Synthesis, Characterization and In Vitro Assessment of Gellan Gum Tamoxifen Citrate Macrobeads and Nanoparticles

Abstract

Objective: Tamoxifen citrate drug (Brand name: Nolvadex), a Selective Estrogen Receptor Modulator (SERM) is a nonsteroidal triphenylethylene derivative with poor solubility and low oral bioavailability. In the present work, an attempt was made to develop a novel system of Tamoxifen citrate encapsulated macrobeads and nanoparticles using a recombinant Gellan gum synthesized. Method: Gellan gum drug macrobead combination was prepared using the ionotropic gelation method and its nanoparticle was synthesized by emulsion cross-linking technology. Result: The results showed that Gellan gum Tamoxifen citrate nanoparticles were found to be more efficient in encapsulation than Gellan gum Tamoxifen citrate macro-beads. Gellan gum Tamoxifen citrate nanoparticles demonstrated a greater drug release profile in the acidic medium compared to Gellan gum Tamoxifen macrobeads based on the in vitro drug release analysis. SEM analysis showed a smooth surface morphology for nanoparticles and beads with a size below 100 nm for the nanoparticles. The interaction between the chemical compounds was studied using FTIR by analyzing the disappearance or shifting of the frequency of functional groups between the Gellan gum and Tamoxifen citrate drug. Higher cytotoxic effect was shown by Gellan gum Tamoxifen citrate nanoparticles than free Tamoxifen citrate drug in breast cancer cell line MCF-7 in an in vitro cytotoxicity study done using SRB assay, which illustrates the major application of Gellan gum in nanoparticle drug delivery system in various fields of cancer research. Conclusion: Gellan gum nanoparticle system may be employed as a better delivery system for poorly water-soluble drugs like Tamoxifen citrate.