Functionalization of mesoporous organosilica nanocarrier for pH/glutathione dual-responsive drug delivery and imaging of cancer therapy process.

A multifunctional drug nanocarrier is developed by incorporating acetaldehyde-modified-cystine (AMC) into mesoporous organosilica nanoparticles (MONs), shortly termed as MONs-AMC. The anticancer drug doxorubicin (DOX) links directly to MONs-AMC through electrostatic interaction between DOX and AMC to produce a conjugate, MONs-AMC-DOX, with a drug loading efficiency of 26.24 ± 1.35%, corresponding to a loading capacity of 0.26 ± 0.01mgmg-1 for DOX. Schiff base AMC contains a -S-S- bond and two -C˭N- bonds which cleave in the presence of certain level of GSH and in an acidic medium, providing MONs-AMC-DOX the capability for triggering pH and glutathione (GSH) dual-responsive drug release. Further, the self-fluorescent nature of AMC offers the tracing capability without the need of fluorescent label, which facilitates real-time tracing of the drug delivery and cancer therapy process. With 10mmolL-1 GSH and at pH 5.0, a drug release efficiency of 52.27 ± 2.84% is achieved. The intracellular drug release process is traced with confocal laser scanning microscope by monitoring the green fluorescence of MONs-AMC-DOX and red fluorescence of DOX with excitation at 408nm and 488nm, respectively. The drug loaded nanocarriers exhibit a time-dependent cellular uptake behavior, providing an enhanced therapeutic effect to A549 cancer cells.

Hu LL ，Meng J ，Zhang DD ，Chen ML ，Shu Y ，Wang JH ... -  《-》

A comparison of mesoporous silica nanoparticles and mesoporous organosilica nanoparticles as drug vehicles for cancer therapy.

Mesoporous silica nanoparticles (MSNs) are promising drug carriers for use in cancer treatment owing to their excellent biocompatibility and drug-loading capacity. However, MSN's incomplete drug release and toxic bioaccumulation phenomena limit their clinical application. Recently, researchers have presented redox responsive mesoporous organosilica nanoparticles containing disulfide (S-S) bridges (ss-MONs). These nanoparticles retained their ability to undergo structural degradation and increased their local release activity when exposed to reducing agents. Disulfide-based mesoporous organosilica nanoparticles offer researchers a better option for loading chemotherapeutic drugs due to their effective biodegradability through the reduction of glutathione. Although the potential of ss-MONs in cancer theranostics has been studied, few researchers have systematically compared ss-MONs with MSNs with regard to endocytosis, drug release, cytotoxicity, and therapeutic effect. In this work, ss-MONs and MSNs with equal morphology and size were designed and used to payload doxorubicin hydrochloride (DOX) for liver cancer chemotherapy. The ss-MONs showed considerable degradability in the presence of glutathione and performed comparably to MSNs on biocompatibility measures, including cytotoxicity and endocytosis, as well as in drug-loading capacity. Notably, DOX-loaded ss-MONs exhibited higher intracellular drug release in cancer cells and better anticancer effects in comparison with DOX-loaded MSNs. Hence, the ss-MONs may be more desirable carriers for a highly efficient and safe treatment of cancer.

Yue J ，Luo SZ ，Lu MM ，Shao D ，Wang Z ，Dong WF ... -  《-》

Facile synthesis of organosilica-capped mesoporous silica nanocarriers with selective redox-triggered drug release properties for safe tumor chemotherapy.

Shen L ，Pan S ，Niu D ，He J ，Jia X ，Hao J ，Gu J ，Zhao W ，Li P ，Li Y ... -  《-》

Smart Cancer Cell Targeting Imaging and Drug Delivery System by Systematically Engineering Periodic Mesoporous Organosilica Nanoparticles.

Lu N ，Tian Y ，Tian W ，Huang P ，Liu Y ，Tang Y ，Wang C ，Wang S ，Su Y ，Zhang Y ，Pan J ，Teng Z ，Lu G ... -  《-》

Cisplatin and doxorubicin high-loaded nanodrug based on biocompatible thioether- and ethane-bridged hollow mesoporous organosilica nanoparticles.

Herein, a mesoporous organosilica nanoparticle (MON) based nanodrug highly loaded with cisplatin (CDDP) and doxorubicin (DOX) (denoted as MONs/CDDP/DOX) has been successfully prepared for the first time. The MONs are characterized with core-contained double hollow shells, thioether and ethane groups separately incorporated frameworks, uniform diameter (420 nm), large surface area (592 m2/g), and ordered pore size (2.5 nm). The safety evaluation of the MONs based on cell viability, haemolytic activity, histological change, and serum biochemical index demonstrates that they have excellent biological compatibility. The efficient uptake of the MONs by human breast cancer MCF-7 cells is further confirmed via confocal laser scanning imaging and flow cytometry. Importantly, the contents of CDDP and DOX in the MONs/CDDP/DOX nanodrug are as high as 120 mg/g and 85 mg/g, respectively. Therefore, the MONs/CDDP/DOX shows a significant improved killing effect against human breast cancer MCF-7 cells compared with sole DOX or CDDP loaded MONs, demonstating the promise of the nanodrug for cancer treatment.

Zhang J ，Weng L ，Su X ，Lu G ，Liu W ，Tang Y ，Zhang Y ，Wen J ，Teng Z ，Wang L ... -  《-》