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1. WO2021046078 - COMB POLYMER AND BLOCK COPOLYMER STABILIZED NANOPARTICLES ENCAPSULATING NUCLEIC ACIDS AND OTHER SOLUBLE HYDROPHILIC COMPOUNDS

Publication Number WO/2021/046078
Publication Date 11.03.2021
International Application No. PCT/US2020/048986
International Filing Date 02.09.2020
IPC
A61K 9/51 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules
51Nanocapsules
CPC
A61K 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 47/34
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 48/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
A61K 9/5031
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules ; having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
5005Wall or coating material
5021Organic macromolecular compounds
5031obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
A61K 9/5138
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules ; having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
51Nanocapsules; Nanoparticles;
5107Excipients; Inactive ingredients
513Organic macromolecular compounds; Dendrimers
5138obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
A61K 9/5146
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules ; having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
51Nanocapsules; Nanoparticles;
5107Excipients; Inactive ingredients
513Organic macromolecular compounds; Dendrimers
5146obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
Applicants
  • THE TRUSTEES OF PRINCETON UNIVERSITY [US]/[US]
Inventors
  • PAGELS, Robert, F.
  • MARKWALTER, Chester, E.
  • PRUD'HOMME, Robert, K.
Agents
  • PATTILLO, Alan, C.
Priority Data
62/895,69504.09.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMB POLYMER AND BLOCK COPOLYMER STABILIZED NANOPARTICLES ENCAPSULATING NUCLEIC ACIDS AND OTHER SOLUBLE HYDROPHILIC COMPOUNDS
(FR) NANOPARTICULES STABILISÉES PAR UN COPOLYMÈRE SÉQUENCÉ ET UN POLYMÈRE EN PEIGNE ENCAPSULANT DES ACIDES NUCLÉIQUES ET D'AUTRES COMPOSÉS HYDROPHILES SOLUBLES
Abstract
(EN)
A precipitation route to form nanoparticles with a hydrophilic core containing water soluble materials and a hydrophobic shell is described. The process requires a stabilizing polymer composed of more polar and more non-polar regions. These regions can be arranged as a linear block copolymer, or as a comb polymer with a linear or branched polar backbone and non-polar side chains or substituents. Nucleic acids, including DNA and RNA, as well as proteins, peptides, and polysaccharides or combinations can be encapsulated in the nanoparticle core. The encapsulation of nucleic acids can require partially or fully neutralizing the acid with a base to enhance the solubility of the nucleic acid in the process solvent stream. The core or the shell of the resulting nanoparticles can be crosslinked. The nanoparticles may be coated with additional polymer to bring them into water, or processed into microparticles or larger monoliths.
(FR)
L'invention concerne une voie de précipitation pour former des nanoparticules comportant un cœur hydrophile contenant des matériaux hydrosolubles et une écorce hydrophobe. Le procédé nécessite un polymère stabilisant constitué de régions plus polaires et de régions plus apolaires. Ces régions peuvent être agencées en tant que copolymère séquencé linéaire, ou en tant que polymère en peigne comportant un squelette polaire linéaire ou ramifié et des substituants ou des chaînes latérales apolaires. Des acides nucléiques, notamment de l'ADN et de l'ARN, ainsi que des protéines, des peptides et des polysaccharides ou des combinaisons de ceux-ci peuvent être encapsulés dans le cœur de la nanoparticule. L'encapsulation d'acides nucléiques peut nécessiter une neutralisation partielle ou complète de l'acide avec une base pour améliorer la solubilité de l'acide nucléique dans le flux de solvant de traitement. Le cœur ou l'écorce des nanoparticules ainsi obtenues peuvent être réticulés. Les nanoparticules peuvent être enrobées d'un polymère supplémentaire pour les mettre dans l'eau, ou traitées en microparticules ou en monolithes plus grands.
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