AR100762A1 - Sistema de liberación micelar a base del híbrido de peg-dendrón anfifílico que responde a enzimas - Google Patents
Sistema de liberación micelar a base del híbrido de peg-dendrón anfifílico que responde a enzimasInfo
- Publication number
- AR100762A1 AR100762A1 ARP150100556A ARP150100556A AR100762A1 AR 100762 A1 AR100762 A1 AR 100762A1 AR P150100556 A ARP150100556 A AR P150100556A AR P150100556 A ARP150100556 A AR P150100556A AR 100762 A1 AR100762 A1 AR 100762A1
- Authority
- AR
- Argentina
- Prior art keywords
- agent
- group
- dendron
- hybrid
- release system
- Prior art date
Links
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- 230000002209 hydrophobic effect Effects 0.000 abstract 6
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- 229960002817 metolazone Drugs 0.000 abstract 1
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- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 abstract 1
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- DFEYYRMXOJXZRJ-UHFFFAOYSA-N sevoflurane Chemical compound FCOC(C(F)(F)F)C(F)(F)F DFEYYRMXOJXZRJ-UHFFFAOYSA-N 0.000 abstract 1
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- 229960002930 sirolimus Drugs 0.000 abstract 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 abstract 1
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- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 abstract 1
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- 239000011721 thiamine Substances 0.000 abstract 1
- WZDGZWOAQTVYBX-XOINTXKNSA-N tibolone Chemical compound C([C@@H]12)C[C@]3(C)[C@@](C#C)(O)CC[C@H]3[C@@H]1[C@H](C)CC1=C2CCC(=O)C1 WZDGZWOAQTVYBX-XOINTXKNSA-N 0.000 abstract 1
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- NCYCYZXNIZJOKI-UHFFFAOYSA-N vitamin A aldehyde Natural products O=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-UHFFFAOYSA-N 0.000 abstract 1
- MECHNRXZTMCUDQ-RKHKHRCZSA-N vitamin D2 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)/C=C/[C@H](C)C(C)C)=C\C=C1\C[C@@H](O)CCC1=C MECHNRXZTMCUDQ-RKHKHRCZSA-N 0.000 abstract 1
- 235000001892 vitamin D2 Nutrition 0.000 abstract 1
- 239000011653 vitamin D2 Substances 0.000 abstract 1
- 229960000820 zopiclone Drugs 0.000 abstract 1
Classifications
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6905—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
- A61K47/6907—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a microemulsion, nanoemulsion or micelle
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- A—HUMAN NECESSITIES
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- Bioinformatics & Cheminformatics (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicación 1: Un sistema de liberación híbrido anfifílico en forma micelar, que comprende un polímero de polietilenglicol hidrofílico (PEG) conjugado con un dendrón hidrofóbico, donde el dendrón comprende al menos un grupo terminal hidrofóbico enzimáticamente escindible que se une covalentemente con el dendrón, en donde la micela se desensambla después del clivaje enzimático del grupo terminal hidrofóbico. Reivindicación 34: El sistema de liberación hibrido de acuerdo con la reivindicación 32 ó 33, en donde el grupo terminal hidrofóbico que se une con el dendrón y/o el compuesto que está encapsulado por dicha micela están cada uno seleccionados, de modo independiente, del grupo que consiste en un agente antiproliferativo, un agente antiinflamatorio no esteroide, un agente antibiótico, un agente antimicrobiano, un agente antiviral, un agente inmunosupresor, un agente inmunomodulador, un agente antihipertensivo, un agente quimiosensibilizante, un agente antihistamínico, un agente anestésico general, un agente anestésico local, un agente analgésico, un agente antifúngico, una vitamina, una vitamina soluble en grasas, un agente hipnótico, un agente sedante, un agente ansiolítico, un agente antidepresivo, un agente anticonvulsivante, un agente analgésico narcótico, un agente antagonista narcótico, un agente anticolinesterasa, un agente simpatomimético, un agente parasimpatomimético, un agente estimulante gangliónico, un agente bloqueante gangliónico, un agente antimuscarínico, un agente bloqueante adrenérgico, un autacoide y antagonista de autacoide, digitalis y congéneres de digitalis, agentes diuréticos y saliuréticos, un agente reductor del colesterol, un agente antineoplásico, hemoglobina y derivados de hemoglobina y polímero, un agente hormonal, un agente antagonista hormonal y combinación de ellos. Reivindicación 35: El sistema de liberación híbrido de acuerdo con la reivindicación 34, en donde el grupo terminal hidrofóbico que se une con el dendrón y/o el compuesto que está encapsulado por dicha micela están cada uno seleccionados, de modo independiente, del grupo que consiste en cumarina, salicilato de metilo, aspirina, ibuprofeno, naproxeno, famciclovir, valaciclovir, aciclovir, penicilina-V, azlocilina, tetraciclina, daunorrubicina, doxorrubicina, antraciclina, mitomicina