期刊
AAPS JOURNAL
卷 19, 期 3, 页码 814-826出版社
SPRINGER
DOI: 10.1208/s12248-017-0057-9
关键词
aptamer; EGFR-mutated lung cancer; liposomal complexes; stability; TDDS
资金
- Ministry of Science and Technology of China [2015CB931804]
- Natural Science Foundation of China [U150520007, 81571802, 81273548]
- Natural Science Foundation of Fujian Province [2016J06020]
- Fujian Development and Reform Commission [2014/168]
Lung cancer is the leading cancer and has the highest death rate. The epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) erlotinib has had a promising response in lung cancer therapy. Unfortunately, individuals with TKI-resistant EGFR mutations often develop acquired resistance against erlotinib. To overcome this resistance, in the present study, we developed liposomes anchored with anti-EGFR aptamer (Apt)conjugated chitosan (Apt-Cs) as stable carriers to deliver erlotinib to the target. We loaded erlotinib into Apt-Cs-anchored liposomal complexes (Apt-CL-E) and characterized the physicochemistry of Apt-CL-E. The nanoparticles showed good biostability and a binding specificity for EGFR-mutated cancer cells guided by the Apt. The specific binding facilitated the uptake of Apt-CL-E into EGFR-mutated cancer cells. A cytotoxicity study showed an advantage of Apt-CL-E over their nontargeted liposomal counterparts in delivering erlotinib to EGFR-mutated cancer cells, resulting in cell cycle arrest and apoptosis. These results provide a good platform for future in vivo animal studies with Apt-CL-E.
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