Triphenylphosphonium-modified poly(ethylene glycol)-poly(ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery

doi:10.1016/j.ijpharm.2017.01.064

	Triphenylphosphonium-modified poly(ethylene glycol)-poly(ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery
	Xu Y.4; Wang S.4; Chan H.F.1; Liu Y.2; Li H.2; He C.4; Li Z.3; Chen M.4
	2017-04-30
Source Publication	International Journal of Pharmaceutics
ISSN	18733476 03785173
Volume	522 Issue:1-2 Pages:21-33
Abstract	Mitochondria are important targets for the intracellular delivery of drugs and DNA. For mitochondria-targeted delivery, a mitochondriotropic molecule, triphenylphosphonium (TPP), was applied to the synthesis of amphiphilic TPP-poly(ethylene glycol)-poly(ε-caprolactone) (TPP-PEG-PCL) polymers. The TPP-PEG-PCL polymer was used to prepare micelles using a solvent evaporation method for the delivery of gambogic acid (GA) (GA-TPP). The micelles were obtained with a favorable particle size of 150.07 ± 11.71 nm and an encapsulation efficiency of 80.78 ± 1.36%, and they displayed homogeneous spherical shapes. The GA-TPP micelles exerted enhanced cytotoxic and pro-apoptotic effect against A549 cells compared to free GA and GA-loaded PEG-PCL (GA-PP) micelles, due to the inhibition of the expression of apoptosis-related proteins and promotion of caspase 3/7 and caspase 9 activity. Notably, the mitochondria-targeting GA-TPP micelles selectively accumulated in the mitochondria, inducing the loss of mitochondrial membrane potential and the release of cytochrome c, thereby achieving improved mitochondria-targeting effects. In conclusion, the GA-TPP micelle system shows great promise for lung cancer treatment by inducing an apoptotic effect via the mitochondrial signaling pathway.
Keyword	Gambogic acid Lung cancer Mitochondrial targeting Polymeric micelles
DOI	10.1016/j.ijpharm.2017.01.064
URL	View the original
Language	英語
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics	Cited Times [WOS]:11 [WOS Record] [Related Records in WOS]
Document Type	Journal article
Collection	University of Macau
Affiliation	1.Columbia University in the City of New York 2.China Academy of Chinese Medical Sciences 3.Guangdong Second Provincial General Hospital 4.Universidade de Macau
Recommended Citation GB/T 7714	Xu Y.,Wang S.,Chan H.F.,et al. Triphenylphosphonium-modified poly(ethylene glycol)-poly(ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery[J]. International Journal of Pharmaceutics,2017,522(1-2):21-33.
APA	Xu Y..,Wang S..,Chan H.F..,Liu Y..,Li H..,...&Chen M..(2017).Triphenylphosphonium-modified poly(ethylene glycol)-poly(ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery.International Journal of Pharmaceutics,522(1-2),21-33.
MLA	Xu Y.,et al."Triphenylphosphonium-modified poly(ethylene glycol)-poly(ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery".International Journal of Pharmaceutics 522.1-2(2017):21-33.

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