期刊
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
卷 44, 期 8, 页码 1342-1349出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2018.1449857
关键词
Porphyrin; PAMAM; dendrimers; melphalan; anti-cancer activity
资金
- CONACyT [220675]
- DGAPA [IN101117]
- DGAPA-UNAM
p-[bis(chloro-2-ethyl)amino]-L-phenylalanine (melphalan) is an approved anti-cancer agent with a broad spectrum of antitumor activity. However, it has some disadvantages, such as poor water-solubility followed by rapid elimination, which reduce the target specificity. To solve these problems, porphyrin- poly(amidoamine) or PAMAM-conjugates of melphalan were synthesized and characterized. The dendrimeric conjugates showed satisfactory water solubility. It was found that the size of the dendrimer played a crucial role in controlling the drug content and diameter of the melphalan-conjugates. The in vitro studies of cell cytotoxicity revealed that by employing the dendrimeric conjugation strategy and using the PAMAM dendritic arms as spacers, the conjugates had good anti-cancer activity and lower toxicity than free melphalan.
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