Preparation and evaluation of RGD and TAT co-modified paclitaxel loaded liposome.
10.3969/j.issn.1672-7347.2014.08.003
- Author:
Bo GAO
1
;
Weixin MU
Author Information
1. Emergency Department, Fourth Hospital of Hebei Medical University, Shijiazhuang 050000, China gaobohbykd@163.com.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
pharmacology;
Breast Neoplasms;
Cell Survival;
Humans;
Liposomes;
MCF-7 Cells;
drug effects;
Oligopeptides;
chemistry;
Paclitaxel;
pharmacology;
Particle Size;
Peptide Fragments;
chemistry;
Spheroids, Cellular;
drug effects
- From:
Journal of Central South University(Medical Sciences)
2014;39(8):769-774
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To prepare Arg-Gly-Asp (RGD) and cell penetrating peptide TAT co-modified paclitaxel loaded liposome (RGD/TAT-LP-PTX) for MCF-7 cell inhibition.
METHODS:The co-modified liposome was prepared by film-ultrasonic method. The appearance, particle size and zeta potential were evaluated. The cellular uptake by MCF-7 cells in vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD/TAT-LP-PTX was evaluated by MTT assay. Tumor spheroids were used to evaluate anti-tumor ability of RGD/TAT-LP-PTX in vitro.
RESULTS:The particle diameter of the co-modified liposome was (138.8 ± 12.4) nm with the Zeta potential of (25.85 ± 2.75) mV. The entrapment efficiency of PTX was 88.3%. The RGD/TAT-LP uptaken by MCF-7 cells at 4 h was 1.79 times higher than that at 2 h. The co-modified liposome uptaken by MCF-7 cells was 2.25 and 2.72 times higher than that of TAT-LP and RGD-LP, respectively. The anti-proliferation rate of RGD/TAT-LP-PTX increased with time. The inhibition rate of RGD/TAT-LP-PTX for MCF-7 cells at 48 h was 1.78 times higher than that at 24 h. The MTT assay demonstrated the cell viability of RGD/TAT-LP-PTX was 1.65, 1.82 and 2.55 times higher than that of TAT-LP-PTX, RGD-LP-PTX and LP-PTX, respectively.
CONCLUSION:Co-modified liposome may serve as a promising breast cancer delivery system for antitumor drugs.
