Design,Synthesis And Properties Of Intelligent Antitumor Drug Carriers

Intelligent anti-tumor drug carriers have the advantages of controlled drug release,reduction drug toxicity and enhancing bioavailability,which are of great significance for improving the anti-tumor efficacy of chemotherapy drugs.In this study,a series of enzyme-sensitive and ion-responsive hydrogels were constructed based on lysine and drug moleculars as drug carriers.First,the gelator of N-fluorenylmethoxycarbonyl-N-tert-butyloxycar-bonyl-L-lysine-aminomethylbenzoic acid was synthesized.The gel was obtained in PBS（pH=7.4）for the interaction ofπ-πstacking.The gel showed excellent trypsin-sensitivity,characterized by HPLC and SEM.The gel had good drug loading efficiency of doxorubicin and trypsin-sensitively controlled release.Secondly,a kind of repairable hydrogel containing the combination ofγ-aminobutyric acid and lysine was constructed.The trypsin sensitivity and drug release properties of the gel were detected by HPLC.The gel-sol transition realized good trypsin-responsive release of adriamycin and trypsin interpretation and releaseγ-aminobutyric acid.Finally,with amide bond as sensitive group,a both enzyme and ion responsive hydrogel was constructed based on phenylalanine and lysine.The gel has good transaction performance in PBS7.4 buffer solution,and the critical gel concentration was 8mg/m L.The hydrogel had good trypsin sensitivity was verified by HPLC.The gel showed specific response to Ce²⁺cation and BH^4-anion.The sensitive range of BH^4-was between 10^-2mol/L and 10^-1mol/L.This research work provides a new way for sustained-release drug hydrogel drug carriers and combined drug delivery systems.