Microencapsulation of sodium alendronate reduces drug mucosal damage in rats

Pullulan: an advantageous natural polysaccharide excipient to formulate tablets of alendronate-loaded microparticles

“…In addition, both results of gastroresistance (untableted and tableted microparticles) are statistically different (p=0.0034). Comparing the results obtained for untableted AMP (Cruz et al, 2010) and tableted AMP, only pullulan was capable of maintaining the gastroresistance of the microparticulate formulation, which could be explained by its ability to protect the particles against damage caused by the compression force. To corroborate this hypothesis, SEM analyzes of tablet cross-sections were performed.…”

“…Within 120 min, 24.5 ± 0.72% and 27.6 ± 1.18% of alendronate were released from microcrystalline cellulose and lactose tablets, respectively, whereas only 6.7 ± 0.30% of the drug was released from pullulan tablets at the same time. In a previous study (Cruz et al, 2010), it has been shown that about 5% of alendronate was released from Eudragit ® S100 microparticles under the same experimental conditions, which is considered an adequate result since no more than 10% of the drug should be released from a gastroresistant formulation in 2 h of experiment (USP, 2008). In addition, both results of gastroresistance (untableted and tableted microparticles) are statistically different (p=0.0034).…”

“…As previously described (Cruz et al, 2010), alendronate-loaded microparticles (AMP) were prepared by the spray-drying technique. Briefly, an alkaline solution (0.05 mol/L NaOH) of Eudragit ® S100 (16.0 g/L) was prepared under magnetic stirring at 50°C.…”

“…For in vitro release profiles (n=3), experiments were carried out in a dissolution apparatus PTW II (Pharma Test, Brazil): basket, rotation speed of 100 rpm at 37 °C (Cruz et al, 2010). Gastroresistance was evaluated during 120 minutes in 900 mL 0.1 mol/L HCl (pH 1.2).…”

“…A previous study reported the development of gastroresistant microparticles made of Eudragit ® S100 in order to reduce mucosal damage associated with sodium alendronate, an antiosteoporotic drug (Cruz et al, 2010). Although Eudragit ® S100 microparticles can be considered a promising alternative for oral administration of sodium alendronate, microparticles are rarely used directly in their powder form, thus, the development of a final formulation is required.…”