Designing dendrimers for ocular drug delivery

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• 作者：Gr&#xe9 ; gory Spataro ; Fran&#xe7 ; ois Malecaze ; C&#xe9 ; dric-Olivier Turrin ; Vincent Soler ; Carine Duhayon ; Pierre-Paul Elena ; Jean-Pierre Majoral ; Anne-Marie Caminade
• 关键词：Dendrimers ; Drug delivery ; In vivo assays ; Carboxylic acids ; Ammonium salts ; Carteolol
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：January 2010
• 年：2010
• 卷：45
• 期：1
• 页码：326-334
• 全文大小：333 K

文摘

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.