期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 1, 页码 326-334出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.10.017
关键词
Dendrimers; Drug delivery; In vivo assays; Carboxylic acids; Ammonium salts; Carteolol
资金
- Fonds Social Europeen
- CNRS
New series of phosphorus-containing dendrimers, having one quaternary ammonium salt as core and carboxylic acid terminal groups have been synthesized from generation 0 (3 carboxylic acid terminal groups) to generation 2 (12 carboxylic acid terminal groups). These dendrimers react with the neutral form of carteolol (an ocular anti-hypertensive drug used to treat glaucoma) to afford ion pair (saline) species. The solubility in water of these charged dendrimers depends on the generation considered: generation 0 (3 carteolol) is well soluble, whereas generation 1 (6 carteolol) and generation 2 (12 carteolol) are poorly soluble. These dendrimers have been tested in vivo, as vehicle for ocular drug delivery of carteolol to rabbits. (C) 2009 Elsevier Masson SAS. All rights reserved.
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