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Palmitoyl ascorbic acid ester and docetaxel composite nanoparticles

A technology of ascorbate and docetaxel, which is applied in the direction of drug combinations, antineoplastic drugs, and medical preparations of non-active ingredients, can solve problems such as systemic toxicity, clinical application limitations, and damage, and achieve enhanced drug efficacy and heavy process Good performance and simple process

Inactive Publication Date: 2016-10-12
陈西敬
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a cytotoxic antineoplastic drug, docetaxel has systemic toxicity, especially immune system toxicity such as neutropenia, which has caused great damage to the patient's body and mind, and its clinical application has also been limited.

Method used

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  • Palmitoyl ascorbic acid ester and docetaxel composite nanoparticles
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  • Palmitoyl ascorbic acid ester and docetaxel composite nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: A composition of compound palmitoyl ascorbate / docetaxel The nanoparticle formulation and its preparation are as follows:

[0068] The composition nanoparticle preparation process of the compound palmitoyl ascorbate / docetaxel is:

[0069] A, PLA is dissolved in 6mL acetone to form PLA acetone solution;

[0070] B. Add palmitoyl ascorbate and docetaxel to the PLA acetone solution and vortex to form a solution as the oil phase;

[0071] C. Dissolve lecithin in 10% ethanol solution, add poloxamer 188 and DSPE-PEG-BIOTIN (DPB), wherein lecithin:DPB=10:1, (w / w), 30°C water bath Removal of ethanol as the aqueous phase;

[0072] D. Add the oil phase dropwise at a rate of 1mL / min into the water phase which is stirred at 1000rpm at a constant temperature of 30°C;

[0073] E, continued to stir for 2 hours to remove acetone after the dropwise addition;

[0074] F. Add the nanoparticle solution from which acetone has been removed into a dialysis bag for overnight dial...

Embodiment 2

[0081] Example 2: A composition of compound palmitoyl ascorbate / docetaxel The nanoparticle formulation and its preparation are as follows:

[0082] The composition nanoparticle preparation process of the compound palmitoyl ascorbate / docetaxel is:

[0083] A, PGA is dissolved in 4L acetone to form PGA acetone solution;

[0084] B. Add palmitoyl ascorbate and docetaxel to the PGA acetone solution and vortex to form a solution as the oil phase;

[0085] C. Dissolve lecithin in 20% dichloromethane solution, add polyethylene glycol-dodecyl hydroxystearate lithium, and remove dichloromethane in a water bath at 30°C as the water phase;

[0086] D. Add the oil phase dropwise at a rate of 1mL / min into the water phase which is stirred at 100rpm at a constant temperature of 30°C;

[0087] E, continued to stir for 2 hours to remove acetone after the dropwise addition;

[0088] F. Add the nanoparticle solution from which acetone has been removed into a dialysis bag for overnight dialysi...

Embodiment 3

[0095] Example 3: A composition of compound palmitoyl ascorbate / docetaxel The nanoparticle formulation and its preparation are as follows:

[0096] The composition nanoparticle preparation process of the compound palmitoyl ascorbate / docetaxel is:

[0097] A, PLGA is dissolved in 5L acetone to form PLGA acetone solution;

[0098] B. Add palmitoyl ascorbate and docetaxel to the PLGA acetone solution and vortex to form a solution as the oil phase;

[0099] C. Dissolving soybean lecithin in 20% dichloromethane solution, adding Tween-80, removing dichloromethane in a 30°C water bath as the water phase;

[0100] D. Add the oil phase dropwise at a rate of 1mL / min into the water phase which is stirred at a constant temperature of 500rpm at 30°C;

[0101] E, continued to stir for 2 hours to remove acetone after the dropwise addition;

[0102] F. Add the nanoparticle solution from which acetone has been removed into a dialysis bag for overnight dialysis, then add 100 g of trehalose t...

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Abstract

The invention relates to a composite nanoparticle preparation for injection administration for treatment of tumors, in particular to compound palmitoyl ascorbic acid ester and docetaxel composite nanoparticles and a preparation method thereof. Through combination of palmitoyl ascorbic acid ester and docetaxel, it is found through in-vitro and in-vivo experiments that the composite nanoparticles can remarkably enhance the anti-tumor efficacy of docetaxel, and docetaxel can achieve the efficacy at an extremely-low dose. Through intravenous administration, artery administration, intramuscular administration, subcutaneous administration, intraperitoneal administration and other administration modes, especially interventional administration such as intravenous injection and intratumoral injection, the effectiveness and safety of clinical application of docetaxel are improved. The adopted preparation method is simple in process and low in cost. The prepared nanoparticles are uniform in particle size, high in encapsulation rate and good in drug release property. Compared with palmitoyl ascorbic acid ester nanoparticles or docetaxel single-recipe nanoparticles, the effects of inhibiting tumor cell growth in vitro and resisting tumor proliferation in vivo of the compound are enhanced remarkably.

Description

technical field [0001] The invention relates to a composition nano-preparation for injection and administration to treat tumors, in particular to a composition nano-particle of compound palmitoyl ascorbate and docetaxel and a preparation method thereof. Background technique [0002] Docetaxel is currently the most effective taxane antineoplastic drug in clinical use. The mechanism of action of docetaxel is similar to that of paclitaxel, but its antitumor activity is 1.3-12 times that of paclitaxel. It is clinically used in breast cancer, prostate cancer, lung cancer, gastric cancer, ovarian cancer, cervical cancer, head and neck cancer, pancreatic cancer, non-small cell Lung cancer, etc. Due to the poor water solubility of docetaxel, the current clinical use mainly includes freeze-dried powder injection and water injection injection. The injection first dissolves the drug in Tween 80, and before clinical use, it is diluted to 1 mg / mL with 13% ethanol aqueous solution. When...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K31/375A61K9/14A61K47/24A61P35/00
CPCA61K9/145A61K9/146A61K31/337A61K31/375A61K2300/00
Inventor 卢杨王子厚郭朝瑞陈西敬赵娣李宁陈琪马恩龙张玲
Owner 陈西敬
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