Preparation And Characterization Of Transferrin And Adriamycin Conjugates

Serum human holo-transferrin(tf) has been widely used in drug delivery systems, especially in targeting and intellectualized delivery system. By using glutaraldehyde as a bridge, the conjugates of adriamycin(ADR) with transferrin were prepared . The conjugate nanoparticles were divided into larger size and smaller size by centrifugation. Both larger size and smaller size were studied respectively and compared with each other in various parameters.The morphology and sizes of ADR and Tf conjugates (Tf-ADR) was investigated by transmission electron microscope(TEM) and atomic force microscope(AFM). The result showed that the smaller size conjugates appeared discrete and spherical particles with smooth surfaces and a scale of diameter from 50 to 100nm, and the larger size conjugates appeared smooth surfaces and a scale of diameter from 200 to 300nm in size.High-performance liquid chromatography indicated that ADR was reacted with Tf and that ADR strongly binds to Tf. The conjugates were characterized for its ingredient by high-performance liquid chromatography. The conjugation number of ADR and Tf conjugates, was also discussed respectively by absorbance spectrometry and fluorescence quenching method and high-performance liquid chromatography in this article , the smaller size approximately is 2, the larger size approximately is 4.Several mathematical models of drug release were discussed to fit the vitro release of ADR from the conjugation. The release profiles of the conjugates could fit better both first order release model and Higuchi release model. Drug release with a little initial burst and a little cumulate fraction. Results indicated that the ratios of drug release are related to pH and temperature. In general, the smaller size particles have higher release ratios of ADR.