由α-氨基酸合成pH响应超分子聚多肽纳米粒用于联合化学和光热治疗  

Synthesis of pH-responsive supramolecular polypeptide nanoparticles from α-amino acids for combined chemo-photothermal therapy

作　　者：钱红云 党慧萍 滕畅畅 尹大龙 闫立峰[1] Hongyun Qian;Huiping Dang;Changchang Teng;Dalong Yin;Lifeng Yan(Department of Chemical Physics,University of Science and Technology of China,Hefei 230026,China;Department of Hepatobiliary Surgery,the First Affiliated Hospital of USTC,Division of Life Sciences and Medicine,University of Science and Technology of China,Hefei 230001,China)

机构地区：[1]中国科学技术大学化学物理系,安徽合肥230026 [2]中国科学技术大学附属第一医院肝胆外科,安徽合肥230001

出　　处：《中国科学技术大学学报》2023年第3期47-52,I0003,共7页JUSTC

基　　金：This work was supported by the Fundamental Research Funds for the Central Universities(YD2060002015);the National Natural Science Foundation of China(51873201,82172071);the Key Research and Development Program of Anhui Province(202104b11020025).

摘　　要：以α-氨基酸为原料,首先合成了l-谷氨酸和l-赖氨酸的N-硫代羧酸酐单体(NTA),而后聚合制备了聚多肽共聚物P(Glu-co-Lys)。该共聚物可以通过超分子自组装形成聚多肽纳米粒,可以包裹憎水性药物。形成的纳米粒具有pH响应特性,在正常生理环境中(pH 7.4)纳米粒稳定存在,但在肿瘤弱酸性环境中(pH 5.5)纳米粒解体并可释放出包裹的药物。采用该超分子纳米粒可同时负载化疗药阿霉素(DOX)和近红外光热染料(HQS-Cy),细胞实验表明,该纳米粒可以实现pH响应的负载药物和染料的递送,并可以实现近红外二区荧光成像引导的化疗-光热治疗的联合治疗。A new smart supramolecular polypeptide copolymer P(Glu-co-Lys)was synthesized by the polymerization ofα-amino acids using the N-thiocarboxylic acid anhydride(NTA)method,using the pH dynamic response peptide of L-glutamic acid and L-lysine as a carrier for tumor cells.The drug delivery system activated by external acid can self-as-semble(pH 7.4)and disassemble(pH 5.5)under the adjustment of pH to load the drug and control its release.Doxycyc-line(DOX)and the photothermal reagent hydrophilic quanternary stereo-cyanine(HQS-Cy)were loaded into the peptide copolymer to obtain HQS-Cy/DOX nanoparticles(NPs)for chemo-photothermal therapy.Gentle photothermal heating can enhance the absorption of drugs by cells and enhance the efficacy of chemotherapy.In addition,chemo-photothermal ther-apy can solve the defect of easy recurrence after single photothermal therapy.The ingenious nanodrug delivery system of HQS-Cy/DOX NPs provides great potential for the improvement of chemo-photothermal therapy and will achieve excel-lent therapeutic effects in cancer treatment.

关 键 词：有机近红外染料 纳米粒 聚多肽 化疗 光热治疗 

分 类 号：TQ460.1[化学工程—制药化工]