The present invention is directed to a composition suitable for forming an implanted light activated drug depot, methods of making the composition, and methods and systems for using the composition. The composition comprises a plurality of drug conjugates, which comprise a drug molecule and a small solubility modulating portion. The drug conjugates are insoluble upon implantation as a drug depot into a subject, and the drug is preferably soluble once cleaved from the depot. One aspect of the invention is directed to a drug conjugate having a modulating portion that modifies the solubility of the drug conjugate by employing a hydrophobic non-polar moiety. Another aspect of the invention is directed to a drug conjugate having a modulating portion that modifies the solubility of the drug by employing a charged moiety that shifts the isoelectric point of the drug conjugate to a physiological pH.
该发明涉及一种适用于形成植入式光活化药物库的组合物,制备该组合物的方法,以及使用该组合物的方法和系统。该组合物包括多种药物共轭物,其中包括药物分子和小溶解度调节部分。这些药物共轭物在植入到受试者体内作为药物库时是不溶的,而一旦从库中解离出来,药物则最好是可溶的。该发明的一个方面涉及具有通过使用疏
水非极性基团改变药物共轭物溶解度的调节部分的药物共轭物。该发明的另一个方面涉及具有通过使用带电基团改变药物溶解度的调节部分的药物共轭物,该基团将药物共轭物的等电点转移到生理pH值。