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Uncaria-containing brain-targeting nano preparation and preparation method thereof

A nano-preparation, a technology containing urticine, applied in the directions of nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of improving the bioavailability of uricine, lack of slow-release and controlled-release effects, etc., and achieve good encapsulation performance. , high encapsulation rate, overcoming the effect of low solubility

Active Publication Date: 2022-03-22
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the preparation method of the above-mentioned preparation has mild conditions and effectively solves the problem of converting rhynchophylline into isorhynchophylline, it lacks slow-release and controlled-release effects, and it is difficult to improve the bioavailability of rhynchophylline on the basis of maintaining the activity of rhynchophylline. Spend

Method used

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  • Uncaria-containing brain-targeting nano preparation and preparation method thereof
  • Uncaria-containing brain-targeting nano preparation and preparation method thereof
  • Uncaria-containing brain-targeting nano preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The synthetic route of the nuclear material 60%-γ-PFGA is as follows:

[0046]

[0047] Proceed as follows:

[0048] In step (1), 4-methyl-5-hydroxyethylthiazole (35.19mmol) and methyl iodide (106.02mmol) were reacted in an autoclave at 60°C for 3h, the reactant was transferred to a round-bottom flask with an appropriate amount of methanol, and evaporated under reduced pressure. Dry solvent, wash with appropriate amount of ether to obtain tan 3,4-dimethyl-5-(2-hydroxyethyl)iodothiazole;

[0049] In step (2), 1-bromopropane (49.83mmol) was dissolved in 30mL of ethanol containing 0.2mL of PEG400, and 10mL of 5H containing 0.2mL of PEG400 was added dropwise 2 O·Na 2 S 2 O 3 (45.21 mmol) aqueous solution, refluxed at 69 °C for 7 h, evaporated to dryness under reduced pressure, and vacuum dried to obtain white crystalline powder propyl pente salt;

[0050] Step (3), take 3,4-dimethyl-5-(2-hydroxyethyl) iodothiazole (21.1 mmol) and dissolve it in 16 mL of water, add N...

Embodiment 2

[0060] Synthesis of shell material PLA-SS-PEG-A2:

[0061]

[0062] Take PLA-SS-PEG-MAL (the molecular weight of polylactic acid PLA is 2000Da, and the molecular weight of polyethylene glycol PEG is 2000Da) 8.322mg, Angiopep-2-Cys(A2-C) 5.28mg (PLA-SS-PEG-MAL and Angiopep-2-Cys in a molar ratio of 1:1.1), in a PBS buffer of pH 7.4, at room temperature, protected from light and anaerobic reaction for 3h; using a dialysis bag with a molecular weight cut-off of 3500Da, placed in pure water for 24h dialysis to remove Free A2-C and buffer salts were used to prepare PLA-SS-PEG-A2.

[0063] PLA-SS-PEG-A2 1 H-NMR (CDCl 3 ) spectrum shows that the chemical shift of 6.72 ppm is the characteristic peak of maleimide (MAL) group in the raw material PLA-SS-PEG-MAL, while in PLA-SS-PEG-A2 1 The characteristic peaks of MAL disappeared in the H-NMR spectrum, indicating that the MAL group of PLA-SS-PEG-MAL was coupled with the thiol group of A2-C. HPLC chart ( figure 1 ) also shows: the...

Embodiment 3

[0065] Preparation of brain-targeted nanoformulations co-delivered with rhynchophylline and Tariquidar:

[0066]Step (1), preparation of organic phase: take 10 mg of 60%-γ-PFGA (Example 1), add 0.5 mL of DMSO, stir overnight to dissolve, and obtain a 60%-γ-PFGA solution with a concentration of 20 mg / mL; 1 mg of cymenine and 0.5 mg of Tariquidar were added to the 60%-γ-PFGA solution, and stirred for 1 h to dissolve urticine and Tariquidar to obtain a 60%-γ-PFGA solution containing uricine and Tariquidar as the organic phase;

[0067] Step (2), the preparation of water phase: take 2mg PLA-SS-PEG-A2 (Example 2), 8mg E-TPGS, add 1mL of saturated urticine aqueous solution, stir and dissolve to obtain 1mL PLA-SS-PEG-A2 Aqueous phase with a concentration of 2 mg / mL;

[0068] Step (3), preparation of nano-preparation by nano-precipitation method: take 1 mL of aqueous phase, heat to 65°C, add 100 μL of organic phase dropwise to the aqueous phase while stirring, stir for 1 h, and slowl...

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Abstract

The invention discloses a brain-targeted nano preparation containing rhynchophylline, which is a nano preparation with a core-shell structure, which is prepared by taking 60%-gamma-PFGA as a core material of nanoparticles with the core-shell structure, taking PLA-SS-PEG-A2 as a shell material of nanoparticles with the core-shell structure, taking E-TPGS as a nonionic surfactant, and loading rhynchophylline or simultaneously loading rhynchophylline and Tariquilar. The brain-targeted nano preparation containing the rhynchophylline is small in particle size and stable in structure, has slow release and controlled release effects, overcomes the difficulty of low entrapment efficiency of the rhynchophylline, and improves the brain-targeted property of the rhynchophylline at the same time.

Description

technical field [0001] The invention belongs to the field of targeted nano-formulations, and relates to a brain-targeted nano-formulation containing rhynchophylline and a preparation method thereof, in particular to a brain-targeted nano-formulation containing only rhynchophylline or co-delivery of rhynchophylline and Tariquidar, and a preparation method thereof. its preparation method. Background technique [0002] Rhynchophylline (Rhynchophylline) is an alkaloid isolated from the Rubiaceae plant Uncaria. As one of the drugs for the treatment of Parkinson's (PD), rhynchophylline has a protective effect on the nervous system, by regulating glutamate, acetylcholine, regulating inflammatory factors and related pathways, resisting neuronal apoptosis, and reducing intracellular Ca 2+ Overloading, improving neurodegenerative diseases and other ways to play its effect, suggesting that it has a certain development value as a PD treatment or prevention drug. However, it is difficu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/34A61K47/42A61K47/22A61K31/438A61K31/4725A61P25/16B82Y5/00B82Y40/00
CPCA61K9/5146A61K9/5192A61K47/42A61K47/22A61K31/438A61K31/4725A61P25/16B82Y5/00B82Y40/00A61K2300/00Y02A50/30
Inventor 柳文媛韩凌飞谢路宽冯锋刘富垒曲玮
Owner CHINA PHARM UNIV
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