Li Wenpan, Xin Xiu, Jing Shasha, Zhang Xirui, Chen Kang, Chen Dawei, Hu Haiyang
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, P. R. China.
J Mater Chem B. 2017 Feb 28;5(8):1601-1610. doi: 10.1039/c6tb03041f. Epub 2017 Feb 3.
Organic metal complexes as a type of hybrid materials have been used for gene delivery. In the present study, a metal organic complex of zoledronate-calcium (CaZol) was prepared for transporting pDNA. Then, the effects of different molar ratios of Ca to Zol (Ca/Zol) on the formulation characteristics were investigated. The results showed that the CaZol/pDNA complexes generated small particles and efficiently encapsulated pDNA when the Ca/Zol ratio was 30. In addition, CaZol complexes could protect pDNA from being degraded by the serum protein since pH-sensitive CaZol exhibited high stability in the physiological environment (pH 7.4), whereas the encapsulated pDNA could be released in a weakly acidic environment (pH 5.5). Moreover, the complex had better cellular uptake efficiency and desired gene expression efficiency in vitro and in vivo. Overall, these results indicated that CaZol, as a potential nanocarrier, was suitable for pDNA delivery.
有机金属配合物作为一种杂化材料已被用于基因递送。在本研究中,制备了唑来膦酸 - 钙(CaZol)金属有机配合物用于转运质粒DNA(pDNA)。然后,研究了不同钙与唑来膦酸摩尔比(Ca/Zol)对制剂特性的影响。结果表明,当Ca/Zol比为30时,CaZol/pDNA复合物产生小颗粒并能有效包封pDNA。此外,由于pH敏感的CaZol在生理环境(pH 7.4)中表现出高稳定性,CaZol复合物可以保护pDNA不被血清蛋白降解,而包封的pDNA可以在弱酸性环境(pH 5.5)中释放。此外,该复合物在体外和体内具有更好的细胞摄取效率和理想的基因表达效率。总体而言,这些结果表明CaZol作为一种潜在的纳米载体,适用于pDNA递送。