Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray di raction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this property signi cantly increased with higher pH values. SDs allowed drug dissolution to occur in a controlled manner. HPMCP decreased the dissolution rates in the acid medium. The mucoadhesiveness of SDs was demonstrated and the permeability of AZT carried in solid dispersions was signi cantly improved. The e ect of the SD carrier polymers on blocking e ux pump can be an important approach to improve the bioavailability of AZT.
1Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista “Júlio de Mesquita Filho, UNESP, Araraquara, São Paulo, Brasil, 2Universidade de Sorocaba, Sorocaba, São Paulo, Brasil
Brazilian Journal of Pharmaceutical Sciences vol. 52, n. 4, oct./dec., 2016 http://dx.doi.org/10.1590/S1984-82502016000400016