Abstract:

BACKGROUND: For the problems of antitumor drugs targeted therapy and tumor cell multidrug resistance, doxorubicin-loaded alginate nanoparticles improved by coupling human transferrin can be used for targete tumor drug delivery.
OBJECTIVE: To prepare the doxorubicin-loaded alginate nanoparticles modified by human transferrin, to study the characterization and to evaluate the surface protein activities.
METHODS: By means of optimized microemulsion-ionic crosslinking, doxorubicin-loaded alginate nanoparticles were prepared, water-soluble carbodiimide served as a crosslinking agent, then sodium alginate nanoparticles were connected with human transferrin to prepare human transferrin-modified alginate nanoparticles loading doxorubicin. The size and morphology of drug-loaded nanoparticles modified by human transferrin was observed by transmission electron microscope. Encapsulation capability and loading content were analyzed by high-performance liquid chromatography. The immunological activity of human transferrin on the nanoparticles were detected by flow cytometer.
RESULTS AND CONCLUSION: The doxorubicin-loaded alginate nanoparticles modified by human transferrin were round shaped, their mean diameters averaged 170 nm. The dose of doxorubicin could affect the encapsulation rate of the nanoparticles, which achieved the optimal encapsulation efficiency and loading content when adding 10% doxorubicin into nanoparticles. It was about 65 μg human transferrin per milligram of the nanoparticles. The nanoparticles displayed 67.3% fluorescent when eliminated non-specific adsorption on the flow cytometer, which illustrated that most doxorubicin-loaded alginate nanoparticles could couple on the human transferrin antibody and maintained its antibody activity, thus providing sufficient target power for drug-loaded nanoparticles specific targeting to tumor cells. The microemulsion-ionic crosslinking method is reliable and simple, the obtained doxorubicin-loaded alginate nanoparticles modified by human transferrin can be a potential specific targeted drug carrier.