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Aurantiamide acetate-scutebarbatine-palmitate self-assembled nanoparticles as well as preparation method and application thereof

A gold amido alcohol ester and self-assembled nanoparticle technology, which is applied in the direction of drug combination, pharmaceutical formula, ester active ingredients, etc., can solve the problems of unsatisfactory function and final efficiency, low drug loading, etc., and achieve particle size Effect of narrow distribution range, simple preparation method, and increased possibility

Active Publication Date: 2021-08-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the toxicity and low drug loading caused by the non-degradability of nanocarrier materials in vivo, their function and ultimate efficiency in clinical applications are still unsatisfactory.

Method used

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  • Aurantiamide acetate-scutebarbatine-palmitate self-assembled nanoparticles as well as preparation method and application thereof
  • Aurantiamide acetate-scutebarbatine-palmitate self-assembled nanoparticles as well as preparation method and application thereof
  • Aurantiamide acetate-scutebarbatine-palmitate self-assembled nanoparticles as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh 1 mg of golden amido alcohol ester (Aa), 1 mg of barbaline (SA) and 1 mg of palmitate (P), dissolve them in 300 μL of dimethyl sulfoxide (DMSO), stir at room temperature for 30 min, and obtain clear Golden amido alcohol ester solution, barbataline solution, palmitate solution.

[0039] Add the golden amido alcohol ester solution dropwise to 6mL of pure water preheated to 65°C. After the dropwise addition, stir at a constant temperature of 65°C for 2h. Use a dialysis bag (molecular cut-off MWCO=1000Da) and dialyze in pure water for 12h .

[0040] Add barbataline solution dropwise to 6 mL of pure water preheated to 65°C, stir at 65°C for 2 hours after the dropwise addition, and dialyze in pure water for 12 hours using a dialysis bag (molecular cutoff: 1000 Da).

[0041] The palmitate solution was added dropwise to 6 mL of pure water preheated to 65°C. After the dropwise addition, the solution was stirred at a constant temperature of 65°C for 2 h, and dialyzed in pu...

Embodiment 2

[0045] Embodiment 2: the preparation of golden amido alcohol ester-scutelinaline-palmitate self-assembled nanoparticles (ASP NPs)

[0046] Weigh 0.362mg of golden amido alcohol ester (Aa), 0.0543mg of barbaline (SA) and 1.584mg of palmitate (P), dissolve them in 300 μL of absolute ethanol, stir at room temperature for 30min, and obtain a clear ASP solution; The above ASP solution was added dropwise to 6 mL of pure water preheated to 65°C. After the dropwise addition, the solution was stirred at a constant temperature of 65°C for 2 h, and dialyzed in pure water for 12 h using a dialysis bag (molecular cut-off: 1000 Da). Observation of the dialyzed solution showed opalescence, indicating that the gold amido alcohol ester, barbaline and palmitate self-assembled to form ASP nanoparticles (ASP NPs).

Embodiment 3

[0047] Embodiment 3: the preparation of golden amido alcohol ester-scutelinaline-palmitate self-assembled nanoparticles (ASP NPs)

[0048] Weigh 0.362mg of golden amido alcohol ester (Aa), 0.0543mg of barbaline (SA), 1.584mg of palmitate (P), dissolve in 300μL of methanol, stir at room temperature for 30min, and obtain a clear ASP solution; The solution was added dropwise to 6 mL of preheated pure water at 65°C, stirred at 65°C for 2 hours after the dropwise addition, and dialyzed in pure water for 12 hours using a dialysis bag (molecular cutoff: 1000 Da). Observation of the dialyzed solution showed opalescence, indicating that the gold amido alcohol ester, barbaline and palmitate self-assembled to form ASP nanoparticles (ASP NPs).

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Abstract

The invention discloses aurantiamide acetate-scutebarbatine-palmitate self-assembled nanoparticles. The aurantiamide acetate-scutebarbatine-palmitate self-assembled nanoparticles are characterized in that the self-assembled nanoparticles are formed by self-assembling aurantiamide acetate, scutebarbatine and palmitate. The average particle size of the self-assembled nanoparticles is about 150nm, the self-assembled nanoparticles are uniformly distributed in a sphere-like shape, the particle size distribution range is narrow, and the stability is high. The invention further discloses a preparation method of the self-assembled nanoparticles. The preparation method comprises the following steps: dissolving the aurantiamide acetate, the scutebarbatine and the palmitate in a benign organic solvent to form a mixed solution; and dropwise adding the mixed solution into pure water at the constant temperature of 60-70 DEG C, stirring, and dialyzing to remove the organic solvent. In-vitro cytotoxicity experiments show that the self-assembled nanoparticles obviously inhibit proliferation of liver cancer, lung cancer and breast cancer cells. The invention further discloses an application of the self-assembled nanoparticles in preparation of anti-cancer drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a gold amide alcohol ester-scutelinine-palmitate self-assembled nanoparticle and a preparation method and application thereof. Background technique [0002] With increasing morbidity and mortality, cancer has become one of the greatest challenges to human health worldwide. Chemotherapy and radiotherapy have achieved good therapeutic effects in anticancer treatment, but because chemotherapy and radiotherapy do not have tumor targeting in the treatment process, they will cause serious systemic side effects and bring great pain to patients. In recent years, with the progress and development of nanomaterial chemistry, nano drug delivery system has become the focus of research. However, due to the toxicity and low drug loading caused by the non-degradability of nanocarrier materials in vivo, their function and final efficiency in clinical applications are still ...

Claims

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Application Information

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IPC IPC(8): A61K31/444A61K31/222A61K31/23A61K9/14A61P35/00
CPCA61K31/444A61K31/222A61K31/23A61K9/14A61P35/00A61K2300/00
Inventor 曲玮柳文媛朱嘉新冯锋张仲涛王如意
Owner CHINA PHARM UNIV