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1. WO2011038278 - MICELLE ENCAPSULATION OF THERAPEUTIC AGENTS

Publication Number WO/2011/038278
Publication Date 31.03.2011
International Application No. PCT/US2010/050276
International Filing Date 24.09.2010
IPC
A61K 9/107 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions
A61K 47/34 2006.01
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 9/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
A61K 31/337 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
337having four-membered rings, e.g. taxol
A61K 31/395 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/436 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
436the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
CPC
A61K 31/337
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
337having four-membered rings, e.g. taxol
A61K 31/395
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/436
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
436the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/439
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
439the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/7048
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7048having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin ; digitoxin or digoxin
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants
  • WISCONSIN ALUMNI RESEARCH FOUNDATION [US]/[US] (AllExceptUS)
  • KWON, Glen S. [US]/[US] (UsOnly)
Inventors
  • KWON, Glen S.
Agents
  • HAUKAAS, Michael
Priority Data
61/245,91825.09.2009US
61/375,68120.08.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MICELLE ENCAPSULATION OF THERAPEUTIC AGENTS
(FR) ENCAPSULATION D'AGENTS THÉRAPEUTIQUES DANS DES MICELLES
Abstract
(EN)
The invention provides active agents, such as paclitaxel, rapamycin, or 17-AAG, encapsulated by safe poly(ethylene glycol)-block-poly(lactic acid) ("PEG-b-PLA") micelles. The compositions provide effective solubilization of drug combinations, such as paclitaxel, rapamycin, and 17-AAG, as well as others described herein. A significant advantage of PEG-b-PLA as a carrier is that it is less toxic than Cremophor® EL or DMSO, which are used in currently known compositions. Additionally, PEG-b-PLA micelles are easier to handle than DMSO and they do not possess a foul odor, which is a problem with formulations currently in clinical trials. Accordingly, the invention provides stable and biocompatible drug formulations that improve bioavailabilty without causing toxicity. It was also found that larger doses of individual drugs in micelle formulations can be administered compared to non-micelle formulations.
(FR)
Cette invention concerne des principes actifs, tels que le paclitaxel, la rapamycine, ou 17-AAG, encapsulés dans des micelles sans danger de poly(éthylène glycol)-bloc-acide poly(lactique) ( » PEG-b-PLA »). Les compositions permettent la solubilisation efficace d'associations de médicaments, telles que paclitaxel, rapamycine, et 17-AAG, et autres médicaments décrits dans la présente. Un avantage significatif du PEG-b-PLA à titre de support est qu'il est moins toxique que le Crémophor® EL ou le DMSO, qui sont utilisés dans les compositions couramment connues. De plus, les micelles de PEG-b-PLA sont plus faciles à manipuler que le DMSO et elles ne dégagent pas une odeur nauséabonde, ce qui est un problème avec les formulations actuellement utilisées dans les essais cliniques. Par conséquent, l'invention concerne des formulations de médicaments stables et biocompatibles qui améliorent la biodisponibilité sans induire de toxicité. Il s'est également avéré que, dans des formulations micellaires, de plus grandes doses de médicaments individuels peuvent être administrées comparativement à des formulations non micellaires.
Also published as
Latest bibliographic data on file with the International Bureau