首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Designing dendrimers for ocular drug delivery.
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Designing dendrimers for ocular drug delivery.

机译:设计用于眼药递送的树枝状聚合物。

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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.
机译:从第0代(3个羧酸端基)到第2代(12个羧酸端基)已经合成了一系列新的含磷树枝状聚合物,它们以一个季铵盐为核并且具有羧酸端基。这些树枝状分子与中性形式的卡替洛尔(一种用于治疗青光眼的眼用降压药)反应,产生离子对(盐)。这些带电树枝状大分子在水中的溶解度取决于所考虑的世代:第0世代(3个卡替洛尔)易溶,而第1世代(6个卡替洛尔)和第2世代(12个卡替洛尔)难溶。这些树状大分子已经在体内进行了测试,作为卡他洛尔向兔子眼内给药的载体。

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