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

Swati Biswas, Namita S Dodwadkar, Rupa R Sawant, Alexander Koshkaryev, Vladimir P Torchilin

Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Boston, MA 02115, USA.

Journal of drug targeting 2011 Aug

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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.

Citation

Swati Biswas, Namita S Dodwadkar, Rupa R Sawant, Alexander Koshkaryev, Vladimir P Torchilin. Surface modification of liposomes with rhodamine-123-conjugated polymer results in enhanced mitochondrial targeting. Journal of drug targeting. 2011 Aug;19(7):552-61