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Hyaluronic acid-modified total alkaloid hybrid lipid nano-preparation and its preparation method and application

A total alkaloid and lipid nanotechnology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, anti-inflammatory agents, etc., can solve the problem of lack of targeting and high toxicity of total alkaloids of bitter wood , Poor water solubility and other issues, to achieve the effect of improving anti-inflammatory activity, good loading performance, and good uniformity

Active Publication Date: 2021-08-31
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, no alkaloid monomers with excellent activity in bitter wood have been found, and the total alkaloid parts of bitter wood are still used clinically [Chen Meng. Research on the active components of bitter wood alkaloids [D]. Yantai University, 2007.]
The total alkaloids of bitter wood have high toxicity, poor water solubility, and lack of targeting, which limits its clinical application. The present invention is aimed at the preparation of nano preparations of total alkaloids of bitter wood with a compound with a large π conjugated system to meet clinical needs

Method used

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  • Hyaluronic acid-modified total alkaloid hybrid lipid nano-preparation and its preparation method and application
  • Hyaluronic acid-modified total alkaloid hybrid lipid nano-preparation and its preparation method and application
  • Hyaluronic acid-modified total alkaloid hybrid lipid nano-preparation and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0058] Synthesis of BzPGA: Dissolve 10 g of γ-PGA with a molecular weight of 1 million Da in 200 mL of deionized water, and add 3% (w / v) cetyltrimethylammonium chloride aqueous solution dropwise under stirring until no precipitation occurs. , stirred for 5 minutes, filtered through a sand core funnel, washed the white precipitate with an appropriate amount of hot deionized water until the dripping filtrate had no bubbles, and freeze-dried to obtain a white solid powder γ-PGA-CTA; take 2 g of the above γ-PGA-CTA and 1.036 g NaHCO 3 Dry in a desiccator overnight to remove trace moisture, add to 60mL anhydrous nitrogen methylpyrrolidone (NMP), add 1.88mL benzyl bromide under ice bath, react at 55°C for 8h until the solution is slightly clear; cool to room temperature, remove excess by suction filtration NaHCO 3 and NaCl, the filtrate was poured into a mixed solution of 200 mL methanol and 100 mL 1% HCl, stirred in an ice bath for 0.5 h, filtered through a sand core funnel, and t...

Embodiment 2

[0060] mPEG-b-C 16 Synthesis:

[0061] (1) Dissolve 5g of mPEG-OH in 50mL of anhydrous toluene, azeotropically remove water for 2-3h under the protection of argon, cool to room temperature, add anhydrous dichloromethane dropwise under ice bath until the solution is clear; 0.520mL triethylamine, then add 0.290mL methanesulfonyl chloride dropwise, react in ice bath for 18h, remove insoluble methanesulfonate hydrochloride by suction filtration, precipitate with excess ether; add the above product into a round bottom flask, add 85mL 25% ammonia water, sealed with a parafilm, stirred and reacted at 20°C for 4 days, volatilized the ammonia in the fume hood until the wet pH test paper did not change color; added 5M sodium hydroxide drop by drop to adjust the pH to 13, dichloro Extracted 3 times with methane (3×25mL), washed with concentrated brine, dried over anhydrous sodium sulfate, concentrated by rotary evaporation, precipitated excess diethyl ether, evaporated diethyl ether by ...

Embodiment 3

[0064] Investigate the effect of different L / P values ​​on particle size and PDI

[0065] Prepare 10mL of 4mg / mL BzPGA / DMSO solution as the organic phase; prepare 10mL of 10% ethanol aqueous solution with soybean lecithin concentrations of 0, 0.04, 0.08, 0.15, and 0.24 mg / mL, and ultrasonicate in a water bath for 3-5 minutes before preparation , heated in a water bath to 65°C as the water phase; use a micro-injection pump to inject the BzPGA solution into the water phase solution at a rate of 30mL / h, during the injection process, keep the water phase at 65°C, the injection volume is 1mL, stir at a low speed, and the injection is completed Then vortex at high speed for 3 minutes to volatilize the ethanol to disperse the soybean lecithin and prevent the soybean lecithin from being wrapped in the nucleus, then slowly stir for 2 hours to room temperature, transfer the solution to the Amicon Ultra-15 ultrafiltration tube for ultrafiltration and centrifugation, Rotate at 2000rpm, wa...

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Abstract

The present invention relates to the total alkaloid hybrid lipid nano-preparation of bitterwood, which discloses the total alkaloid hybrid lipid nano-preparation of bitterwood modified by hyaluronic acid and its preparation method and application; ‑BzPGA) as the core material, amphiphilic compounds such as soybean lecithin containing 98% phosphatidylcholine (PC) and dipalmitoylphosphatidylethanolamine (DPPE) as surfactants, hyaluronic acid (HA) or Polyethylene glycol-b-palmitic acid (PEG-b-C16) is the shell material; this carrier can be used to load the total alkaloids of Materia lanceolata. The preparation method is mature and efficient, and provides the possibility for the preparation of the complex active ingredients of the total alkaloids and other active monomer nano-preparations.

Description

technical field [0001] The present invention relates to total alkaloid hybrid lipid nano-preparation of bitter wood, in particular to hyaluronic acid (HA) or PEGylated total alkaloid hybrid lipid nano-preparation of bitter wood and its preparation method Background technique [0002] Core-shell nanoparticles (Core-shell nanoparticles) consist of one material as its core and another material as its shell wrapped around the outside of the core through non-covalent interactions. It was first used as a lipid-polymer Lipid-polymer hybrid NPs was proposed by Chinese scholar Zhang Liangfang in 2009. Based on polymer micelles and liposomes, the author designed and synthesized a new type of lipid-polymer hybrid NPs for large quantities of fat-soluble drugs. A new type of preparation between body and micelles, the related research results were published in ACS nano, the top journal of American nano preparations [ZhangL, Chan J M, Gu F X, et al.Self-assembled lipid-polymer hybrid nanop...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K36/185A61K47/61A61K47/69A61K47/24A61K47/14A61P19/02A61P29/00A61K135/00
Inventor 曲玮柳文媛刘博文冯锋刘富垒李聪
Owner CHINA PHARM UNIV
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