Sahu Piyush Kumar, Mishra Deepak Kumar, Jain Nivrati, Rajoriya Vaibhav, Jain Ashish Kumar
Pharmaceutics Division, Adina Institute of Pharmaceutical Sciences , Sagar, Madhya Pradesh , India.
Drug Dev Ind Pharm. 2015 Apr;41(4):640-9. doi: 10.3109/03639045.2014.891130. Epub 2014 Feb 24.
The present study discusses paclitaxel (PTX)-loaded mannosylated-DSPE (Distearoyl-phosphatidyl-ethanolamine) solid lipid nanoparticles (M-SLNs) using mannose as a lectin receptor ligand conjugate for lung cancer targeting and to increase the anticancer activity of PTX against A549 lung's epithelial cancer cells.
The PTX-SLNs were prepared by solvent injection method and mannose was conjugated to the free amine group of stearylamine. The M-SLNs obtained were characterized for their particle size, polydispersity index, zeta potential and morphology by transmission electron microscope.
The M-SLNs were spherical in shape with 254 ± 2.3 nm average size, positive zeta potential (3.27 mV), 79.4 ± 1.6 drug entrapment efficiency and showed the lower extent of drug release 40% over 48 h in vitro. Cytotoxicity study on A549 cell lines and biodistrubtion study of drug revealed that M-SLNs deliver a higher concentration of PTX as compared to PTX-SLNs in an alveolar cell site.
These results suggested that mannosylated M-SLNs are safe and potential vector for lung cancer targeting.
本研究探讨以甘露糖作为凝集素受体配体共轭物的载紫杉醇（PTX）甘露糖基化 - DSPE（二硬脂酰磷脂酰乙醇胺）固体脂质纳米粒（M - SLNs）用于肺癌靶向，并提高PTX对A549肺上皮癌细胞的抗癌活性。
采用溶剂注入法制备PTX - SLNs，并将甘露糖与硬脂胺的游离氨基共轭。通过透射电子显微镜对所得的M - SLNs进行粒径、多分散指数、zeta电位和形态表征。
M - SLNs呈球形，平均粒径为254±2.3nm，zeta电位为正（3.27mV），药物包封率为79.4±1.6，体外48小时内药物释放率较低，为40%。对A549细胞系的细胞毒性研究和药物的生物分布研究表明，与PTX - SLNs相比，M - SLNs在肺泡细胞部位递送更高浓度的PTX。
这些结果表明，甘露糖基化的M - SLNs是安全且有潜力的肺癌靶向载体。
