Gold nanoparticles (AuNPs) and matrix metalloproteinase (MMP)-2 cleavable peptides are clicked into gold nanoparticle clusters (AuNCs) for enhanced drug localization and micro computerized tomography (μCT) theranostic of tumors. AuNPs are co-functionalized with doxorubicin (DOX) and an azide-terminated polymer (DOX/N₃@AuNPs), and the DOX/N₃@AuNPs are associated into [email protected] in the presence of an alkyne-terminated MMP-2 cleavable peptide (alkyne-peptide-alkyne; APA) by click chemistry. MMP-2-dependent dissociation shows that [email protected] are highly sensitive to the MMP-2 and are almost completed digested into single nanoparticles. DOX liberation shows that > 75% of the conjugated DOX is bursted out from the digested [email protected] while < 20% of DOX is released from the integrate [email protected] within 3 h in acidic conditions, suggesting that DOX is only liberated from dissociated [email protected] in acidic conditions. In vivo study shows that [email protected] accumulate in tumor ~ 150 times higher than DOX/N₃@AuNPs do and efficiently suppress tumor growth. Mice administered with AuNCs shows clearer μCT images of tumors. Thus, [email protected] are expected promising carriers for both anticancer therapy and tumor imaging.

将金纳米颗粒（AuNPs）和基质金属蛋白酶（MMP）-2可裂解肽单击到金纳米颗粒簇（AuNCs）中，以增强药物定位和肿瘤的显微计算机断层扫描（μCT）。金纳米粒子是共官能化多柔比星（DOX）和叠氮基封端的聚合物（DOX / N _3个@AuNPs）和DOX / N ₃通过点击化学，在存在炔烃封端的MMP-2可裂解肽（炔烃-肽-炔烃； APA）的情况下，@ AuNP被关联到[电子邮件保护的]中。MMP-2依赖性解离表明[受电子邮件保护]对MMP-2高度敏感，几乎可以完全消化成单个纳米颗粒。DOX释放表明，在酸性条件下3小时内，> 75％的共轭DOX会从消化的[电子邮件保护]中爆发，而<20％的DOX是从整合的[电子邮件保护]中释放出来的，这表明DOX仅从在酸性条件下会解离[受电子邮件保护]。体内研究表明[受电子邮件保护]在肿瘤中蓄积〜比DOX / N ₃高150倍@AuNPs确实并且有效地抑制了肿瘤的生长。给予AuNCs的小鼠显示出更清晰的肿瘤μCT图像。因此，[电子邮件保护的]有望用于抗癌治疗和肿瘤成像。