Timosaponin aⅢ nano liposome and its preparation method and application

Abstract

The invention relates to the field of pharmaceutical preparations and traditional Chinese medicine preparations and discloses a nano liposome containing a traditional Chinese medicine effective component timosaponin AIII. A preparation method of the nano liposome comprises the following steps: (1) mixing a timosaponin AIII solution and a film material solution; removing a solvent and moisture to obtain a lipid thin film; (2) adding a phosphate buffering solution and hydrating to obtain a timosaponin AIII liposome rough suspension solution; (3) carrying out ultrasonic treatment or high-pressure homogenization treatment at 40 DEG C to 60 DEG C to obtain the timosaponin AIII nano liposome. The timosaponin AIII nano liposome can be used for preparing a medicine for inhibiting tumor cell proliferation and has a good application prospect.

Description

technical field

[0001] The invention relates to the field of preparations of medicine and Chinese pharmacy, in particular to the nanoliposome of timosaponin AⅢ, an active ingredient of traditional Chinese medicine, its preparation method and its application in the preparation of antitumor drugs. Background technique

[0002] Cancer, also known as malignant tumor (Malignant neoplasm), is a disease caused by the abnormal mechanism of controlling cell growth and proliferation. As a major disease that seriously threatens human life, tumor has become the main factor of human death due to its low cure rate and high recurrence rate. According to reports, in 2012, a total of 8.2 million people died worldwide, of which lung cancer, liver cancer, gastric cancer, and colorectal cancer were the main causes. At present, the main treatment methods for cancer include surgery, radiation therapy and chemotherapy to treat the disease or prolong life and improve the quality of life of patient...

Examples

Embodiment 1

[0038] Embodiment 1, timosaponin AⅢ nano liposome preparation (prescription 1)

[0039]Weigh 0.8 mg timosaponin AⅢ and dissolve in 400 μL methanol; weigh 8.35 mg egg yolk lecithin (EPC) and dissolve it in 200 μL chloroform solution, and ultrasonically dissolve. Combine the above solutions into a round-bottomed test tube with a stopper, blow dry with nitrogen to remove methanol and chloroform, until a uniform lipid film is formed on the wall of the round-bottomed test tube. The molar ratio of EPC to timosaponin AⅢ was 10:1. -0.09MPa, 45~50℃, dry under reduced pressure to remove residual solvent and moisture, add 200μL 0.01mol / L phosphate buffer (pH=7.4), hydrate under 45~50℃ water bath for 1 hour, and obtain timosaponin AⅢ ester Plastid suspension. The timosaponin AⅢ liposome suspension is sonicated 3 times under the conditions of ultrasonic frequency 40-100 Hz and power 200-300 W, each ultrasonic time is 3-5 min, to obtain timosaponin AⅢ nano liposome.

Embodiment 2

[0040] Embodiment 2, timosaponin AⅢ nano liposome preparation (prescription 2)

[0041] Weigh 0.8 mg timosaponin AⅢ and dissolve in 400 μL methanol, weigh 8.53 mg distearoylphosphatidylcholine (DSPC) and dissolve in 200 μL chloroform solution, and dissolve by ultrasonication. Combine the above solutions into a round-bottomed test tube with a stopper, blow dry with nitrogen to remove methanol and chloroform, until a uniform lipid film is formed on the wall of the round-bottomed test tube. The molar ratio of DSPC to timosaponin AⅢ was 10:1. -0.09MPa, 45~50℃, dry under reduced pressure to remove residual solvent and moisture, add 200μL 0.01mol / L phosphate buffer (pH=7.4), hydrate under 45-50℃ water bath for 1 hour, and obtain timosaponin AⅢ ester Plastid suspension. The timosaponin AⅢ liposome suspension is subjected to ultrasonication at an ultrasonic frequency of 40-100 Hz and a power of 200-300 W, and ultrasonicated 3 times for 3-5 minutes each time to obtain timosaponin AⅢ ...

