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Preparation method for palm wax solid lipid drug carrier loaded with gossypol and derivative thereof

A technology of palm wax and derivatives, which is applied in the direction of pharmaceutical formulation, drug combination, drug delivery, etc., to achieve good biocompatibility, improve therapeutic effect, and good therapeutic effect

Inactive Publication Date: 2016-03-09
扶风慈缘生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on using palm wax as a drug nanocarrier preparation

Method used

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  • Preparation method for palm wax solid lipid drug carrier loaded with gossypol and derivative thereof
  • Preparation method for palm wax solid lipid drug carrier loaded with gossypol and derivative thereof
  • Preparation method for palm wax solid lipid drug carrier loaded with gossypol and derivative thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A preparation method of a palm wax solid lipid drug carrier of gossypol acetate, comprising the following steps:

[0027] Step 1. Disperse 25 mg of gossypol acetate in 10 mL of ethanol under 100 KHz ultrasound for 3 minutes to prepare a mixture of gossypol acetate and ethanol;

[0028] Step 2: Take 1g of palm wax, heat it to melt, fully mix 10mL of the gossypol acetate ethanol mixture in step 1 with the melted palm wax, and use a rotary evaporator to distill under reduced pressure to remove the ethanol in the system to obtain 25mg / mL of acetic acid Gossypol Palm Wax Blend;

[0029] Step 3, configuring a Pluronic F127 aqueous solution with a concentration of 0.5% (M / V);

[0030] Step 4, heat and melt the gossypol acetate palm wax mixture in step 3, take 50 μ L in a test tube, add 4 mL of 0.5% (M / V) Pluronic F127 solution, and use an ultrasonic probe under ice-water bath conditions. Ultrasound at 400w power for 2 minutes to form nano solid lipid particles;

[0031] Ste...

Embodiment 2

[0035] A preparation method of a palm wax solid lipid drug carrier of apogossypol, comprising the following steps:

[0036] Step 1. Dissolve 50 mg of apogossybolone in 20 mL of ethanol, and disperse it under 100KHz ultrasound for 30 minutes to prepare apogossypolone-ethanol mixture;

[0037] Step 2: Take 0.5g of palm wax, heat and melt; fully mix 20mL of the apogossolone ethanol mixture in step 1 with the melted palm wax, and use a rotary evaporator to distill under reduced pressure to remove the ethanol in the system to obtain 100mg / mL of apogossolone palm wax mixture;

[0038] Step 3, configuring a Pluronic F127 aqueous solution with a concentration of 1% (M / V);

[0039] Step 4, heat and melt the apogossolone palm wax mixture in step 3, take 100 μL in a test tube, add 4 mL of 1% (M / V) Pluronic F127 solution, and use an ultrasonic probe under ice-water bath conditions. Ultrasound at 400w power for 10 minutes to form nano solid lipid particles;

[0040] Step 5, using a cen...

Embodiment 3

[0044] A preparation method of a palm wax solid lipid drug carrier of apogossypol, comprising the following steps:

[0045] Step 1. Dissolve 50 mg of apogossypol in a mixture of 14 mL of ether and 6 mL of ethanol, and disperse it under 100 KHz ultrasound for 15 minutes to prepare a mixture of apogossypol ether and ethanol;

[0046] Step 2: Take 1g of palm wax, heat and melt; mix 20mL of the apogossypol ether-ethanol mixture in step 1 with the melted palm wax, and use a rotary evaporator to distill under reduced pressure to remove the ether and ethanol in the system to obtain 50mg Apogosypol palm wax mixture in / mL;

[0047] Step 3, configuring a Pluronic F68 aqueous solution with a concentration of 1% (M / V);

[0048] Step 4. Heat and melt the apogossypol palm wax mixture in step 3, take 500 μL in a test tube, add 10 mL of 1% (M / V) Pluronic F68 solution, and use an ultrasonic probe under ice-water bath conditions, using 400w Ultrasonic power for 2 minutes to form nano solid l...

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Abstract

The invention provides a preparation method for a palm wax solid lipid drug carrier loaded with gossypol and a derivative thereof. The preparation method comprises the following steps: mixing an organic solvent solution containing gossypol and the derivative thereof with palm wax in a fusion state; carrying out reduced-pressure distillation to remove the organic solvent; allowing the obtained mixture to form nanometer particles in an aqueous solution of a surfactant under the action of supersonic waves; carrying out dialysis to remove the surfactant; and then carrying out filtering and sterilization so as to obtain the gossypol-loaded palm wax solid lipid drug carrier which can be directly applied to intravenous injection administration. The preparation method is a safe, convenient and stable preparation means for preparing drug carrier preparations loaded with gossypol and the derivative thereof.

Description

technical field [0001] The invention relates to a preparation method of a drug carrier, in particular to a method for preparing a palm wax solid lipid drug carrier of gossypol and its derivatives. Background technique [0002] Gossypol is a kind of polyphenolic hydroxyl bis-naphthaldehyde compound, which is a natural product extracted from the seeds of Malvaceae plant cotton. [0003] Gossypol has an effective inhibitory effect on sperm formation and was once widely used as a male contraceptive. In recent years, the anti-tumor properties of gossypol and its derivatives have been discovered. They have the effect of inhibiting cell proliferation for various tumor cells, especially for prostate cancer. Gossypol and its derivatives can also reduce the activity of DNA polymerase and inhibit the proliferation of tumor cells. Gossypol and its derivatives can also bind to the mitochondrial BcL-2 receptor of tumor cells to promote apoptosis of tumor cells. [0004] However, gossyp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/11A61K47/44A61P35/00A61P15/16
CPCA61K9/0019A61K9/5176A61K31/11
Inventor 吴道澄刘佳俊吴宥伸
Owner 扶风慈缘生物科技有限公司