Cargando…
Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects
Aim: To prepare RGD-modified long circulating liposome (LCL) loading matrine (RGD-M-LCL) to improve the tumor-targeting and efficacy of matrine. Methods: LCL which was prepared with HSPC, cholesterol, DSPE-PEG2000 and DSPE-PEG-MAL was modified with an RGD motif confirmed by high performance liquid c...
Autores principales: | , , , , , |
---|---|
Formato: | Texto |
Lenguaje: | English |
Publicado: |
Ivyspring International Publisher
2010
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2894219/ https://www.ncbi.nlm.nih.gov/pubmed/20596360 |
_version_ | 1782183161523863552 |
---|---|
author | Liu, Xiao-yan Ruan, Li-ming Mao, Wei-wei Wang, Jin-Qiang Shen, You-qing Sui, Mei-hua |
author_facet | Liu, Xiao-yan Ruan, Li-ming Mao, Wei-wei Wang, Jin-Qiang Shen, You-qing Sui, Mei-hua |
author_sort | Liu, Xiao-yan |
collection | PubMed |
description | Aim: To prepare RGD-modified long circulating liposome (LCL) loading matrine (RGD-M-LCL) to improve the tumor-targeting and efficacy of matrine. Methods: LCL which was prepared with HSPC, cholesterol, DSPE-PEG2000 and DSPE-PEG-MAL was modified with an RGD motif confirmed by high performance liquid chromatography (HPLC). The encapsulation efficiency of RGD-M-LCL was also detected by HPLC. MTT assay was used to examine the effects of RGD-M-LCL on the proliferation of Bcap-37, HT-29 and A375 cells. The percentage of apoptotic cells and morphological changes in Bcap-37 cells treated with RGD-M-LCL were detected by Annexin-V-FITC/PI affinity assay and observed under light microscope, respectively. Results: Spherical or oval single-chamber particles of uniform sizes with little agglutination or adhesion were observed under transmission electronic microscope. The RGD motif was successfully coupled to the DSPE-PEG-MAL on liposomes, as confirmed by HPLC. An encapsulation efficiency of 83.13% was obtained when the drug-lipid molar ratio was 0.1, and the encapsulation efficiency was negatively related to the drug-lipid ratio in the range of 0.1~0.4, and to the duration of storage. We found that, compared with free matrine, RGD-M-LCL had much stronger in vitro activity, leading to anti-proliferative and pro-apoptotic effects against cancer cells (P<0.01). Conclusion: RGD-M-LCL, a novel delivery system for anti-cancer drugs, was successfully prepared, and we demonstrated that the use of this material could augment the effects of matrine on cancer cells in vitro. |
format | Text |
id | pubmed-2894219 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2010 |
publisher | Ivyspring International Publisher |
record_format | MEDLINE/PubMed |
spelling | pubmed-28942192010-07-01 Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects Liu, Xiao-yan Ruan, Li-ming Mao, Wei-wei Wang, Jin-Qiang Shen, You-qing Sui, Mei-hua Int J Med Sci Research Paper Aim: To prepare RGD-modified long circulating liposome (LCL) loading matrine (RGD-M-LCL) to improve the tumor-targeting and efficacy of matrine. Methods: LCL which was prepared with HSPC, cholesterol, DSPE-PEG2000 and DSPE-PEG-MAL was modified with an RGD motif confirmed by high performance liquid chromatography (HPLC). The encapsulation efficiency of RGD-M-LCL was also detected by HPLC. MTT assay was used to examine the effects of RGD-M-LCL on the proliferation of Bcap-37, HT-29 and A375 cells. The percentage of apoptotic cells and morphological changes in Bcap-37 cells treated with RGD-M-LCL were detected by Annexin-V-FITC/PI affinity assay and observed under light microscope, respectively. Results: Spherical or oval single-chamber particles of uniform sizes with little agglutination or adhesion were observed under transmission electronic microscope. The RGD motif was successfully coupled to the DSPE-PEG-MAL on liposomes, as confirmed by HPLC. An encapsulation efficiency of 83.13% was obtained when the drug-lipid molar ratio was 0.1, and the encapsulation efficiency was negatively related to the drug-lipid ratio in the range of 0.1~0.4, and to the duration of storage. We found that, compared with free matrine, RGD-M-LCL had much stronger in vitro activity, leading to anti-proliferative and pro-apoptotic effects against cancer cells (P<0.01). Conclusion: RGD-M-LCL, a novel delivery system for anti-cancer drugs, was successfully prepared, and we demonstrated that the use of this material could augment the effects of matrine on cancer cells in vitro. Ivyspring International Publisher 2010-06-14 /pmc/articles/PMC2894219/ /pubmed/20596360 Text en © Ivyspring International Publisher. This is an open-access article distributed under the terms of the Creative Commons License (http://creativecommons.org/licenses/by-nc-nd/3.0/). Reproduction is permitted for personal, noncommercial use, provided that the article is in whole, unmodified, and properly cited. |
spellingShingle | Research Paper Liu, Xiao-yan Ruan, Li-ming Mao, Wei-wei Wang, Jin-Qiang Shen, You-qing Sui, Mei-hua Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects |
title | Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects |
title_full | Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects |
title_fullStr | Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects |
title_full_unstemmed | Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects |
title_short | Preparation of RGD-modified Long Circulating Liposome Loading Matrine, and its in vitro Anti-cancer Effects |
title_sort | preparation of rgd-modified long circulating liposome loading matrine, and its in vitro anti-cancer effects |
topic | Research Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2894219/ https://www.ncbi.nlm.nih.gov/pubmed/20596360 |
work_keys_str_mv | AT liuxiaoyan preparationofrgdmodifiedlongcirculatingliposomeloadingmatrineanditsinvitroanticancereffects AT ruanliming preparationofrgdmodifiedlongcirculatingliposomeloadingmatrineanditsinvitroanticancereffects AT maoweiwei preparationofrgdmodifiedlongcirculatingliposomeloadingmatrineanditsinvitroanticancereffects AT wangjinqiang preparationofrgdmodifiedlongcirculatingliposomeloadingmatrineanditsinvitroanticancereffects AT shenyouqing preparationofrgdmodifiedlongcirculatingliposomeloadingmatrineanditsinvitroanticancereffects AT suimeihua preparationofrgdmodifiedlongcirculatingliposomeloadingmatrineanditsinvitroanticancereffects |