C, aminopertina, micofenolato mofetilo, azatioprina, sirolimus, glucocorticoide, metotrexato, azatioprina, ciclosporina, tacrolimus, talidomida, lenalidomida, pomalidomida, clorotiazida, metolazona, amiloride, acrivastina, bilastina, buclizina, cimetidina, clobenpropit, desflurano, isoflurano, sevoflurano, propofol, metohexital, benzocaina, dibucaina, lidocaína, proparacaína, paracetamol, morfina, oxicodona, celecoxib, flupirtina, anfotericina B, candicidina, bifonazol, butoconazol, fluconazol, abafungina, anidulafungina, retinol, tiamina, riboflavina, biotina, ergocalciferol, retinal, retinol, amobarbital, alprazolam, zopiclona, midazolam, amobarbital, alprazolam, sertralina, clobazam, codeina, naltrexona, fisostigmina, efedrina, dimetilfenilpiperazinio, pentamina, atropina, terazosina, histamina, hidroclorotiazida, estatina, tibolona, acetato de ganirelix, septrina y sus derivados. Reivindicación 36: El sistema de liberación hibrido de acuerdo con cualquiera de las reivindicaciones precedentes, está representado por la estructura de la fórmula (1), en donde R es H o un grupo alquileno C₁₋₄; T está ausente o es un grupo funcional seleccionado del grupo que consiste en -O-, -S-, -NH-, -C(=O)-, -O-C(=O)-O-, -C(=O)-O-, -C(=O)-NH-, -NH-C(=O)-NH-, NH-C(=O)-O-, -S(=O)-, -S(=O)-O-, PO(=O)-O-, -C=C-, -CºC-, -(CH₂)ₜ,- en donde t es un número entero de 1 - 10 y cualquiera de sus combinaciones; Y está ausente, de modo independiente en cada aparición, o es un resto de ligador / unidad de ramificación; Z es, de modo independiente en cada aparición, una unidad de repetición de dendrones seleccionada del grupo que consiste en: un resto seleccionado del grupo de fórmulas (2) y cualquier combinación de lo anterior; en donde X¹ está seleccionad, de modo independiente en cada aparición, del grupo que consiste en a O, S y NH; A es un grupo terminal hidrofóbico que se conjuga con el dendrón a través de un grupo funcional enzimáticamente escindible seleccionado del grupo que consiste en un éster, una amida, un carbamato, un carbonato, una urea, un sulfato, una amidina, un éter, un fosfato, una fosfoamida, sulfamatos, y un tritionato; n es un número entero en el rango de 1 a 1500, con preferencia, de 1 a 1000; y m y z son cada uno un número entero de 1 a 15.
Applications Claiming Priority (1)
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| WO (1) | WO2016038595A1 (es) |
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| EP3190880A4 (en) * | 2014-09-09 | 2018-04-18 | Ramot at Tel-Aviv University Ltd. | AGROCHEMICAL DELIVERY SYSTEM BASED ON ENZYME- OR pH- RESPONSIVE AMPHIPHILIC PEG-DENDRON HYBRIDS |
| US10869939B2 (en) | 2015-08-03 | 2020-12-22 | Ramot At Tel-Aviv University Ltd. | Delivery system in micellar form having modular spectral response based on enzyme-responsive amphiphilic PEG-dendron hybrid polymers |
| CN109593158B (zh) * | 2017-09-30 | 2021-02-26 | 浙江大学 | 一种γ-谷氨酰转肽酶催化水解致电荷翻转的聚合物及其在药物输送领域的应用 |
| CN109998993A (zh) * | 2019-04-22 | 2019-07-12 | 西南交通大学 | 用于治疗心血管类疾病的载药聚合物胶束及其制备方法和应用 |
| CN111297876B (zh) * | 2020-01-16 | 2021-04-27 | 武汉理工大学 | 一种塞来昔布胶束和和厚朴酚胶束药物联用控释系统及其制备方法 |
| CA3222840A1 (en) * | 2021-06-16 | 2022-12-22 | Geoffrey M. Lynn | Self-assembling nanoparticles based on amphiphilic peptides for drug delivery applications |
| WO2024052920A1 (en) * | 2022-09-08 | 2024-03-14 | Ramot At Tel-Aviv University Ltd. | Programmable stimuli-responsive polymeric formulations |
| CN115960346B (zh) * | 2023-01-04 | 2025-05-27 | 中国药科大学 | 一种以视黄醇衍生物为疏水链的两亲性聚合物 |
| CN116650401B (zh) * | 2023-04-20 | 2024-11-08 | 西南医科大学 | 一种双效聚合物胶束复合水凝胶及其制备方法与应用 |
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| US20080294089A1 (en) * | 2007-06-06 | 2008-11-27 | Biovaluation & Analysis, Inc. | Dendritic Polymers for Use in Acoustically Mediated Intracellular Drug Delivery in vivo |
| WO2011001657A1 (ja) * | 2009-07-01 | 2011-01-06 | 独立行政法人科学技術振興機構 | ポリイオンデンドリマー、及びそれよりなるハイドロゲル |
| US9457099B2 (en) * | 2010-11-12 | 2016-10-04 | Rutgers, The State University Of New Jersey | Polyethylene glycol-based dendrons |
| WO2012116073A2 (en) * | 2011-02-23 | 2012-08-30 | The Board Of Trustees Of The University Of Illinois | Amphiphilic dendron-coils, micelles thereof and uses |
| US9283279B2 (en) * | 2011-05-11 | 2016-03-15 | Ramot At Tel-Aviv University Ltd. | Targeted polymeric conjugates and uses thereof |
-
2015
- 2015-02-25 CN CN201580048552.2A patent/CN106687142A/zh active Pending
- 2015-02-25 EP EP15840235.4A patent/EP3191137A4/en not_active Withdrawn
- 2015-02-25 AR ARP150100556A patent/AR100762A1/es unknown
- 2015-02-25 US US15/509,962 patent/US20170348430A1/en not_active Abandoned
- 2015-02-25 WO PCT/IL2015/050212 patent/WO2016038595A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016038595A1 (en) | 2016-03-17 |
| CN106687142A (zh) | 2017-05-17 |
| EP3191137A4 (en) | 2018-04-25 |
| EP3191137A1 (en) | 2017-07-19 |
| US20170348430A1 (en) | 2017-12-07 |
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