Journal
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 42, Issue 8, Pages 1283-1290Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/03639045.2015.1125915
Keywords
Colonic drug delivery; dissolution test; ionotropic gelation; mucoadhesion; multiparticulate system
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Funding
- CNPq (Centro Nacional de Desenvolvimento Cientifico e Tecnologico)
- FAPESP (Fundacao de Amparo a Pesquisa do Estado de Sao Paulo)
- CAPES (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior)
- Faculdade de Ciencias Farmaceuticas de Araraquara - UNESP
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Gellan gum microspheres were obtained by ionotropic gelation technique, using the trivalent ion Al3+. The percentage of entrapment efficiency ranged from 48.76 to 87.52% and 2(2) randomized full factorial design demonstrated that both the increase of polymer concentration and the decrease of crosslinker concentration presented a positive effect in the amount of encapsulated drug. Microspheres size and circularity ranged from 700.17 to 938.32m and from 0.641 to 0.796m, respectively. The increase of polymer concentration (1-2%) and crosslinker concentration (3-5%) led to the enlargement of particle size and circularity. However, the association of increased crosslinker concentration and reduced polymer content made the particles more irregular. In vitro and ex vivo tests evidenced the high mucoadhesiveness of microspheres. The high liquid uptake ability of the microspheres was demonstrated and the pH variation did not affect this parameter. Drug release was pH dependent, with low release rates in acid pH (42.40% and 44.93%) and a burst effect in phosphate buffer pH (7.4). The Weibull model had the best correlation with the drug release data, demonstrating that the release process was driven by a complex mechanism involving the erosion and swelling of the matrix or by non-Fickian diffusion.
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