Drug Design, Development and Therapy (Jul 2019)
Delivery of folic acid-modified liposomal curcumin for targeted cervical carcinoma therapy
Abstract
Wen-Yan Wang,1,2 Yun-Xia Cao,2 Xiao Zhou,3 Bing Wei11Department of Obstetrics and Gynecology, The Second Hospital of Anhui Medical University, Hefei, Anhui, 230601, People’s Republic of China; 2Teaching and Research Group of Obstetrics and Gynecology, Anhui Medical University, Hefei, Anhui, 230032, People’s Republic of China; 3Department of Cardiothoracic Surgery, The Second Hospital of Anhui Medical University, Hefei, Anhui, 230601, People’s Republic of ChinaIntroduction: In this study, novel folic acid (FA)-modified curcumin (CUR) liposomes (LPs) were developed and evaluated for their antitumor activity in vitro and in vivo.Methods: Characterization of the LPs, including transmission electron microscopy, morphology, particle size, and zeta potential studies, was carried out. Drug entrapment efficiency, drug-loading capacity, and release properties in vitro were tested. The in vitro growth inhibition activity, cellular uptake efficiency, and cell apoptosis of FA-modified CUR LPs were also investigated by a cervical cancer HeLa cell model.Results: The optimized distearoyl-l-a-phosphatidylethanolamine (DSPE)-PEG2000-FA-LPs/CUR formed spherical vesicles of nanometer sizes and had particle sizes of 112.3±4.6 nm, polydispersity index of 0.19±0.03, and zeta potential of −15.3±1.4 mV. In addition, the EE% and DL% of (DSPE)-PEG2000-FA-LPs/CUR were 87.6% and 7.9%, respectively. Compared with the free drug, FA-modified CUR LPs had sustained-release properties in vitro. In vivo, a strong green fluorescence was observed in the cytoplasmic region after incubation of (DSPE)-PEG2000-FA-LPs/CUR for 2 hrs.Conclusion: (DSPE)-PEG2000-FA-LPs/CUR showed a superior antiproliferative effect on HeLa cells and had a better antitumor effect in vivo than the non-modified LPs. These results indicated that (DSPE)-PEG2000-FA-LPs/CUR was a promising candidate for antitumor drug delivery.Keywords: curcumin, folic acid, liposome, release, cell uptake, antiproliferative, antitumor study, HeLa
