilol from the microspheres.

Keywords: Microspheres; sodium alginate; carvedilol; factorial design; nasal delivery

Document Type: Research article

DOI: http://dx.doi.org/10.1080/02652040802456726

Affiliations: 1: New Drug Delivery Research Laboratory, TIFAC Center of Relevance and Excellence in NDDS, Pharmacy Department, The M. S. University of Baroda, Vadodara, Gujarat, India

Publication date: 2009-08-01

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