Development of zinc protoporphyrin micelles for cancer photodymanic therapy with xenon light

本研究通过比较不同ZnPP胶束的理化特性、稳定性和体内药代动力学，发现粒径约为80 nm的HPMA-ZnPP在循环中表现出良好的稳定性，从而延长了血浆半衰期，并具有肿瘤选择性蓄积（EPR效应）。因此，我们选择了HPMA-ZnPP进行进一步的开发。在海拉细胞的体外研究中，HPMA-ZnPP在光照射下表现出很强的细胞毒性。体内实验表明，HPMA-ZnPP对肿瘤生长的抑制具有剂量依赖性和照射依赖性（强度和持续时间）。此外，在体内成像系统中可以清楚地检测到HPMA-ZnPP的肿瘤选择性积累。总之，这些发现强烈表明，HPMA-ZnPP作为一种新的癌症PDT药物的潜力，同时具有肿瘤检测能力。

In this study, by comparing the physiochemical characteristics, stability as well as in vivo pharmacokinetics of different ZnPP micelles, we found that HPMA-ZnPP, with the particle size of about 80 nm, showed good stability in circulation, resulting in prolonged plasma half-life as well as tumor-selective accumulation (EPR effect). We thus selected HPMA-ZnPP for further development. In vitro studies using Hela cells exhibited a strong cytotoxicity of HPMA-ZnPP upon light irradiation. In vivo experiments showed an HPMA-ZnPP dose-dependent and irradiation dependent (intensity and duration) suppression of tumor growth. Moreover, the tumor-selective accumulation of HPMA-ZnPP was clearly detected in an in vivo imaging system. Token together, these findings strongly suggest the potential of HPMA-ZnPP as a new PDT drug for cancer, at the same time with tumor-detecting potency.