含苯硼酸材料在药物投递中的研究进展  

Advances of phenylboronic acid-containing materials in drug delivery

作　　者：吕娟[1] 马如江[1] 史林启[1,2] 

机构地区：[1]南开大学高分子化学研究所药物化学生物学国家重点实验室功能高分子材料教育部重点实验室,天津300071 [2]天津化学化工协同创新中心,天津300071

出　　处：《科学通报》2016年第19期2113-2123,2199-2201,共11页Chinese Science Bulletin

基　　金：国家自然科学基金(21274001;51390483;91527306);天津市应用基础与前沿技术研究计划(15JCYBJC29700);教育部创新团队支持计划(IRT1257)资助

摘　　要：苯硼酸(PBA)及其衍生物是一类非天然的人工合成的二醇类物质识别体,在水溶液中可以与具有邻二醇或间二醇结构的多羟基化合物可逆反应形成共价复合物.近年来,基于PBA与二醇类物质可逆结合,人们对含有PBA的材料在糖尿病和癌症治疗相关药物投递领域进行了广泛深入的研究,取得了显著的成果.本文综述了该领域最新的研究进展,重点关注了含PBA材料的癌细胞靶向性和刺激响应性,包括葡萄糖响应性、pH响应性、三磷酸腺苷(ATP)响应性和H_2O_2响应性,并对今后的深入研究进行了展望.Phenylboronic acid（PBA） and its derivatives are a kind of synthetic chemicals which can recognize diols via reacting reversibly with them in aqueous solutions. Recently, based on the reversible covalent PBA/diol complexes, strategies to construct drug delivery system for diabetes treatments and cancer therapy have made enormous progress. Diabetis mellitus have greatly increased all over the world in recent decades. With the regular use of insulin in diabetes treatment, there is a high demand of insulin self-regulated release system responding to glucose concentration in vivo. Since the apparent p Ka value of PBA and its derivatives is around 8.2–8.6, which is higher than human physiological p H 7.4, efficient glucose-responsiveness of PBA-based polymer materials could not be obtained at physiological p H and glucose level. Recently, studies to construct this insulin release system based on PBA polymer materials have made enormous progress, such as reducing the p Ka of the PBA group, achieving ＂on-off＂ release of insulin according to the change of glucose concentration and so on. Similar to diabetes treatments, significant efforts have recently been made to develop drug delievery system based on PBA polymer materials in cancer therapy. Traditional chemotherapy has disadvantages such as poor permeability, short resident time, and toxic side effects. Therefore, the ideal drug delivery carrier should possess tumor targeting ability to prolong the retention time and enhance the aggregation of carriers in tumors. Inaddition, carriers should release drugs and degrade in response to intracellular triggers when inside the cancer cells, in order to increase delivery efficiency and reduce toxicity. The recognition ability of boronic acid to polyol residues in cell membranes enables PBA-functionalized nanocarriers to specific target to sialic acid groups, which are overexpressed on tumor cells. The high affinity and specificity of PBA to SA could significantly improve drug accumulation and retention in tumor, and i

关 键 词：苯硼酸 药物投递 刺激响应性 糖尿病 癌症 

分 类 号：O627.31[理学—有机化学] TQ460.1[理学—化学]