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Vinorelbine tartrate (VLBT), as a kind of high hydrophilic and temperature-induced degradation drug, was prepared into nanoparticles by a desolvation procedure. Bovine serum albumin (BSA), as a drug carrier, was stabilized by chemical cross-linking with glutaraldehyde. Firstly, the optimization process of preparing VLBT-loaded BSA nanoparticles (VLBT-BSANPs) was accomplished using response surface methodology (RSM) by desolvation. Then VLBT-BSANPs were conjugated with folate, namely Fa-BSANPs-VLBT. Hence targeting drug carrier delivery system loading VLBT was produced. In this study, the characteristics of the nanoparticles, such as the amount of folate conjugation, surface morphology, surface chemistry, physical status of VLBT in Fa-BSANPs-VLBT, stability of Fa-BSANPs-VLBT with mannitol and  in vitro  drug release behavior were all investigated. The VLBT-BSANPs were obtained under optimum conditions, with a mean particle size (MPS) of 155.4 nm and a zeta potential (ZP) of −32.97 mV at a pH value of 5.4. Drug loading efficiency (DLE) and drug entrapment efficiency (DEE) of this obtained drug were approximately 45.6% and 90.6%, respectively.

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A Novel Active Targeting Preparation, Vinorelbine Tartrate (VLBT) Encapsulated by Folate-Conjugated Bovine Serum Albumin (BSA) Nanoparticles: Preparation, Characterization and in Vitro Release Study