Effect of Additives on Dissolution and Swelling of Soybean Lecithin Microcapsules Prepared Using the Wurster Process

Abstract

Microcapsules whose membranes contained soybean lecithin (SL), cholesterol (CH), stearic acid (SA) and polyvinylpyrrolidone (PVP) at various compositions were prepared. Then, dissolution and swelling behaviors of the microcapsules in a 0.9% saline solution were studied to be related to the phase diagram of three components containing 42% of PVP in anhydrous state. In the aqueous solution, when an anhydrous microcapsule membrane was composed of SL not saturated with both CH and SA, the microcapsules showed rapid release of carbazochrome sodium sulfonate (CCSS, a model drug), poor particle-swelling and spouting of droplets containing CCSS. Long-delayed relase of CCSS and drastic particle-swelling with no spouting of droplets were observed when the anhydrous membrane was composed of SL saturated with both CH and SA and the composition was not close to the two-component line, CH-SA, or to the saturation line. The spounting of droplets would be attributable to the CH and/or SA-poor SL phase and to the SL phase which dissolved CH and SA, but contained either CH or SA only in a small amount, and the delayed relase would be due to the CH and SA-rich SL phase dissoleving a great amount of CH and SA formed by hydration. The degree of release suppression and particle-swelling depended on the SL content. At 20-45% of SL content, the prologed-release, great particle-swelling and no spouting of drolets at the early stage were observed only when the CH and SA-rich SL phase formed by hydration contained a high content of CH and SA.