Polymeric micelle particle comprising anionic drugs and method of preparing the same
AssigneeSamyang Biopharmaceuticals Corporation
InventorsSe-Ho Kim, Ji-Yeon Son, Muhn-Ho La, Sung-Won Choi, Min-Hyo Seo
Life of this patent
Estimating the term…
Abstract
Disclosed are an anionic drug-containing polymeric micelle particle comprising: an anionic drug as an active ingredient; a cationic lipid; and an amphiphilic block copolymer, wherein the anionic drug forms a complex with the cationic lipid, and the complex is entrapped in the micelle structure of the amphiphilic block copolymer, and a method for preparing the same. The particle may increase stability of the anionic drug in blood or in a body fluid, and it may enable intracellular delivery to improve efficacy of anionic drugs.
Claims16
A polymeric micelle particle, comprising:
- an anionic drug as an active ingredient;
- a lipid comprising a cationic lipid;
- and
- an amphiphilic block copolymer,
- wherein the anionic drug forms a complex with the cationic lipid by electrostatic interactions, and the complex of the anionic drug and the cationic lipid is entrapped in the core-shell type polymeric micelle structure of the amphiphilic block copolymer which is an A-B type di-block copolymer comprising a hydrophilic A block forming the shell and a hydrophobic B block forming the core,
- wherein the hydrophilic A block is one or more selected from the group consisting of polyalkyleneglycol, polyvinyl alcohol, polyvinyl pyrrolidone, polyacrylamide, and a derivative thereof, and the hydrophobic B block is one or more selected from the group consisting of polyester, polyanhydride, polyamino acid, polyorthoester, and polyphosphazine, and
- wherein the particle is free from a polyethyleneglycol (PEG)-lipid conjugate, and a polyamide (ATTA)-lipid conjugate,
- wherein the hydrophobic B block has a number average molecular weight of 1,000 to 50,000 Dalton,
- wherein a weight ratio of (a) the complex of the anionic drug and the cationic lipid to (b) the amphiphilic block copolymer ((a)/(b)×100) is 0.01 to 50 wt %.
Dependencies are inferred from the claim text.