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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 PublicationInternational Journal of Pharmaceutics
ISSN18733476 03785173
Volume522Issue:1-2Pages:21-33
AbstractMitochondria 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.
KeywordGambogic acid Lung cancer Mitochondrial targeting Polymeric micelles
DOI10.1016/j.ijpharm.2017.01.064
URLView the original
Language英語
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Cited Times [WOS]:11   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.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
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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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