32 results about "Polymeric prodrug" patented technology

A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.

The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

The present invention relates to methods of treating a HER2 positive cancer in mammals. The present invention includes administering a HER2 antagonist in combination with a polymeric prodrug of 7-ethyl-10-hydroxycamptothecin to the mammals in need thereof.

The invention discloses a nano-carrier for drug and gene co-delivery and a preparation method and application thereof, and particularly relates to a co-delivery nano-carrier TCPL-siRNA-PPX for simultaneously carrying a chemotherapeutic drug and a gene-based drug. A polymeric prodrug carrier TCPL, siRNA and a multifunctional polyanionic polymer PPX are self-assembled by electrostatic adsorption between ingredients to form the drug delivery system; a drug and a gene can be targeted to be delivered to the same tumor cell, and moreover, siRNA is released in cytoplasm to silence the Bc1-2 protein, promoting apoptosis and releasing the inhibition of Bcl-2 on lonidamine; the chemotherapeutic drug acting on mitochondria, lonidamine, is delivered to the mitochondria; both cooperatively trigger the apoptosis of the mitochondrial pathway, jointly killing the tumor cell. By in-vitro and in-vivo activity evaluation, the invention proves that the system is better than the simultaneous delivery of each single component, can remarkably increase anti-cancer activity, and has a definite synergistic treatment effect.

The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxy-camptothecin to patients in need thereof.

The invention relates to a reduced response camptothecin prodrug monomer as shown in a formula I, reduced response camptothecin polymeric prodrug amphipathic molecules of the reduced response camptothecin prodrug monomer, and a preparation method and application of the reduced response camptothecin prodrug monomer and the reduced response camptothecin polymeric prodrug amphipathic molecules. In the formula I, each i is 2 or 3 independently, each X is O or NH independently, and R is H, CH3 or CH2CH3. According to the preparation method, raw materials including camptothecin, triphosgene and the like are used for modifying 20 bits of hydroxyls of camptothecin to prepare a camptothecin prodrug monomer containing disulfide bonds, then the camptothecin prodrug monomer is subjected to high-conversion-rate polymerization by using active free radical polymerization method to obtain an amphiphilic polymer which contains a camptothecin drug repetitive unit and has an extremely high drug loading capacity (more than 50wt%), and in a tumor cell reducing environment, a side chain disulfide bond is broken to perform molecular rearrangement and release camptothecin prodrug molecules, so that the amphiphilic polymer has characteristics of a reduced response controlled-release raw drug. The polymeric prodrug amphipathic molecules improve the water solubility and stability of the drug and have a controlled release characteristic.

Heterobifunctional polymeric prodrug platforms for delivering biologically active compounds, including proteins, monoclonal antibodies and the like are disclosed. One preferred compound is Methods of making and using the compounds and conjugates described herein are also provided.

The present invention relates to multi-branched polymeric prodrugs and applications thereof. Specifically, the present invention relates to a multi-branched polymeric prodrug having a structure of formula (I) or a pharmaceutically acceptable salt thereof, which is effective for topoisomerase I-related diseases in mammalian subjects, In particular, solid tumors in mammalian subjects have very good therapeutic effects. In the case of the same in vitro activity as inhibiting the proliferation of cancer cells, it has a more reasonable half-life and residence time of the drug in the body, greatly reduces the clearance rate, is more conducive to determining the way of drug administration, and reduces the number of administrations. It is expected to be developed into a new drug. A generation of antineoplastic drugs.

The invention provides a redox-responsive hyperbranched polyprodrug nano-micelle and its preparation method and application. In the invention, the hydrophobic drug is connected with the disulfide bond that can be cut by high GSH, and then the redox-responsive amphiphilic hyperbranched polyprodrug nano-micelle is synthesized through two-step RAFT polymerization. The redox-responsive hyperbranched polyprodrug nano-micelle of the present invention has the advantages of simple preparation process, good stability, prolonged blood circulation time, improved bioavailability of drugs, and the like. Moreover, the nano-micelle can break under the reducing environment of high GSH concentration in tumor cells, release hydrophobic drugs rapidly, and inhibit the proliferation of tumor cells. The redox-responsive hyperbranched polyprodrug nanomicelles of the present invention provide a new option for tumor therapy.

The invention relates to the fields of chemical synthesis and biological representation, and more particularly, provides a preparation method and an application of a pH-responsive amphiphilic rod-likepolymer prodrug, which is represented as the drawing in the specification. The preparation method of the amphiphilic rod-like polymer material includes the following steps: 1) synthesizing a rod-likeATRP initiator on the basis of glucan; 2) introducing a pH-responsive hydrophobic block on the basis of ATRP reaction; 3) introducing a hydrophilic block on the basis of ATRP reaction to obtain an amphiphilic polymer material; 4) substituting an ester group on the terminal of MGMA by means of hydrazine hydrate, thus producing a pH-responsive precursor; 5) forming a hydrazone bond by means of a carbonyl group on adriamycin and an amino group on the polymer material, thus producing the pH-responsive polymer prodrug. By means of weak acidity of interior of cancer cells, the amphiphilic rod-likepolymer prodrug can selectively release a drug by means of pH-stimulating response. The polymer prodrug is high in micelle stability, is high in drug carrying capacity and enables drug release to be under stimulating response control.

The invention relates to a preparation method for different nano particles of reducing response camptothecin polymeric prodrug amphipathic molecules represented in a formula I as well as a product and an application of the nano particles, wherein morphology of a polymeric prodrug amphipathic molecule final assembly can be controlled just by regulating the kind of a solvent and through a way of adding water and regulating a water adding speed, so as to obtain four typical nano structures: spherical structure, disc-shaped structure, flower-shaped compound vesicle and staggered accumulated lamellar nano particles. The nano structures have high drug loading rate (more than 50wt%); compared with the most studied spherical nano particle at present, an assembly of the staggered accumulated lamellar structure is the longest in blood circulation time, followed by the disc-shaped nano particles. In addition, non-spherical particle is greater in tumor cytotoxicity compared with the spherical nano particles. In the formula I, various is independently represent 2 or 3; various Xes independently represent O or NH; R is H, CH3 or CH2CH3; m ranges from 4 to 400; and n ranges from 2 to 300; and number-average molecular weight of the reducing response camptothecin polymeric prodrug amphipathic molecule is 1200-220000.

The present invention relates to methods of inhibiting angiogenesis in mammals. The present invention includes administering polymeric prodrugs of 07-ethyl-10-hydroxycamptothecin to the mammals in need thereof. The present invention also relates to methods of treating a disease associated with angiogenesis in mammals by administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to the mammals in need thereof.