scholarly journals An in vitro examination of the impact of polyethylene glycol 400, pluronic P85, and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine

AAPS PharmSci ◽  
2002 ◽  
Vol 4 (4) ◽  
pp. 193-205 ◽  
Author(s):  
Brendan M. Johnson ◽  
William N. Charman ◽  
Christopher J. H. Porter
2021 ◽  
Vol 22 (10) ◽  
pp. 5072
Author(s):  
Olakunle Oladimeji ◽  
Jude Akinyelu ◽  
Aliscia Daniels ◽  
Moganavelli Singh

Advances in nanomedicine have seen the adaptation of nanoparticles (NPs) for subcellular delivery for enhanced therapeutic impact and reduced side effects. The pivotal role of the mitochondria in apoptosis and their potential as a target in cancers enables selective induction of cancer cell death. In this study, we examined the mitochondrial targeted delivery of betulinic acid (BA) by the mitochondriotropic TPP+-functionalized epigallocatechin gallate (EGCG)-capped gold NPs (AuNPs), comparing the impact of polyethylene glycol (PEG) and poly-L-lysine-graft-polyethylene glycol (PLL-g-PEG) copolymer on delivery efficacy. This included the assessment of their cellular uptake, mitochondrial localization and efficacy as therapeutic delivery platforms for BA in the human Caco-2, HeLa and MCF-7 cancer cell lines. These mitochondrial-targeted nanocomplexes demonstrated significant inhibition of cancer cell growth, with targeted nanocomplexes recording IC50 values in the range of 3.12–13.2 µM compared to that of the free BA (9.74–36.31 µM) in vitro, demonstrating the merit of mitochondrial targeting. Their mechanisms of action implicated high amplitude mitochondrial depolarization, caspases 3/7 activation, with an associated arrest at the G0/G1 phase of the cell cycle. This nano-delivery system is a potentially viable platform for mitochondrial-targeted delivery of BA and highlights mitochondrial targeting as an option in cancer therapy.


1987 ◽  
Vol 93 (5) ◽  
pp. 975-985 ◽  
Author(s):  
Ronald J. Sokol ◽  
James E. Heubi ◽  
Nancy Butler-Simon ◽  
H.Juhling McClung ◽  
John R. Lilly ◽  
...  

2003 ◽  
Vol 92 (1) ◽  
pp. 21-26 ◽  
Author(s):  
Erin D. Hugger ◽  
Clayton J. Cole ◽  
Thomas J. Raub ◽  
Philip S. Burton ◽  
Ronald T. Borchardt

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