Preparation of cross-linked guar gum nanospheres containing tamoxifen citrate by single step emulsion in situ polymer cross-linking method

Abstract

In the present work, guar gum nanospheres containing tamoxifen citrate (TC) were prepared and characterized for using it as a carrier for targeted drug delivery. Tamoxifen is a non steroidal drug used in the treatment of breast cancer. The compound administered to patients is the citrate salt of the trans isomer, tamoxifen citrate. Single step emulsion in situ polymer crosslinking technique was employed to prepare polymer coated drug nanoparticles. Model polymer used in this study was guar gum, which is commonly used for colon specific drug delivery in the pharmaceutical industry. During preparation four-different drug loading solvents were tried and dichloromethane provided the best drug loading result. Briefly, 5 mg drug was dissolved in dichloromethane and emulsified with an aqueous solution of guar gum using span 80 as emulsifier. Cross-linking was made by the use of cross linker glutaraldehyde during the process. A core shell type particles were observed. Drug load was confirmed by FT-IR and quantitated by HPLC. Nanoparticles were further characterized for particle size and morphology. Particle size between 200 and 300 nm were obtained. Influence of process variables on the size of nanoparticles were studied. It was observed that the concentration of polymer and stabilizer determined the size of nanoparticles.