CN103462898A - Breast cancer treatment triptolide liposome preparation and preparation method thereof - Google Patents
Breast cancer treatment triptolide liposome preparation and preparation method thereof Download PDFInfo
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- CN103462898A CN103462898A CN2013103403368A CN201310340336A CN103462898A CN 103462898 A CN103462898 A CN 103462898A CN 2013103403368 A CN2013103403368 A CN 2013103403368A CN 201310340336 A CN201310340336 A CN 201310340336A CN 103462898 A CN103462898 A CN 103462898A
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Abstract
The present invention discloses a breast cancer treatment triptolide liposome preparation and a preparation method thereof, wherein the breast cancer treatment triptolide liposome preparation is a liposome preparation prepared from a breast cancer treatment traditional Chinese medicine active effective component triptolide. The preparation method comprises: adopting an ethanol injection method to prepare liposomes to obtain the breast cancer (breast cancer and triple-negative breast cancer) treatment triptolide liposome preparation. According to the breast cancer treatment triptolide liposome preparation, in vivo animal anti-cancer pharmacological experiment results show that: significant growth inhibition effects are provided for breast cancer and triple-negative breast cancer, and anti-cancer activity of the breast cancer treatment triptolide liposome preparation is respectively and significantly higher than anti-cancer activities of chemotherapy drugs such as paclitaxel and cisplatin. In addition, the triptolide liposome preparation provides a higher anti-cancer effect than the triptolide non-liposome preparation.
Description
One, technical field
The present invention relates to the Chinese medicine technical field, specifically relate to a kind of triptolide Liposomal formulation for the treatment of breast carcinoma and preparation method thereof.
Two, background technology
Cancer is the formidable enemy of harm humans health.The annual new cases of cancer of China approximately has 1,600,000 people, and that dies from cancer every year approximately has 1,300,000 people, rises year by year because of the dead number of cancer in the whole nation, the zone occurred frequently that China is the cancers such as breast carcinoma, pulmonary carcinoma, and cancer mortality is high.
There is no at present the most of cancer patients of effective cured substance.Though chemotherapeutics has certain curative effect to cancer, toxic and side effects is large, and Chinese patent medicine is generally lower to the curative effect of cancer, and curative effect is all undesirable.
The inventor is through the arduous anticancer active substance of studying the Chinese medicines such as Herba Phyllanthi Urinariae, Ramulus et folium taxi cuspidatae, dry maxima skin, Radix Tripterygii Wilfordii decades, therefrom extract multiple anti-cancer active compound, through anticancer experimentation, show, the cancerous cell such as human breast carcinoma, pulmonary carcinoma and zoografting carcinoma are all had to significant inside and outside anticancer therapy effect, and applied for obtaining 10 antineoplastic product invention patent certificates (as the patent No. is respectively: ZL200410041122.1; ZL200610085781.4; ZL200610085781.4; ZL200810124590.3; ZL200810124588.6; ZL201210033666.8 etc.).On the basis of above-mentioned research, the inventor studies again and has invented a kind of triptolide Liposomal formulation for the treatment of breast carcinoma and preparation method thereof, and its active anticancer is high, toxicity is low.
Three, summary of the invention
1, goal of the invention: the purpose of this invention is to provide the anti-breast cancer medicines that a kind of active anticancer is high, toxicity is low, specifically be to provide a kind of triptolide Liposomal formulation for the treatment of breast carcinoma and preparation method thereof.
2, technical scheme:
A kind of triptolide Liposomal formulation for the treatment of breast carcinoma of the present invention is characterized in that it is made by the active effective ingredient of triptolide:
Triptolide (triptolide, TL), (claim again: Radix Tripterygii Wilfordii lactone alcohol), molecular formula: C
20h
24o
6, molecular weight: 360.4.
Chemical structural formula:
A kind of triptolide Liposomal formulation for the treatment of breast carcinoma is characterized in that it is made by triptolide and the liposome of following quality proportioning:
Triptolide: liposome is 1:30; Wherein, the proportioning raw materials of liposome is: the mass ratio of lecithin and amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine is 10:1, and the mass ratio of lecithin and cholesterol is 10:1.
