Vinblastine (VB), as a chemotherapeutic agent, is widely used in treatment of different types of
cancer. However, its clinical application is limited due to its low water solubility, side effects, and multidrug resistance. The aim of this study was to increase the therapeutic efficacy of VB using drug delivery systems. For this purpose, a PEGylated niosomal formulation of
vinblastine (Pn-VB) was prepared by thin film hydration method and physicochemically characterized. Drug release pattern was performed by dialysis diffusion method. The cytotoxicity of Pn-VB was investigated against murine
lung cancer TC-1 cells using MTT assay and its
tumor inhibitory effect was evaluated in lung
tumor-bearing C57BL/6 mice. Mean particle size, zeta potential, entrapment, and loading efficiency of
niosomes were obtained to be about 234.3 ± 11.4 nm, -34.6 ± 4.2 mV, 99.92 ± 1.6%, and 2.673 ± 0.30%, respectively. While, the mean particle size and zeta potential for non-PEGylated
niosomes were obtained about 212.4 nm and -31.4 mV, respectively. The in vitro release pattern of
drug from
niosomes showed a sustained release behavior. Pn-VB indicated a significant increase in toxicity against TC-l cells as compared to free VB. In animal model, Pn-VB exhibited stronger
tumor inhibitory effect and longer life time in comparison to free VB. In conclusion, Pn-VB showed appropriate stability, high-entrapment efficacy, lower releasing rate, and stronger cytotoxic activity against
lung cancer TC-1 cells as compared to free
drug. Thus, the Pn-VB could be a promising formulation for delivery of
vinblastine to
tumor cells with enhanced
drug bioavailability and therapeutic efficacy.