To enhance the therapeutic activity of drugs known to act on mitochondria of cells, drug delivery approaches must efficiently mediate specific delivery to the subcellular site of action. We hypothesize that functionalization of poly(D,L-lactic-co-glycolic acid)-b-poly(ethylene glycol) (PLGA-b-PEG) polymers with mitochondriotropic triphenylphosphonium cations (TPP) and engineering of size and charge of their nanoparticles (NPs) using a blending approach can facilitate the subcellular delivery of encapsulated drug, zinc-phthalocyanin (ZnPc) to the mitochondria of cells . We synthesized two copolymers PLGA-b-PEG-OH and PLGA-b-PEG-TPP. Targeted NPs with different size and charges were prepared by blending PLGA-b-PEG-TPP with PLGA-COOH or PLGA-b-PEG-OH. In vitro intracellular trafficking showed that the targeted NPs were selectively accumulated in the mitochondria of the cells. The photodynamic activities of ZnPc in targeted and non-targeted NPs against HeLa cells indicated a higher phototoxic effect when the targeted NPs were used. These results provide an engineering strategy for improving organelle-targeting properties of NPs.

Functionalized polymers for mitochondria trafficking of nanoparticles

243rd National Meeting (2012)

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