3 results about "Polymeric prodrug" patented technology

This invention provides a platinum-based polymeric prodrug with liver-slowing function and its preparation method. The platinum-based polymeric prodrug comprises a copolymer of first, second, and third monomers; the first monomer contains a platinum precursor, a linker group, and an acrylic acid group, and has a carbamate bond; the second monomer is selected from zwitterionic monomers; the third monomer is selected from small acrylic acid molecules, enabling the copolymer to self-assemble into nanoparticles with a core, linker arms, and a shell in an aqueous solvent. This invention utilizes the anti-plasma protein adsorption properties of zwitterionic groups to reduce their non-specific accumulation in the liver; the carbamate bond allows for slow drug release within the liver. Therefore, it fundamentally reduces oxidative stress and DNA damage in the liver, maintaining the therapeutic effect of tumor treatment while inhibiting chemotherapy-induced hepatocyte senescence, reducing tumor metastasis and colonization promoted by the aging microenvironment, and possessing the advantages of high drug loading capacity, stability, and intelligent responsive release.

This invention discloses a omegacycline tosylate nanocrystal lyophilized formulation and its preparation method, relating to the field of pharmaceutical synthesis technology. The formulation comprises, by weight, the following components: 12-20 parts of omegacycline polymeric prodrug, 80-120 parts of a lyophilization protectant, 2-8 parts of a stabilizer, and 150-300 parts of a solvent. The omegacycline polymeric prodrug is formed by covalently linking omegacycline molecules to the terminal hydroxyl groups of a hyperbranched aliphatic polyester synthesized using 2,2-dimethylolpropionic acid as a monomer and pentaerythritol as a core. This omegacycline tosylate nanocrystal lyophilized formulation not only exhibits high stability but also provides advantages in high drug loading and precise drug release.

The present invention relates to a mucoadhesive polymeric prodrug comprising a partially succinated polyvinyl alcohol (PVA-SA) with adjusted amount of hydroxyl and carboxyl pendant groups, which form an ester and / or amide linkage with amino and / or carboxyl and / or hydroxyl groups of biologically active compounds such as proteins, peptides, synthetic chemical, or natural products compounds (e.g. doxorubicin as an antitumor agent and antifibrotic drug). Preferably, said biologically active compounds are cysteamine (CYS) as the aminothiol compound and one compound selected from the group consisting of doxorubicin (DOX), ketoprofen (KETO), or 4-hydroxybenzyl alcohol (HBA). Moreover, the simultaneous presence of both hydroxyl and carboxyl groups in the partially succinated polyvinyl alcohol (PVA-SA) chain of the prodrug enables the self-assembled formation of 50-260 nm particles from the linear macromolecules and thus the drug release can be prolonged or adjusted. The present invention also relates to improving the mucoadhesive properties of the polymeric prodrug by the regulation of the amount of conjugated aminothiol compound. Further, the present invention relates to the method for producing said mucoadhesive polymeric prodrug, and nanoparticles of the said mucoadhesive polymeric prodrug.