Abstract
In situ—forming biodegradable polymeric systems loaded with betamethasone (BTM) and betamethasone acetate (BTMA) (5, 7, and 10% (w/w)) were prepared using poly(DL-lactide-co-glycolide) (33% (w/w)), ethyl heptanoate (5% (w/w)), and N-methyl-2-pyrrolidone as biodegradable material, additive, and solvent, respectively. The effects of gamma irradiation, drug loading, and solvent removal on release profiles were evaluated. The drug release in phosphate-buffered solution (pH = 7.4, 37°C) was measured using high-performance liquid chromatography. The release profiles of irradiated and nonirradiated formulations based on BTMA showed a three-phase release pattern, whereas the pattern for BTM was biphasic. Gamma irradiation had no significant effect on the BTMA release profiles ( p>0.05). Unexpectedly, irradiation had a significant effect on release behavior of BTM ( p<0.05); also, the rate of BTM release was decreased with an increase in drug loading up to 10%. The amount of BTM that was released in the burst phase decreased by about 1.4 and 1.5 times for 7 and 10% BTM loading, respectively. The duration of BTM release was more than that of BTMA. Changes in hydrophobicity and hydrogen bonding had a strong effect on the release behavior of the two forms of BTM from the in situ—forming systems.
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