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Alkaloids U 0600Synthesis and Cytotoxicity Studies of Thiazole Analogues of the Anticancer Marine Alkaloid Dendrodoine. -Among a variety of dendrodoine analogues, the derivative (IIIc) shows significant in vitro cytotoxicity against a panel of human cancer cell lines. -(REJI, T. F. A. F.; DEVI, S. K. C.; THOMAS, K. K.; SREEJALEKSHMI, K. G.; MANJU, S. L.; FRANCIS, M.; PHILIP, S. K.; BHARATHAN, A.; RAJASEKHARAN*, K. N.; Indian J. Chem.

Background: Mathematical modelling may be able to reduce the number of in vitro experiments and provide an insight into the elementary physical and chemical mechanisms that regulate the rate and degree of drug release. The aim of the present examination was to develop a simple mathematical model to portray drug release from the alginate-type hydrophilic matrix, taking into account the Fickian diffusion of drug and swelling of the matrix using theophylline as the model drug. Results: The nanoparticles show a remarkable swelling in the simulated intestinal fluid. The theoretical drug release values were validated with experimental values by considering diffusion and diffusion with swelling. The experimental value fitted well with the theoretical value predicted based on diffusion. It was found that after 3 h, the entire drug release followed a pure diffusion transport. Conclusions: The numerical model was found to be sufficiently accurate in guessing the drug release from the alginate matrix. The developed model could be extended to quantitatively prognosticate the drug release from hydrophilic spherical matrices.

Alginate/chitosan nanoparticles were synthesized by ionotropic method using natural honey as the stabilizing agent. The nanoparticles were characterized and the potential of these nanoparticles for the controlled oral delivery of antitubercular drug rifampicin was evaluated in terms of entrapment efficiency, swelling behaviour and in vitro release of the drug. Carboxyl content and in vitro cytotoxicity of the nanoparticles were also evaluated. The swelling and in vitro drug release indicates that the system undergoes pH-dependent swelling and release of drug. Drug release was very low in acidic pH and a maximum of only 20 % of the drug was released in 5 h. A sustained release of drug was observed at pH 7.4 and complete release was obtained in 8 h. Kinetics of the drug release was analyzed by fitting the experimental data into Korsmeyer-Peppas equation and show that the mechanism involved in the release was non-Fickian, controlled by a combined mechanism of diffusion and polymer relaxation. This study shows that the obtained nanoparticles can be a potential carrier for the pH controlled oral delivery of rifampicin.