Polymorphic behavior of sprayed lipid micropellets and its evaluation by differential scanning calorimetry and...

Considering the importance of polymorphism occurring in solid dosage forms causing instability, the polymorphic behavior of spray-dried and -congealed lipid micropellets was examined by differential scanning calorimetry and scanning electron microscopy. The results showed that both of the spraying processes exert an important effect on their polymorphic and crystallization properties. In spray-drying, due to the rapid solvent evaporation, the obtained lipid micropellets possess an unstable polymorphic form. This unstable form transforms gradually toward a stable form by storage at elevated temperatures. The same modifications were observed with spray-congealed lipid micropellets. The type of glyceride (composition, chain length), solvent and drugs (estradiol cypionate, medroxyprogesterone acetate) and, further, the presence of a stabilizing agent such as lecithin affect the polymorphic transition and its rate.