Gambogic acid core-shell structure composite nanometer preparation and preparation method thereof

A nano-formulation, core-shell structure technology is applied in the field of gambogic acid core-shell structure composite nano-formulation and its preparation, and can solve problems such as affecting drugability and the like

Active Publication Date: 2018-02-23
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The object of the present invention is to provide gambogic acid C-SNP with controllable process, good stability, and active targeti

Method used

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  • Gambogic acid core-shell structure composite nanometer preparation and preparation method thereof
  • Gambogic acid core-shell structure composite nanometer preparation and preparation method thereof
  • Gambogic acid core-shell structure composite nanometer preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0137] Preparation of poly(γ-glutamic acid)-hexadecyltrimethylammonium complex:

[0138] Weigh 10 g of poly(γ-sodium glutamate) with a molecular weight of 100 KDa, dissolve it in 200 mL of water, add 3% cetyltrimethylammonium bromide aqueous solution dropwise under stirring until no precipitation occurs, and depressurize The precipitate filtered by suction was washed three times with an appropriate amount of hot water, and dried in vacuo to obtain 21.53 g of a white solid, which was poly(γ-glutamic acid)-hexadecane prepared from poly(γ-sodium glutamate) with a molecular weight of 100KDa. Alkyltrimethylammonium complex (expressed as γ-P gambogic acid-CTA-100KDa).

Embodiment 2

[0140] Preparation of poly(γ-glutamic acid)α-benzyl ester:

[0141] Take 2 g of γ-P gambogic acid-CTA-100KDa (containing 4.84 mmol of glutamic acid units), dissolve it in 60 mL of NMP, add 1.22 g of NaHCO 3 (14.52mmol), 0.414mL benzyl bromide (5.33mmol), heated and stirred at 50°C to dissolve the γ-P gambogic acid-CTA complex, and reacted at 50°C for 8h. After the reaction finishes, let it stand for cooling, and filter to remove insoluble matter (excessive NaHCO 3 and the generated NaBr), the filtrate was poured into 200mL of methanol, and then 100mL of 4% aqueous hydrochloric acid was added, stirred for 0.5h in an ice bath, filtered under reduced pressure, and washed three times with an appropriate amount of cold methanol:water (2:1), and the obtained precipitate was dissolved In 50mL NMP, repeat the above operation, and vacuum dry to obtain 0.9044g of white powder, which is poly(γ-glutamic acid)α-benzyl poly(γ-glutamic acid sodium) with a molecular weight of 100,000 Da. Es...

Embodiment 3

[0144] Acidification of sodium hyaluronate and preparation of hyaluronic acid-tetrabutylammonium complex:

[0145] Take 31.5 g of the pretreated strong-acid ion-exchange resin, wash it with deionized water until neutral. Weigh 9 g of HA-Na (14600 Da), add 450 mL of deionized water to obtain a 2% (w / v) HA-Na aqueous solution, add it to a strong acid ion exchange resin column, stir at room temperature for 6 hours, and check the exchange effect with pH test paper. HA aqueous solution was obtained by filtration (the pH of 2% w / v HA-Na aqueous solution was 6-7, and the pH of 2% w / v HA aqueous solution was 3).

[0146] Take 25% TBA-OH aqueous solution and add it dropwise to the above HA aqueous solution under stirring at room temperature until the pH of the solution system is ~7 (a total of 21 mL of TBA-OH aqueous solution is used), freeze-dry to obtain 13.6 g of white solid, which is transparent Hyaluronic acid-tetrabutylammonium complex (HA-TBA), which 1 H-NMR see image 3 .

...

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Abstract

The invention discloses a gambogic acid core-shell structure composite nanometer preparation and a preparation method thereof. According to the composite nanometer preparation, poly-(gamma-glutamic acid)alpha-benzyl ester is adopted as a nuclear material, hyaluronic acid grafted with retinoic acid is adopted as a shell material, the nuclear material is located inside the nanometer preparation in ananoparticle mode, pi-pi stacking and lyophobic impact force is used for loading gambogic acid, an amphipathy material adopts lipophilic retinoic acid to be arranged around nanoparticles in a wrapping mode, a hydrophilic hyaluronic acid chain is located on the outermost side of the nanometer preparation, and the shell material achieves the effects of protecting medicine inside a core, maintainingthe stability of the nanometer preparation and achieving active targeting. The preparation mainly has the advantages that the nanometer preparation is controllable in preparation technology, good instability and high in packaging rate, has the active targeting capability, can well solve the problems affecting the druggability of gambogic acid that the water solubility is poor, instability is caused, metabolic clearance is likely to be caused, can improve the anti-neoplastic activity of gambogic acid, and can eliminate the existing slight toxic and side effect of the gambogic acid.

Description

technical field [0001] The invention belongs to the field of biomedical polymer materials and nano-biotechnology, and specifically relates to a gambogic acid core-shell structure composite nano-preparation and a preparation method thereof. Background technique [0002] Gambogic acid is one of the main anti-tumor active ingredients of the traditional Chinese medicine gambogic resin. A large number of studies have shown that gambogic acid can play a very good anti-tumor effect through various mechanisms, and compared with traditional chemotherapy drugs, gambogic acid has less toxic side effects. Low, except for the vascular irritation during intravenous injection, it has no significant impact on the hematopoietic function and immune function of tumor-bearing animals, and the animals are well tolerated. Clinical test data show that the maximum tolerated dose of gambogic acid is 55mg / m 2 , the main adverse reactions are liver function damage, vascular irritation and so on. Howe...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/34A61K47/36A61K47/12A61K47/26A61K47/08A61K31/352A61P35/00C08G69/48C08B37/08
CPCA61K9/5123A61K9/5146A61K9/5161A61K31/352C08B37/0072C08G69/48
Inventor 柳文媛冯锋刘富垒曲玮胡乐坚韩凌飞黄晓娴李凌超
Owner CHINA PHARM UNIV
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