The use of gelatin microparticles to delay the release of readily water-soluble materials

The adsorption of D-arabinose onto gelatin microparticles demonstrated a Langmuirian adsorption pattern. Evaluation of the dissolution behaviour of D-arabinose-loaded gelatin microparticles suggested that the saccharide, loaded at a level below the adsorption saturation level, was released uniformly over a 14-h period after the loaded gelatin microparticles had been lyophilized for a second time. When dissolution curves were corrected for the initial burst effect seen after the gelatin microparticles had been loaded at higher levels of D-arabinose and lyophilized, steady-state release rates were also evident over prolonged periods. In addition, it was evident that the D-arabinose was adsorbed onto internal surfaces of the hydrated gelatin matrix. Calculation of this internal surface demonstrated the influence of the concentration of the glutaraldehyde used as a cross-linking agent and this parameter, in turn, influenced both the adsorption maxima and the subsequent equilibrium release rates. Application of this data base to a highly water-soluble complex polysaccharide antineoplastic agent, which has a higher molecular weight (22.4 kDa vs 150 Da), demonstrated similar behaviour in that a near zero-order release pattern over at least 16 h could be obtained by attention to the conditions under which the gelatin microparticles were made and subsequently loaded before lyophilization.