期刊
JOURNAL OF DRUG TARGETING
卷 16, 期 9, 页码 660-667出版社
INFORMA HEALTHCARE
DOI: 10.1080/10611860802201464
关键词
Targeting; folate receptor; nanoemulsion; folate-PEG lipid; PEG-coating; aclacinomycin
资金
- NOF Corporation (Tokyo, Japan)
- Promotion and Mutual Aid Corporation for Private School of Japan
- Scientific of Research from the Ministry of Education, Culture, Sports, Science and Technology, Japan
To investigate the use of folate-targeted nanoemulsion-loaded aclacinomycin A (ACM) to folate receptor (FR)-positive cells, we attempted to optimize the targeting ability of nanoemulsions by modifying the chain length and amount of the folate-PEG linker. Folate-linked, nanoemulsion-loaded ACM were formulated with 0.24mol% of folate-poly (ethylene glycol)3400- (folate-PEG3400-) and folate-PEG5000-distearoylphosphatidylethanolamine (DSPE), and 0.03mol% of folate-PEG5000-DSPE in nanoemulsions. Selective FR-mediated uptake was achieved in a human nasopharyngeal tumor cell line, KB, which overexpresses FR, but not in a human hepatoblastoma cell line, (FR(-)) HepG2. At the same amount of folate modification, the association with KB cells was increased with increasing the PEG-chain length. The association of 0.03and 0.24mol% folate-PEG5000-linked nanoemulsions with cells was 5- and 3.3-fold higher than that of non-folate nanoemulsion, respectively, while their cytotoxicity was similar. Both 0.03 and 0.24mol% folate-PEG5000-linked nanoemulsions and non-folate nanoemulsion following intravenous injection inhibited tumor growth more significantly than ACM solution on day 24 following tumor inoculation (p0.01). This study demonstrates that a folate-linked nanoemulsion is feasible for tumor-targeted ACM delivery, and that folate modification with a sufficiently long PEG-chain and a small amount of nanoemulsion is an effective way of targeting nanoemulsion to tumor cells.
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