Sun Zhi-Zhong,Wei Hong-Yuan,Wang Guan-Quan,Zhou Zhi-Jun,He Jia-Heng,Wang Jing,Luo Shun-Zhong
[ 131 I]-5,10,15,20-tetrakis(4-hydroxyphenyl)porphyrin and [ 131 I]-5-(4-aminophenyl)-10,15,20-triphenylporphyrin ( 131 I-TPPOH and 131 I-TPPNH 2 ) were prepared and their biodistribution properties were evaluated in normal Kunming (KM) mice and SMMC-7721 tumor-bearing BALB/c mice. The optimized labeling yields were 98 and 96 % for 131 I-TPPOH and 131 I-TPPNH 2 , respectively. They were stable in vitro saline and in vivo. Both compounds had a specific affinity to liver and lung, and mainly metabolized through liver. They showed a time-dependent accumulation and retainable characteristics in SMMC-7721 tumor. These results supported their potential value for targeted tumor therapy agents.
Song Hu,Wang Guanquan,Wang Jing,Wang Yunhan,Wei Hongyuan,He Jiaheng,Luo Shunzhong
Porphyrin derivatives are usually used for photodynamic therapy (PDT) and labeled with raidonuclide for radiopharmaceuticals. In this work, 5,10,15,20-tetrakis (4-hydroxyphenyl) porphyrin (TPPOH) and 5,10,15,20-tetrakis (4-aminophenyl) porphyrin (TPPNH 2 ) were labeled by 131 I. 131 I-TPPOH and 131 I-TPPNH 2 were cultured with SMMC-7721 and HL-7702 cells for affinity test. The results show high uptake ratios of SMMC-7721 than HL-7702. 131 I-TPPOH and 131 I-TPPNH 2 were performed radionuclide therapy (RNT) and PDT via tumor in situ injection. At 14 days post injection, the volumes of tumors injected 131 I-TPPOH and 131 I-TPPNH 2 diminished 64 ± 11 and 54 ± 10%, respectively. The therapeutic effect is better than either single PDT or single RNT. The combination therapy of PDT and RNT could be a more effectual method for cancer therapy.
Hao Chen,Dong Ye,Yuan Huang,Xinxin Luo,Xiaoyuan Wu,Jinzhi Zhang,Qichao Zou,Hangxing Wang,Suxiao Wang
Protein corona formation can lead to obstructive screening of targeting groups of nanoparticles (NPs). Also, the targeting groups are subjected to physiochemical interactions when exposed to solvents. Here, these two factors can influence NP targeting efficiency. Therefore, it is necessary to prepare a general method of preparing an anti-fouling NPs with protected targeting groups. Here, we designed α-amylase-starch double-layer coated poly (methyl methacrylate- co -acrylic acid) NPs (α-ams-SCMMA NPs), functionalized with aptamer targeting groups and doped with Tetrakis(para-hydraoxylphenyl) porphyrin (TPPOH) as a payload drug. Natural polysaccharide starch and enzyme α-amylase were applied here for thermo-sensitive activation of starch hydrolyzation in order to render the NPs' self-polishing from protein corona effects. During incubation with serum media, the protein corona was formed at the exterior shell of NPs, while the self-polishing process was activated to remove the “protein fouling” when the incubation temperature increased to 37 °C (body temperature). Mechanistically, the starch layer of α-ams-SCMMA NPs was readily hydrolysed by α-amylase, whereby the adsorbed protein corona could be efficiently eliminated and the targeting groups were then presented. With this unique self-polishing NP design, we believe our method can be applied for potential NP applications in cancer therepy due to excellent antifouling property and protected targeting groups.
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