Embodiment 3

[0042] Embodiment 3, timosaponin AⅢ nano liposome preparation (prescription 3)

[0043] Weigh 0.8 mg timosaponin AⅢ and dissolve in 400 μL methanol, weigh 7.51 mg egg yolk lecithin (EPC), 3.02 mg distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) and dissolve in 500 μL chloroform solution , ultrasonically dissolved, combined the above solutions in a round-bottomed test tube, blown dry with nitrogen to remove methanol and chloroform, until a uniform lipid film was formed on the wall of the round-bottomed test tube. The molar ratio of EPC, DSPE-PEG2000 and timosaponin AⅢ was 9:1:1. -0.09MPa, 45~50℃, dry under reduced pressure to remove residual solvent and moisture, add 200μL 0.01mol / L phosphate buffer (pH=7.4), hydrate under 45-50℃ water bath for 1 hour, and obtain timosaponin AⅢ ester Plastid suspension. The timosaponin AⅢ liposome suspension is subjected to ultrasonication at an ultrasonic frequency of 40-100 Hz and a power of 200-300 W, and ultrason...

technical field

[0001] The invention relates to the field of preparations of medicine and Chinese pharmacy, in particular to the nanoliposome of timosaponin AⅢ, an active ingredient of traditional Chinese medicine, its preparation method and its application in the preparation of antitumor drugs. Background technique

[0002] Cancer, also known as malignant tumor (Malignant neoplasm), is a disease caused by the abnormal mechanism of controlling cell growth and proliferation. As a major disease that seriously threatens human life, tumor has become the main factor of human death due to its low cure rate and high recurrence rate. According to reports, in 2012, a total of 8.2 million people died worldwide, of which lung cancer, liver cancer, gastric cancer, and colorectal cancer were the main causes. At present, the main treatment methods for cancer include surgery, radiation therapy and chemotherapy to treat the disease or prolong life and improve the quality of life of patient...

Examples

Embodiment 1

[0038] Embodiment 1, timosaponin AⅢ nano liposome preparation (prescription 1)

[0039]Weigh 0.8 mg timosaponin AⅢ and dissolve in 400 μL methanol; weigh 8.35 mg egg yolk lecithin (EPC) and dissolve it in 200 μL chloroform solution, and ultrasonically dissolve. Combine the above solutions into a round-bottomed test tube with a stopper, blow dry with nitrogen to remove methanol and chloroform, until a uniform lipid film is formed on the wall of the round-bottomed test tube. The molar ratio of EPC to timosaponin AⅢ was 10:1. -0.09MPa, 45~50℃, dry under reduced pressure to remove residual solvent and moisture, add 200μL 0.01mol / L phosphate buffer (pH=7.4), hydrate under 45~50℃ water bath for 1 hour, and obtain timosaponin AⅢ ester Plastid suspension. The timosaponin AⅢ liposome suspension is sonicated 3 times under the conditions of ultrasonic frequency 40-100 Hz and power 200-300 W, each ultrasonic time is 3-5 min, to obtain timosaponin AⅢ nano liposome.

Embodiment 2

[0040] Embodiment 2, timosaponin AⅢ nano liposome preparation (prescription 2)

[0041] Weigh 0.8 mg timosaponin AⅢ and dissolve in 400 μL methanol, weigh 8.53 mg distearoylphosphatidylcholine (DSPC) and dissolve in 200 μL chloroform solution, and dissolve by ultrasonication. Combine the above solutions into a round-bottomed test tube with a stopper, blow dry with nitrogen to remove methanol and chloroform, until a uniform lipid film is formed on the wall of the round-bottomed test tube. The molar ratio of DSPC to timosaponin AⅢ was 10:1. -0.09MPa, 45~50℃, dry under reduced pressure to remove residual solvent and moisture, add 200μL 0.01mol / L phosphate buffer (pH=7.4), hydrate under 45-50℃ water bath for 1 hour, and obtain timosaponin AⅢ ester Plastid suspension. The timosaponin AⅢ liposome suspension is subjected to ultrasonication at an ultrasonic frequency of 40-100 Hz and a power of 200-300 W, and ultrasonicated 3 times for 3-5 minutes each time to obtain timosaponin AⅢ ...

Embodiment 3

[0042] Embodiment 3, timosaponin AⅢ nano liposome preparation (prescription 3)

[0043] Weigh 0.8 mg timosaponin AⅢ and dissolve in 400 μL methanol, weigh 7.51 mg egg yolk lecithin (EPC), 3.02 mg distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) and dissolve in 500 μL chloroform solution , ultrasonically dissolved, combined the above solutions in a round-bottomed test tube, blown dry with nitrogen to remove methanol and chloroform, until a uniform lipid film was formed on the wall of the round-bottomed test tube. The molar ratio of EPC, DSPE-PEG2000 and timosaponin AⅢ was 9:1:1. -0.09MPa, 45~50℃, dry under reduced pressure to remove residual solvent and moisture, add 200μL 0.01mol / L phosphate buffer (pH=7.4), hydrate under 45-50℃ water bath for 1 hour, and obtain timosaponin AⅢ ester Plastid suspension. The timosaponin AⅢ liposome suspension is subjected to ultrasonication at an ultrasonic frequency of 40-100 Hz and a power of 200-300 W, and ultrason...

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