合成具有天冬氨酸接枝的新型树枝状大分子及其提高模型药物水溶性的能力。
Synthesis of novel dendrimers having aspartate grafts and their ability to enhance the aqueous solubility of model drugs.
机构信息
Key Laboratory of Drug Targeting and Drug Delivery System of Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China.
出版信息
Eur J Med Chem. 2010 Jun;45(6):2705-11. doi: 10.1016/j.ejmech.2010.01.069. Epub 2010 Feb 2.
In this study, a series of aspartate based dendrimers with different cores were synthesized in a convergent approach and well characterized by NMR and MS techniques. The aqueous solubility of the model drugs (L-Histidine, Naproxen, Methotrexate) was measured in the presence of this kind of dendrimers at room temperature in PBS buffers at pH 6, 7 and 8. Results clearly confirmed that the solubility enhancement was due to presence of dendrimers at different pH compared to their corresponding aqueous solubility at different pH. The results indicated that the aspartate based dendrimers could be considered as an effective supplement of PAMAM dendrimers in solubility enhancement and drug delivery. The surface groups played an important role in dendrimer-mediated solubility enhancement.
在这项研究中，通过收敛方法合成了一系列具有不同核心的基于天冬氨酸的树状聚合物，并通过 NMR 和 MS 技术进行了很好的表征。在室温下，在 PBS 缓冲液（pH 6、7 和 8）中测量了模型药物（L-组氨酸、萘普生、甲氨蝶呤）在这种树状聚合物存在下的溶解度。结果清楚地证实，与不同 pH 值下的相应水溶液溶解度相比，在不同 pH 值下存在树状聚合物可导致溶解度增强。结果表明，基于天冬氨酸的树状聚合物可被视为提高溶解度和药物传递的 PAMAM 树状聚合物的有效补充。表面基团在树状聚合物介导的溶解度增强中起着重要作用。
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