Preparation, Characterization, and In Vitro Release of Vinorelbine Tartrate (VLBT)- Loaded Folate-conjugated Recombination Human Serum Albumin (rHSA) Nanoparticles with Different Degree of Cross-linking

Vinorelbine tartrate is a semi-synthetic drug with a broad-spectrum anti-tumor activity. An injectable formulation of vinorelbine (Navelbine® IV) has been widely used in the world, despite existing some disadvantages. In this study, in order to improve the efficacy of vinorelbine injection metabolism with minimal side effects, rHSA nanoparticles entrapping VLBT were prepared by a desolvation procedure, and subsequently decorated by folic acid. A central composite design was applied for modeling the process. To some extent, the drug release rate could be adjusted by cross-linking with different amount of glutaraldehyde. In this paper, FarHSANPs- VLBT with three degrees (25%, 50% and 75%) of cross-linking were obtained under the optimum conditions for preparing the nanoparticles. Then we carried out a further study to compare the characteristics of the nanoparticles, such as drug entrapment efficiency (DEE), drug-loading efficiency (DLE), surface morphology, surface chemistry, physical status of VLBT in Fa-rHSANPs-VLBT, amount of folate conjugation, and release kinetics in vitro. The experiment results displayed that as the degree of cross-linking increased, both the zeta potential (ZP) and folate content associated with the VLBT-rHSANPs showing a reduced tend. Moreover, the increasing glutaraldehyde concentration made the rate of release of the VLBT from these nanoparticles decrease.