Patent RU-2737893-C2 (RU)
Title: Pegylated lipid nanoparticle with a bioactive lipophilic compound
Inventor: GAILLARD PIETER JAAP
IPC: A61K47/06
Filed: 2016-08-11
Granted: 2020-12-04
Abstract: FIELD: medicine; pharmaceuticals. 
     SUBSTANCE: present invention relates to a nanoparticle, a composition, a preparation of eye drops and an applicator. Nanoparticle contains: a) two or more neutral phospholipids selected from a group consisting of 1,2-dilauryl-sn-glycero-3-phosphate (DLPA), 1,2-dilauryl-sn-glycero-3-phosphoethanolamine (DLPE), 1,2-dimyristoyl-sn-glycero-3-phosphate (DMPA), 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), 1,2-dimyristoyl-sn-glycero-3-phosphoethanolamine (DMPE), 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG), 1,2-dimyristoyl-sn-glycero-3-phosphoserine (DMPS), 1,2-dipalmitoyl-sn-glycero-3-phosphate (DPPA), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) , 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE), 1,2-dipalmitoyl-sn-glycero-3-phosphoglycerol (DPPG), 1,2-dipalmitoyl-sn-glycero-3-phosphoserine (DPPS), 1,2-distearoyl-sn-glycero-3-phosphate (DSPA) , 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE), 1,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG), 1,2-distearoyl-sn-glycero-3-phosphoserine (DSPS) and hydrogenated soybean phosphatidyl choline (HSPC); and b) at least one of acyl ethanolamide and macrolide. Size of the nanoparticles is not more than 125 nm. Surface of the nanoparticles contains a water-soluble polymer. Water-soluble polymer is conjugated with one of two or more phospholipids. Water-soluble polymer is at least one of the following substances: i) polyalkyl ether, preferably polyalkyl ether, which is linear polyethylene glycol (PEG), star PEG or branched PEG with multiple branches; ii) a homopolymer which is a substitute for PEG or an alternative to PEG, preferably such a homopolymer is selected from a group consisting of polymethylethylene glycol (PMEG), polyhydroxypropylene glycol (PHPG), polypropylene glycol (PPG), polymethyl propylene glycol (PMPG), polyhydroxypropylene oxide (PHPO), poly-oxazoline (POZ) and hydroxyethyl starch (HES); and iii) heteropolymer from small alkoxy-monomers, preferably containing polyethylene glycol/polypropylene glycol (PEG/PPG). Composition is used for ophthalmic treatment or for skin treatment. Said composition contains a therapeutically or prophylactically effective amount of nanoparticles and an excipient or carrier, which are suitable for use in humans or for veterinary use. Nanoparticle is used in ophthalmic treatment or for skin treatment. Eye drops preparation contains a therapeutically or prophylactically effective amount of nanoparticles or contains a composition. Applicator for applying an effective amount of a preparation of eye drops in an eye containing a preparation of eye drops. Preparation of compositions for treating or ameliorating a disease or disorder of skin, mucosa or eyes, which do not cause (severe) side effects at the point of administration. 
     EFFECT: technical result is obtaining improved (stable, inert, transparent and solvent-free) lipophilic substances (such as immunomodulating macrolides) for systemic or local administration of effective concentration of such substances. 
     12 cl, 3 tbl, 6 ex, 2 dwg