This invention provides compositions for use in distributing active agents for treating a malignant tumor in a subject. The compositions contain RNAi molecules targeted to a human GST-π, along with RNAi molecules targeted to a human p21, and a pharmaceutically acceptable carrier. The carrier can include nanoparticles composed of an ionizable lipid, a structural lipid, one or more stabilizer lipids, and a lipid for reducing immunogenicity of the nanoparticles. This invention further provides methods for preventing or treating a malignant tumor by administering a therapeutically effective amount of an RNAi composition.

An embodiment of the present invention provides a nanocarrier in a micelle structure, a pharmaceutical composition for diagnosis of cancer, comprising the same nanocarrier, and a method for preparing the same nanocarrier. The nanocarrier is obtained by dispersing a water-in-oil nanoemulsion containing an oil phase ingredient, a surfactant, and an aqueous phase ingredient inclusive of a cancer cell fluorescence-inducing substance and a cancer cell-targeting polysaccharide in water to remove the oil phase ingredient, whereby the nanocarrier includes the aqueous phase ingredient.

A micro-nano structure formed by self-assembling a compound represented by formula (I), an isomer thereof, a pharmaceutically acceptable salt, a hydrate or a solvate in an aqueous solution, a preparation method for the micro-nano structure, and use thereof are described. The micro-nano structure has the advantages of having high photothermal conversion efficiency, good photothermal stability, good photothermal effect and photodynamic effect, being easily degraded, and having high safety, and can be passively targeted to tumor sites, having a broad prospect in the diagnosis and treatment of cancers and skin diseases.

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An imaging device includes a body having a first end portion configured to be held in a user's hand and a second end portion configured to direct light onto a surgical margin. The device includes at least one excitation light source configured to excite autofluorescence emissions of tissue cells and fluorescence emissions of induced porphyrins in tissue cells of the surgical margin. A white light source is configured to illuminate the surgical margin during white light imaging of the surgical margin. The device includes an imaging sensor, a first optical filter configured to permit passage of autofluorescence emissions of tissue cells and fluorescence emissions of the induced porphyrins in tissue cells to the imaging sensor, and a second optical filter configured to permit passage of white light emissions of tissues in the surgical margin to the imaging sensor. Systems and methods relate to imaging devices.

Ligand-bimodal nanoparticle conjugates capable of crossing the blood-brain barrier are disclosed. Methods of making and using the conjugates also are disclosed. The bimodal nanoparticle includes a polymeric matrix, one or more magnetic particles disposed within the polymeric matrix or conjugated to an outer surface of the polymeric matrix, and a dye disposed within the polymeric matrix. A ligand for a blood-brain barrier amino acid transporter is conjugated to the outer surface of the bimodal nanoparticle.

Systems and methods are described for using a combination of high-resolution, optical-sectioning imaging modalities to provide quantitative measures of the distribution of a contrast agent in tissue samples by identifying its cellular distribution. In some instances, the systems and methods may be used in an intraoperative setting to guide a biopsy or surgical procedure.

Hypoxia occurs when limited oxygen supply impairs physiological functions and is a pathological hallmark of many diseases including cancer and ischemia. Thus, detection of hypoxia can guide treatment planning and serve as a predictor of patient prognosis. Current methods suffer from invasiveness, poor resolution and low specificity. To address these limitations, various hypoxia-responsive probes (HyPs) for photoacoustic imaging are disclosed. The emerging modality converts safe, non-ionizing light to ultrasound waves, enabling acquisition of high-resolution 3D images in deep tissue. The HyPs feature an N-oxide trigger that is reduced in the absence of oxygen by haem proteins such as CYP450 enzymes. Reduction of HyPs produce a spectrally distinct product, facilitating identification via photoacoustic imaging. HyPs exhibit selectivity for hypoxic activation in vitro, in living cells and in multiple disease models in vivo. HyPs are also compatible with NIR fluorescence imaging, establishing its versatility as a multimodal imaging agent.

Fluorescent nucleobase surrogates capable of Watson-Crick hydrogen bonding are essential probes of nucleic acid structure and dynamics. Their limited brightness and short absorption and emission wavelengths have rendered them unsuitable for single-molecule detection. Herein, we synthesized a new tricyclic pyrimidine nucleoside analogue with a push-pull conjugated system. The resulting C-linked 8-(diethylamino)benzo[b][1,8] naphthyridin-2(1H)-one nucleoside (ABN), exhibits ε.sub.442=20,000 M.sup.−1 cm.sup.−1 and Φ.sub.em,540=0.39 in water, increasing to Φ.sub.em=0.50-0.53 when base paired with adenine in duplex DNA oligonucleotides. Single-molecule fluorescence measurements of ABN using both one-photon and two-photon excitation demonstrate its excellent photostability and indicate that the nucleoside is present to >95% in a bright state with count rates of at least 15 kHz per molecule. This new fluorescent nucleobase analogue, which, in duplex DNA, is the brightest and most red-shifted known, is first to offer robust single-molecule fluorescence detection capabilities.

A therapeutic agent has an antineoplastic drug bonded with an X-ray-cleavable bond to cobalt of cobalamin. In embodiments, the drug is doxorubicin, paclitaxel, methotrexate, erlotinib, chlorambucil, dasatinib, SN38, colchicine, or gefitinib; and in embodiments a Cy5 fluorophore bonded to ribose of the cobalamin. The agent is formed by reducing hydroxocobalamin with zinc, reacting with 3-bromopropylamine to form aminopropyl cobalamin; and linking the drug to the aminopropyl cobalamin by conjugation through a hydroxyl group by carbamate formation with 1, 1′-Carbonyl-di-(1,2,4-triazole). An optional Cy5 handle is added by coupling a 5′ hydroxyl group of a ribose first with ethylene diamine and then with N-hydroxysuccinimide of Cy5. The agent treats cancer by administration in a dose expected to induce apoptosis in cells of the cancer when the light-cleavable bond is cleaved, the cancer absorbs the agent; and the cancer is exposed to X-ray or visible light to cleave the X-ray-light-cleavable bond.

Nanoparticles, nanoparticle conjugates, devices for making nanoparticles and nanoparticle conjugates, and related methods of use and synthesis are described.