Delivery of vinblastine-containing niosomes results in potent in vitro/in vivo cytotoxicity on tumor cells.

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.

Preparation, Characterization and Cytotoxicity of Silibinin- Containing Nanoniosomes in T47D Human Breast Carcinoma Cells.

BACKGROUND: Breast cancer is one of the most frequent cancer types within female populations. Silibinin is a chemotherapeutic agent active against cancer. Niosomes are biodegradable, biocompatible, safe and effective carriers for drug delivery. OBJECTIVE: To prepare nanoniosomal silibinin and evaluate its cytotoxicity in the T-47D breast cancer cell line. MATERIALS AND METHODS: Niosomes were prepared by reverse phase evaporation of a mixture of span 20, silibinin, PEG-2000 and cholesterol in chloroform and methanol solvent (1:2 v/v). The solvent phase was evaporated using a rotary evaporator and the remaining gel phase was hydrated in phosphate buffer saline. Mean size, size distribution and zeta potential of niosomes were measured with a Zetasizer instrument and then nanoparticles underwent scanning electron microscopy. The drug releasing pattern was evaluated by dialysis and the cytotoxicity of nanoniosomes in T-47D cells was assessed by MTT assay. RESULTS: Particle size, size variation and zeta potential of the niosomal nanoparticles were measured as 178.4 ± 5.4 nm, 0.38 ± 0.09 and -15.3 ± 1.3 mV, respectively. The amount of encapsulated drug and the level of drug loading were determined 98.6 ± 2.7% and 22.3 ±1.8%, respectively; released drug was estimated about 18.6±2.5% after 37 hours. The cytotoxic effects of nanoniosome were significantly increased when compared with the free drug. CONCLUSIONS: This study findings suggest that silibinin nanoniosomes could serve as a new drug formulation for breast cancer therapy.