Surface modification of liposomes with rhodamine-123-conjugated polymer results in enhanced mitochondrial targeting

被引：63

作者：

Biswas, Swati ^{[1
]}

Dodwadkar, Namita S. ^{[1
]}

Sawant, Rupa R. ^{[1
]}

Koshkaryev, Alexander ^{[1
]}

Torchilin, Vladimir P. ^{[1
]}

机构：

[1] Northeastern Univ, Ctr Pharmaceut Biotechnol & Nanomed, Boston, MA 02115 USA

来源：

JOURNAL OF DRUG TARGETING | 2011年 / 19卷 / 07期

关键词：

Liposomes; rhodamine-123; amphiphilic polymer; mitochondrial targeting; drug delivery; paclitaxel; cytotoxicity; CELL-DEATH; DELIVERY; DNA; DISEASE; DYSFUNCTION; APOPTOSIS; BCL-2; DRUG;

D O I：

10.3109/1061186X.2010.536983

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A novel mitochondrial-targeted liposomal drug-delivery system was prepared by modification of the liposomal surface with a newly synthesized polymer, rhodamine-123 (Rh123)-PEG-DOPE inserted into the liposomal lipid bilayer. This novel polymer was synthesized by conjugating the mitochondriotropic dye Rh123, with the amphiphilic polyethylene glycol-phosphatidylethanolamine (PEG-PE) conjugate. The modified liposomes showed better uptake by cells (HeLa, B16F10) estimated by fluorescence microscopy and FACS analysis. The co-localization study with stained mitochondria as well as with the isolation of mitochondria of the cultured cells after their treatment with Rh123 liposomes showed a high degree of accumulation of the modified liposomes in the mitochondria. We also prepared mitochondrial-targeted and nontargeted paclitaxel (PCL)-loaded liposomes. Mitochondrial-targeted PCL-loaded liposomes demonstrated enhanced cytotoxicity toward cancer cells compared with nontargeted drug-loaded liposomes or free PCL. Thus, Rh123-modified liposomes target mitochondria efficiently and can facilitate the delivery of a therapeutic payload to mitochondria.

引用

页码：552 / 561

页数：10