Physicochemical properties and controlled drug release of microcapsules prepared by simple coacervation.

Ternary phase diagrams of gelatin-water-methanol, gelatin-water-ethanol, and gelatin-water-propanol systems were prepared to evaluate optimal coacervation. The results of their evaluation suggested that the optimal coacervation region expands with the hydrophobicity of the added poor solvent (methanol, ethanol, 1-propanol, and 2-propanol). Microcapsules prepared based on the optimal coacervation region differed in controlled drug release among poor solvents used even when the concentration of gelatin, a membrane component, is the same. Compared with microcapsules prepared using the gelatin-water-ethanol system, those prepared using the gelatin-water-propanol system showed a 34% decrease in the drug release rate 24h after the initiation of the drug release test. These results suggested that microcapsules prepared using gelatin-water-various lower alcohol systems can readily control drug release and can be a useful drug delivery system (DDS).

Rheological properties of reversible thermo-setting in situ gelling solutions with the methylcellulose-polyethylene glycol-citric acid ternary system (2): Effects of various water-soluble polymers and salts on the gelling temperature.

The influences of various salts and water-soluble polymers on the phase transition temperature of thermo-setting gels prepared by combining methylcellulose (MC)-sodium citrate (SC)-polyethylene glycol (PEG) at appropriate ratios (the MC-SC-PEG system) were investigated. Concerning cations, comparison of the phase transition temperature between SC and tripotassium citrate (PC) showed a rapid increase in the viscosity of SC between 20 degrees C and 25 degrees C and an increase in the viscosity of PC between 30 degrees C and 35 degrees C. Concerning the valency of anions, comparisons among SC, disodium tartrate dihydrate (ST), disodium maleate hemihydrates (SM), and sodium sulfate (SS) showed a rapid increase in the viscosity of trivalent SC between 20 degrees C and 25 degrees C and changes in the viscosity of the three bivalent sodium salts (ST, SM, and SS) at > or =30 degrees C. Thus the phase transition temperature decreased with an increase in the valency of anions. Subsequently, the influences of various water-soluble polymers on the gelling temperature were compared. Using polyvinylpyrrolidone (PVP) instead of PEG, the gelling temperature decreased with an increase in the PVP concentration even without the addition of SC. Unlike PVP, the addition of xanthan gum as a viscosity-increasing polysaccharide did not reduce the gelling temperature irrespective of its concentration. Temperature-associated changes in viscosity were observed at a fixed SC concentration with changes in the concentration of PVP or PEG. The gel phase transition temperature increased from 46 degrees C to 50 degrees C in gels not containing PVP or PEG. The viscosity did not differ between the addition of PVP or PEG at a low concentration and its absence. However, the viscosity clearly changed after the addition of each agent at a high concentration.