Top > Search of International Patents > CROSSLINKED HYDROPHOBIZED-POLYSACCHARIDE NANOGEL PARTICLES AND MANUFACTURING METHOD THEREFOR

CROSSLINKED HYDROPHOBIZED-POLYSACCHARIDE NANOGEL PARTICLES AND MANUFACTURING METHOD THEREFOR

Foreign code F150008222
Posted date Mar 26, 2015
Country WIPO
International application number 2014JP059082
International publication number WO 2014157606
Date of international filing Mar 28, 2014
Date of international publication Oct 2, 2014
Priority data
  • P2013-072258 (Mar 29, 2013) JP
Title CROSSLINKED HYDROPHOBIZED-POLYSACCHARIDE NANOGEL PARTICLES AND MANUFACTURING METHOD THEREFOR
Abstract The principal problem addressed by the present invention is the provision of appropriately sized crosslinked hydrophobized-polysaccharide gel particles. To solve said problem, crosslinked hydrophobized-polysaccharide gel particles having particle diameters from 1 to 100 µm are provided.
Outline of related art and contending technology BACKGROUND ART
Due to the development of biotechnology, in a cell or a peptide involved in a signaling system, within the cells of the biologically important proteins and plays a role in the cell the nucleic acid delivery to the attempt has been actively performed. These are conventional small molecule compounds from the pharmacological effect cannot be implemented by the pharmaceutical agents can be increased, many outcome is increasing. As a typical insulin and human growth hormone, monoclonal antibodies, various cytokines and the like, in recent years is a complex higher-order structure having a protein or nucleic acid can be isolated and purified relatively easy also for the reason that, of bio-pharmaceuticals is, in a medical field increasingly popular, thought to be important. However, these bio-pharmaceuticals is, generally reduces the stability, decomposition or inactivation in the body to be amenable to from, of very short half-life of the agent as is known. This short half-life, when using the actual maximum efficient in clinical situations in which a problem occurs. At present, many proteins such as cytokines or antibody medicament is, from several days to several weeks to several months or more for each period of administration, must be continuously administered. In many cases, such as infusion treatment methods are performed by injection, patient's quality of life (quality of life, QOL) cannot be said to be high, the distal end of the next generation of bio-pharmaceuticals in medicine is using, by a suitable carrier, in an appropriate location, the desired concentration and time pattern development of regenerative medicine and drug delivery system can deliver been desired earnestly.
On the other hand, in recent years, the field of material science and nanotechnology has generated a new materials than is applied to regenerative medicine and drug delivery attempt has been actively performed. The inventors of the present invention in the case of the polysaccharide mainly constituted by a physically cross-linked nano-gel, have great promise as a carrier protein can be enclosed medicament revealed have shown. By previous studies, nano gel molecular chaperones, cancer immunotherapy clinical levels, intracellular introduction, nasal type such as a vaccine to be used as an important material in the currently known.
Existing work by the inventors of the present invention (patent document 1, non-patent document 1, 2) in, in order to increase the application range of the nano-gel, nano-gel a gel cross-linking points in the preparation of (nano-gel cross-linked gel) attempted. Specifically, the conventional cholesteryl group-introduced pullulan modified with acryloyl groups, the polymerizable nanoparticles having gel was prepared. This polymerizable nano gel, polyethylene glycol is attached to a thiol group at an end by reacting, nano gel crosslinked to form a gel. The nano gel cross-linked gel, encapsulating a protein internal nano gel and has a sustained release is characterized, in particular of regenerative medicine as scaffolding material for many results (non-patent document 2) are enhanced.
Non-patent document 3-7 obtained by the prior art such as nano-gel cross-linked gel, particles or smaller than the particle size of about 100 nm, greater than or equal to the number of large particles either mm, with the size of a micrometer range from a sub-micron nano-gel cross-linked gel that has not been obtained. In the order of magnitude of about 100 nm in a particle of the containment vessel or limited by the claims, is not able to adjust the rate of sustained release, of a size larger than the number of mm nano gel cross-linked gel surgical methods of administration to a body to the surface of the embedded or limited by the joining means. The crosslinking agent without using the nano-gel nano-gel to each other by cross-linking a cross-linked gel was not able to be prepared.
Scope of claims (In Japanese)請求の範囲 [請求項1]
粒子径が1~100マイクロメートルである、架橋された疎水化多糖ナノゲル粒子。

[請求項2]
架橋された疎水化多糖ナノゲル粒子が、架橋性基を有する疎水化多糖ナノゲルと架橋剤を反応させて得られたもの、または架橋性基を有する疎水化多糖ナノゲル同士を反応させて得られたものである、請求項1に記載の疎水化多糖ナノゲル粒子。

[請求項3]
架橋性基を有する疎水化多糖ナノゲルが、多糖部分、疎水性部分及び架橋性部分を含む、請求項2に記載の疎水化多糖ナノゲル粒子。

[請求項4]
多糖部分が、プルラン、アミロペクチン、アミロース、デキストラン、ヒドロキシエチルデキストラン、マンナン、レバン、イヌリン、キチン、キトサン、キシログルカンまたは水溶性セルロースである、請求項3に記載の疎水化多糖ナノゲル粒子。

[請求項5]
疎水性部分が炭素数8~50の炭化水素基またはステリル基を含む、請求項3に記載の疎水化多糖ナノゲル粒子。

[請求項6]
疎水性部分がコレステリル基を含む、請求項5に記載の疎水化多糖ナノゲル粒子。

[請求項7]
架橋性部分がアクリロイル、メタアクリロイル、ビニル及びアリルから選択される少なくとも1種の架橋性基を含む、請求項3に記載の疎水化多糖ナノゲル粒子。

[請求項8]
架橋剤がメルカプトエチルポリエチレングリコール化合物である、請求項2に記載の疎水化多糖ナノゲル粒子。

[請求項9]
架橋剤がチオール基含有アミノ酸又はチオール基含有アミノ酸残基を含むペプチドとポリエチレングリコール化合物との縮合物である、請求項2に記載の疎水化多糖ナノゲル粒子。

[請求項10]
核酸、薬物及びタンパク質から選択される少なくとも1種を担持する、請求項1~9のいずれか1項に記載の疎水化多糖ナノゲル。

[請求項11]
(1)(i)架橋性基を有する疎水化多糖ナノゲル、架橋剤及び界面活性剤、又は、
(ii)架橋性基を有する疎水化多糖ナノゲル及び界面活性剤を、水及び油相成分を含む溶媒中で混合してW/0型エマルションを調製する工程、並びに、
(2)得られたW/0型エマルションの架橋反応を行い粒子径が1~100マイクロメートルである架橋された疎水化多糖ナノゲル粒子を得る工程を含む、架橋された疎水化多糖ナノゲル粒子の製造方法。

[請求項12]
工程(1)において、さらに核酸、薬物及びタンパク質から選択される少なくとも1種を添加することを特徴とする、請求項11に記載の製造方法。

  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • KYOTO UNIVERSITY
  • Inventor
  • AKIYOSHI, Kazunari
  • TAHARA, Yoshiro
  • MUKAI, Sadaatsu
  • SAWADA, Shinichi
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LT LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN TD TG
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