| 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 | 522Issue:1-2Pages: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 | |
| Citation statistics | |
| 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. |
| Files in This Item: | There are no files associated with this item. | |||||
Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.
Edit Comment