Peptide functionalized actively targeted MoS2 nanospheres for fluorescence imaging-guided controllable pH-responsive drug delivery and collaborative chemo/photodynamic therapy.

The combination of imaging and different therapeutic strategies into one single nanoplatform often demonstrates improved efficacy over monotherapy in cancer treatments. Herein, a multifunctional nanoplatform (labelled as MPRD) based on molybdenum disulfide quantum dots (MoS2 QDs) is developed to achieve enhanced antitumor efficiency by integrating fluorescence imaging, tumor-targeting and synergistic chemo/photodynamic therapy (PDT) into one system. First, polyethylene glycol (PEG)ylated MoS2 QDs (MP) with desirable stability are synthesized via a hydrothermal process using MoS2 QDs and carboxyamino-terminated oligomeric PEG as raw materials. Then, MP were conjugated with arginine-glycine-aspartic acid (RGD) peptide via amidation to form a novel nanocarrier (MPR), which possesses strong blue fluorescence, good biocompatibility and ανß3 receptor-mediated targeting ability. More importantly, MPR generated reactive oxygen species under 808 nm laser activation to realize targeted antitumor PDT. Further doxorubicin (DOX) was loaded onto MPR, which endows MPRD with localized chemotherapy and pH-responsive drug release. The MPRD exhibits improved chemotherapy performance on HepG2 cells (overexpressing integrin ανß3) owing to enhanced cellular uptake mediated by ανß3 receptor and effective drug release triggered by intracellular pH. Notably, MPRD with efficient tumor targeting ability and high chemo/PDT efficacy under NIR laser irradiation is capable of inhibiting HepG2 tumor cell growth both in vitro and in vivo, which is significantly superior to each individual therapy. These findings demonstrate that MPRD holds great potential in effective cancer therapy.

A Polydopamine-Coated Platinum Nanoplatform for Tumor-Targeted Photothermal Ablation and Migration Inhibition.

In this work, Arg-Gly-Asp (RGD) peptide-coupled polydopamine-modified mesoporous platinum nanoparticles (mPt@PDA-RGD NPs) were developed for targeted photothermal therapy (PTT) and migration inhibition of SKOV-3 cells. mPt@PDA-RGD NPs with obvious core/shell structure demonstrated high photothermal performance under 808-nm near-infrared (NIR) laser irradiation. mPt@PDA-RGD NPs with favorable biocompatibility exhibited remarkable SKOV-3 inhibition ability under NIR laser irradiation. Moreover, compared to mPt@PDA NPs, the RGD-functionalized NPs achieved more tumor uptake and PTT performance, which was attributed to the specific interaction between RGD of NPs and αvß3 integrin overexpressed by SKOV-3. Importantly, cell scratch experiments indicated that the photothermal effect of mPt@PDA-RGD NPs can effectively inhibit the migration of surviving SKOV-3 cells, which was assigned to disturbance of the actin cytoskeleton of SKOV-3. Thus, mPt@PDA-RGD NPs presented great potential for targeted tumor photothermal ablation and migration inhibition.

A near-infrared triggered upconversion/MoS2 nanoplatform for tumour-targeted chemo-photodynamic combination therapy.

The combination of photodynamic therapy and chemotherapy has shown a great potential in cancer treatment. As a promising photosensitizer, MoS2 quantum dots (QDs) have limited application due to the low tissue penetration of its light absorbing wavelength in the ultraviolet and visible regions. For the purpose of utilizing MoS2QDs in higher NIR absorption region, herein, we constructed a core/shell nano-photosensitizer upconversion@MoS2 with doxorubicin loading. This nanoplatform can convert 980 nm NIR into visible light, activating MoS2QDs to produce reactive oxygen species through fluorescence resonance energy transfer. In addition, this nanoplatform presented good biocompatibility and tumor targeting after polyethylene glycol and folic acid modification. Interestingly, with pH-responsive drug release performance, this nanoplatform presented efficient chemotherapy effects. Thus, the tumour-targeted nanoplatform can achieve up-converted luminescence imaging guided chemo-photodynamic synergistic therapy effectively.

A multifunctional nanoplatform based on graphitic carbon nitride quantum dots for imaging-guided and tumor-targeted chemo-photodynamic combination therapy.

Graphitic carbon nitride quantum dots (g-CNQDs) have shown great potential in imaging, drug delivery and photodynamic therapy (PDT). However, relevant research on g-CNQDs for PDT or drug delivery has been conducted separately. Herein, we develop a g-CNQDs-based nanoplatform (g-CPFD) to achieve simultaneously imaging and chemo-photodynamic combination therapy in one system. A g-CNQDs-based nanocarrier (g-CPF) is first prepared by successively introducing carboxyamino-terminated oligomeric polyethylene glycol and folic acid onto the surface of g-CNQDs via two-step amidation. The resultant g-CPF possesses good physiological stability, strong blue fluorescence, desirable biocompatibility, and visible light-stimulated reactive oxygen species generating ability. Further non-covalently loaded doxorubicin enables the system with chemotherapy function. Compared with free doxorubicin, g-CPFD expresses more efficient chemotherapy to HeLa cells due to improved folate receptor-mediated cellular uptake and intracellular pH-triggered drug release. Furthermore, g-CPFD under visible light irradiation shows enhanced inhibition on the growth of cancer cells compared to sole chemotherapy or PDT. Thus, g-CPFD exhibits exceptional anti-tumor efficiency due to folate receptor-mediated targeting ability, intracellular pH-triggered drug release and a combined treatment effect arising from PDT and chemotherapy. Moreover, this nanoplatform benefits imaging-guided drug delivery because of inherent fluorescent properties of doxorubicin and g-CPF, hence achieving the goal of imaging-guided chemo-photodynamic combination treatments.