Designing dendrimers for ocular drug delivery

作者：Spataro Gregory; Malecaze Francois; Turrin Cedric Olivier; Soler Vincent; Duhayon Carine; Elena Pierre Paul; Majoral Jean Pierre; Caminade Anne Marie^*

来源：European Journal of Medicinal Chemistry, 2010, 45(1): 326-334.

DOI：10.1016/j.ejmech.2009.10.017

• Dendrimers
• Drug delivery
• In vivo assays
• Carboxylic acids
• Ammonium salts
• Carteolol

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.

• 出版日期2010-1