期刊
JOURNAL OF MATERIALS CHEMISTRY
卷 21, 期 47, 页码 19114-19123出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c1jm13576g
关键词
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资金
- National Fund for Distinguished Young Scholars [50888001]
- National Science Foundation of China [21090352]
- National Basic Research Program (973 Program) [2009CB526403]
- Program for Changjiang Scholars and Innovative Research Team in University of China
- Department of Defence Breast Cancer Idea Award [BC083821]
- CDMRP [BC083821, 544639] Funding Source: Federal RePORTER
Cationic polymer polyethyleneimine (PEI) can carry DNA across the cell membrane and enter the nucleus, and thus can be a very useful carrier for nuclear drug delivery; however, its highly positive charges make it toxic and not applicable for systemic drug delivery. Here, well-defined linear PEI (M-n = 1000 or 1500 or 2000)-block-polycaprolactone (M-n 2000) (LPEI-PCL) was synthesized and used to fabricate a pH-triggered charge-reversal nanoparticle to solve this problem. LPEI's secondary amines are amidized as acid-labile beta-carboxylic amides (LPEI/amide-PCL). LPEI/amide-PCL formed negatively charged nanoparticles with very low toxicity and low interaction with cells. Once in an acidic environment, the amides hydrolyze to regenerate the amine groups, producing LPEI-PCL nanoparticles carrying cationic charges. The LPEI-PCL escapes from the lysosomes and traverses into the nucleus. Folic-acid targeting groups are introduced to render the nanoparticles cancer-cell targeting capability. The nanoparticles efficiently enter folate-receptor overexpressing cancer cells and traverse to their nuclei. The DOX loaded in the carrier shows much improved cytotoxicity to cancer cells.
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