The present invention relates to improved prodrugs, and compositions thereof. In particular, it relates to amphiphilic gemcitabine prodrugs or amphiphilic prodrugs of other biologically active molecules with the capacity to make liquid crystalline nanostructured nanoparticles, and uses thereof to treat animals, including humans.

The field of various phototriggered drug release and photoreactions, including reactions generally based on triplet-triplet energy transfer with light excitation at long wavelengths. Systems and methods for absorbing energy in a photosensitizer, and methods for making or using such systems, kits including such systems. The systems and methods comprise transferring that energy by triplet-triplet energy transfer to cleave a cleavable or other active moiety, for instance, in order to cause the release of a releasable moiety. In some cases, these may be contained within a suitable carrier material, for example, a particle or a micelle. Such systems and methods may be used in a variety of applications, including various biological or physical applications. For example, such systems and methods may be useful for delivering drugs or other releasable moieties to regions of a subject.

An isolated cancer-targeting peptide that includes at least two copies of the amino acid sequence PFLP (SEQ ID NO: 1) or PFLF (SEQ ID NO: 2). Also disclosed is a pharmaceutical composition for treating cancer. The composition contains the isolated cancer-targeting peptide and an anti-cancer agent. Further disclosed is a bispecific anti-cancer antibody that includes the isolated cancer-targeting peptide and an antigen-binding peptide that stimulates T cell activity. Methods are provided for treating cancer by administering the pharmaceutical composition or the bispecific anti-cancer antibody. Further provided is a method for diagnosing cancer by administering a radionuclide-labeled cancer-targeting peptide to an individual and imaging a location of the radionuclide.

The present disclosure includes cationic carrier units comprising (i) a water soluble polymer, (ii) a positively charged carrier, and (iii) an adjuvant moiety, wherein when the cationic carrier unit is mixed with an anionic payload (e.g., an antisense oligonucleotide) that electrostatically interacts with the cationic carrier unit, the resulting composition self-organizes into a micelle encapsulating the anionic payload in its core. The cationic carrier units can also comprise a tissue specific targeting moiety, which would be displayed on the surface of the micelle. The disclosure also includes micelles comprising the cationic carrier units of the disclosure, methods of manufacture of cationic carrier units and micelles, pharmaceutical compositions comprising the micelles, and also methods of treating diseases or conditions comprising administering the micelles to a subject in need thereof.

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises

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wherein R′ is —H or —CH.sub.3, wherein R is —NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

The application discloses a functional nucleic acid having nucleoside analog drug integrated into skeleton, a derivative, and preparation methods thereof wherein the derivative is obtained by conjugating or self-assembling the functional nucleic acid having nucleoside analog drug integrated into skeleton with one of a polymer, a hydrophobic molecule, and a transfection reagent. Compared with the prior art, the functional nucleic acid having nucleoside analog drug integrated into skeleton and the derivative thereof can efficiently enter cells and be used to regulate genes; subsequently, the functional nucleic acid having nucleoside analog drug integrated into skeleton can be degraded by nuclease and release active ingredient of the nucleoside analog drug, thus playing a role in chemotherapy. Hence, the functional nucleic acid having nucleoside analog drug integrated into skeleton and the derivative thereof can simply and efficiently realize a combination therapy of gene therapy and chemotherapy, and a complex synthesis procedure is avoided.

The present invention relates to the field of pharmaceutical preparations, in particular, to a mannose modified targeting nano-preparations, a composition for preparing nano-preparations, a targeting element, a targeting vector, a prepared targeting drug and a preparation method and the application thereof. The described nano-preparations with targeting function is composed of the targeting ligand mannose and its derivatives, nano-preparations and main drug components, and the described targeting material is linked with the spacer material, and then linked with the nano-preparations material to prepare the nano-preparations. The targeting nano-preparations in the present invention has good targetability of mannose receptor, can effectively bond with mannose receptor on target cell. Moreover, the preparation method has universality, can be used for synthesizing a variety of targeting nano-preparations, and is conducive to purification and characterization.

The present disclosure provides compositions which shown preferential targeting or delivery of a nucleic acid composition to a particular organ. In some embodiments, the composition comprises a steroid or sterol, an ionizable cationic lipid, a phospholipid, a PEG lipid, and a permanently cationic lipid which may be used to deliver a nucleic acid.

The disclosure is related to compositions and methods comprising spherical nucleic acids (SNAs) and their use in penetrating skin and inhibiting gene expression to develop a scar treatment.

A compound represented by formula (I), or an isomer, a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, pharmaceutically acceptable salts or a prodrug thereof.

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