No abstract

Hepatocellular carcinoma (HCC) is characterized by a high mortality and early diagnosis and treatment are critically needed. Ang II type 1 receptor (AT1R) has recently emerged as a potential molecular target for cancer diagnosis and intervention. Here, we labeled angiotensin II (Ang II), an AT1R ligand that is overexpressed in various solid cancers, with the near-infrared fluorescent dye, MPA, and radionuclide technetium-99m, and evaluated its capacity for HCC detection. These analyses were done in vitro using HepG2 (AT1R-positive) and BxPC3 (AT1R-negative) cell lines, and in vivo using a subcutaneous and orthotopic xenograft mouse model by fluorescence and SPECT imaging. Both Ang II-PEG4-MPA- and [99mTc]­Tc-HYNIC-PEG4-Ang II-bound AT1R exhibited a high affinity in vitro and [99mTc]­Tc-HYNIC-PEG4-Ang II displayed an acceptable level of in vitro stability in rat plasma and whole blood. In vivo imaging revealed excellent specific tumor-targeting in HepG2 mouse xenografts models. In vitro and in vivo competition experiments revealed specific Ang II-PEG4-MPA and [99mTc]­Tc-HYNIC-PEG4-Ang II uptake by HepG2 cells and tumors. Altogether, AT1R-positive tumors were successfully detected via fluorescence and SPECT imaging using Ang II-PEG4-MPA and [99mTc]­Tc-HYNIC-PEG4-Ang II, respectively. Given their superior targeting capacity, Ang II-PEG4-MPA and [99mTc]­Tc-HYNIC-PEG4-Ang II are promising tools for HCC detection and warrant clinical translation.

Colorectal cancer (CRC) is the third most common cancer worldwide, and the prognosis of CRC is better with an earlier diagnosis. The presence of the gastrin-releasing peptide receptor (GRPR) has...

A polyelectrolyte microcapsule-based layer-by-layer (LbL) technique has been widely used as a multifunctional vehicle for combined tumor therapy. Meanwhile, with the rapid development of combined tumour therapy, the challenge for designing multifunctional drug delivery system has attracted much more attention. Herein, we developed a new type of microcapsule (MC) system called MPA@siRNA@DOX@MC, which conjugated with siRNA and DOX as well as ICG-Der-02 (MPA) by electrostatic absorption. MPA as indocyanine green (ICG) fluorescence dye, exhibiting high fluorescence emission and photothermal conversion ability under NIR laser irradiation, was uploaded onto this drug system for realizing the controllable drug release and cancer theranostics. In addition, the results revealed that MPA@siRNA@DOX@MC possessed several ideal properties including high drug-loading capacity, excellent siRNA transfection efficiency, siRNA sequence protection and remarkably improved tumour-targeting capacity. Moreover, the combined therapy based on this drug system displayed improved therapeutic efficacy and negligible side effects both in vivo and in vitro experiment. Ultimately, MPA@siRNA@DOX@MC drug delivery system successfully combined the photothermal therapy and chemotherapy with controlled siRNA sequence silencing may have a promising potential in combined tumor therapy.

Combined with an integrin αvβ3 binding element, fusion peptides maintained the prime activity of membrane cracking, simultaneously increasing precision of cancer treatment by using computational simulation technology.