Park, Ji Sun and Han, Tae Hee and Lee, Kuen Yong and Han, Sung Soo and Hwang, Jung Jin and Moon, Dae Hyuk and Kim, Sang Yoon and Cho, Yong Woo (2006) N-acetyl histidine-conjugated glycol chitosan self-assembled nanoparticles for intracytoplasmic delivery of drugs: Endocytosis, exocytosis and drug release. Journal of Controlled Release, 115 (1). 37 - 45.
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Official URL: http://www.sciencedirect.com/science/article/B6T3D...
Nano-sized vesicular systems (nanoparticles), ranging from 10 nm to 1000 nm in size, have potential applications as drug delivery systems. Successful clinical applications require the efficient intracellular delivery of drug-loaded nanoparticles. Here we describe N-acetyl histidine-conjugated glycol chitosan (NAcHis-GC) self-assembled nanoparticles as a promising system for intracytoplasmic delivery of drugs. Because N-acetyl histidine (NAcHis) is hydrophobic at neutral pH, the conjugates formed self-assembled nanoparticles with mean diameters of 150−250 nm. In slightly acidic environments, such as those in endosomes, the nanoparticles were disassembled due to breakdown of the hydrophilic/hydrophobic balance by the protonation of the imidazole group of NAcHis. Cellular internalization and drug release of the pH-sensitive self-assembled nanoparticles were investigated by flow cytometry and confocal microscopy. NAcHis-GC nanoparticles internalized by adsorptive endocytosis were exocytosed or localized in endosomes. The amount of exocytosed nanoparticles was dependent on the pre-incubation time prior to removal of free nanoparticles from the culture media. Flow cytometry and confocal microscopy showed that NAcHis-GC nanoparticles released drugs into the cytosol and cell cycle analysis demonstrated that paclitaxel-incorporated NAcHis-GC nanoparticles were effective in inducing arrest of cell growth.
|Uncontrolled Keywords:||Nanoparticle; Histidine; Chitosan; Endocytosis; Exocytosis; Endosome; Paclitaxel; Cell cycle arrest|
|Subjects:||Biomedical Science > Nanomedicine|
|Deposited On:||24 Jul 2009 09:56|
|Last Modified:||24 Jul 2009 09:56|
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