Study On The Solid Lipid Nanoparticles Of Tartaric Acid And

In this present study, the SLNs were prepared by improved cold homogenization technique and the vinorelbine bitartrate （VB） was selected to be the model drug.The glyceryl monostearate was selected as the lipid material prepared SLNs because of its comparative good compatibility with VB. 15% sugar and 1% bile salt were selected as the lyophilization protectors.The particle sizes of VB-SLNs were assayed by a Zetasizer and the range of particle sizes were 150-350 nm, the zeta potentials were about + 20mV. The atomic force microscopy （AFM） images displayed that the shape of the SLNs was irregular sphere with smooth surface. The highest drug entrapment efficiency of VB-SLNs could reach up to 80%. The results of drug release behavior studies suggested that the drug release could last for 48 h, and the accumulative release amount of drug can reach to about 50%-70%. After PEG modification, the drug entrapment efficiency decreased in a certain degree, but it was still above 60%. The rate of drug release was accelerated and the accumulative release amount of drug can reach to about 80% within 48 h.MCF-7 （Human breast adenocarcinoma cell line） and A549 （human alveolar basal epithelial cell line） were employed to study the uptake to SLNs by cancer cells. RAW264.7 （A mouse macrophage cell line） was employed to investigate the phagocytosis to pSLNs by MPS. The results from cellular uptake indicated that the phagocytosis of VB-pSLNs by RAW264.7 cells was inhibited effectively by the PEG modification of SLNs, while the uptake by cancer cells （MCF-7 and A549） could be improved significantly. Furthermore, the anticancer activity in vitro of VB-SLNs and VB-pSLNs was assayed on the MCF-7 and A549 cell lines. The assay of anticancer activity in vitro demonstrated that the anticancer activity of VB was significantly enhanced by the encapsulation of SLNs and pSLNs due to the increased cellular intemalization of drug. The 50% growth inhibitory concentration （IC50） of free VB, VB-SLNs and VB-10%pSLNs on MCF-7 cell lines was about 7.64μg/ml, 1.18μg/ml and 0.322μg/ml, respectively. The IC₅₀ value of free VB, VB-SLNs and VB-10%pSLNs on A549 cell lines was 8.28μg/ml 2.68μg/ml and 0.580μg/ml, respectively. The anticancer activity in vitro on MCF-7 and A549 cell lines of VB was enhanced 6.5 folders and 2.68 folders by entrapping VB into SLNs, respectively. The numbers on MCF-7 and A549 cell lines can reach to 23.7 folders and 14.3 folders by entrapping VB into 10%pSLNs, respectively.The paper provided a method to prepare SLNs loading hydrophilic drug, which could be used in industry. Both VB-SLNs and VB-pSLNs with comparative higher drug entrapment efficiency displayed ideal stability. The results suggested that the VB-SLNs and VB-pSLNs had the potential to be used in clinical.