Celastrol/sodium tanshinone IIA sulfonate-coloaded liposome: Preparation, characterization, and synergistic anti-breast cancer treatment
10.7501/j.issn.0253-2670.2018.22.009
- Author:
Yue QIN
1
Author Information
1. Anhui University of Chinese Medicine
- Publication Type:Journal Article
- Keywords:
Celastrol;
Codelivery liposome;
Film dispersion method;
Sodium tanshinone IIA sulfonate;
Synergistic anti-tumor treatment;
Synergistic effect
- From:
Chinese Traditional and Herbal Drugs
2018;49(22):5271-5279
- CountryChina
- Language:Chinese
-
Abstract:
Objective To explore the preparation technology of celastrol/sodium tanshinone IIA sulfonate-coloaded liposome (Cel/STS-CL) and verify the synergistic anti-breast cancer effects in vitro. Methods The optimal ratio of celastrol to sodium tanshinone IIA sulfonate for synergistic anti-breast cancer effect was explored by MTT assay. The liposome was prepared by conventional film dispersion method. The physiochemical properties and morphology were measured by dynamic light scattering (DLS), HPLC, and transmission electron microscopy (TEM), respectively. Meanwhile, the in vitro synergistic anti-breast cancer effect of liposome was investigated by cellular uptake, antiproliferative assay, and cell apoptosis induction using MCF-7 cells as model. Results Hydrophilic sodium tanshinone IIA sulfonate and hydrophobic celastrol were simultaneously encapsulated into liposomes by film dispersion method. The liposome had a nearly spherical shape with a clear bilayer, as well exhibited the particle sizes of (104.7 ± 2.1) nm, narrow polydispersion index (PDI) of (0.217 ± 0.002), and zeta potential of (-48.8 ± 2.3) mV. The encapsulation efficiency of celastrol and tanshinone IIA sulfonate were (82.2 ± 2.7)% and (66.2 ± 2.3)%, respectively. In cellular studies, the cellular uptake of liposome was 30 times higher than that of control group; The half proliferation inhibitory concentration (IC50) was (1.42 ± 0.12) μmol/L against MCF-7 cells with a combined index as 0.81. Besides, 80% of MCF-7 cells were induced to apoptosis by Cel/STS-CL, which was 0.1 time higher than Cel-Lip. Conclusion The preparation of Cel/STS-CL was feasible and efficiently, and promising for the in vitro synergistic anti-breast cancer effect, as well in the further studies.