A kind of triptolide Liposomal formulation for the treatment of breast carcinoma for preparing is characterized in that the preparation process of said preparation is as follows:
(1) proportioning raw materials for preparing liposome is: the mass ratio of lecithin and amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine is 10:1, and the mass ratio of lecithin and cholesterol is 10:1;
(2) preparation method of triptolide liposome adopts the alcohol injection preparation: get the PBS buffer of pH7.4 in eggplant type bottle, in 50～55 ℃ of preheating 30～35min of water bath with thermostatic control;
(3) liposome of getting step 1 proportioning in beaker, the triptolide that to add with the liposome mass ratio be 1:30, then add appropriate dehydrated alcohol to make its dissolving;
(4) after all dissolving, triptolide is injected into rapidly in the eggplant type bottle that buffer solution is housed of step 2 constant temperature preheating, obtain the milky liposome turbid liquor, continue to stir aquation 1～1.2h, evacuation is except ethanol, 800P crosses 10～12 circulations of high pressure dispersing emulsification machine, obtains the triptolide Liposomal formulation.
The application of described triptolide liposome in preparation treatment breast cancer medicines.
The application of described triptolide liposome in preparation treatment three negative breast cancer medicines.
Described triptolide Liposomal formulation has obvious inhibitory action to the growth of breast carcinoma, three negative breast cancer in vivo, and its active anticancer is respectively apparently higher than chemotherapeutic paclitaxel and cisplatin.
The described triptolide Liposomal formulation inhibitory action to breast carcinoma, three negative breast cancer growths in vivo is higher than the non-Liposomal formulation of triptolide.
3, beneficial effect:
A kind of triptolide Liposomal formulation for the treatment of breast carcinoma of the present invention is through Anticancer experiment in animal body, and the growth of breast carcinoma is had to obvious inhibitory action,
The triptolide lipid physical ability of 8mg/kg dosage significantly suppresses the growth (P<0.01) of nude mice transplanted breast carcinoma, nude mice transplantability three negative breast cancer, and its tumour inhibiting rate is respectively 68.70%, 62.62%;
Its active anticancer to breast carcinoma and three cloudy breast carcinoma is respectively higher than chemotherapeutic paclitaxel (P<0.01) and cisplatin (P<0.01).This provides very promising efficient preliminary election medicine for the clinical efficacy that improves anti-breast cancer and anti-three cloudy breast carcinoma.Can be used for treating breast carcinoma and three cloudy breast carcinoma.
Four, the specific embodiment
Embodiment 1: a kind of triptolide Liposomal formulation for the treatment of breast carcinoma, and made by triptolide, the preparation method of its liposome is as follows:
(1) proportioning raw materials for preparing liposome is: lecithin 900mg, and, amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine 90mg, cholesterol 90mg;
(2) preparation method of triptolide liposome adopts the alcohol injection preparation: get the PBS buffer 90ml of pH7.4 in eggplant type bottle, in 50 ℃ of preheating 35min of water bath with thermostatic control;
(3) liposome of getting step 1 proportioning, in beaker, adds the 36mg triptolide, then adds appropriate dehydrated alcohol to make its dissolving;
(4) after all dissolving, triptolide is injected into rapidly in the eggplant type bottle that buffer solution is housed of step 2 constant temperature preheating, obtain the milky liposome turbid liquor, continue to stir aquation 1h, evacuation is except ethanol, 800P crosses 10 circulations of high pressure dispersing emulsification machine, obtains the triptolide Liposomal formulation.
Embodiment 2: a kind of triptolide Liposomal formulation for the treatment of breast carcinoma, and made by triptolide, the preparation method of its liposome is as follows:
(1) proportioning raw materials for preparing liposome is: lecithin 600mg, and, amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine 60mg, cholesterol 60mg;
(2) preparation method of triptolide liposome adopts the alcohol injection preparation: get the PBS buffer 90ml of pH7.4 in eggplant type bottle, in 55 ℃ of preheating 30min of water bath with thermostatic control;
(3) liposome of getting step 1 proportioning, in beaker, adds the 24mg triptolide, then adds appropriate dehydrated alcohol to make its dissolving;
(4) after all dissolving, triptolide is injected into rapidly in the eggplant type bottle that buffer solution is housed of step 2 constant temperature preheating, obtain the milky liposome turbid liquor, continue to stir aquation 1.2h, evacuation is except ethanol, 800P crosses 12 circulations of high pressure dispersing emulsification machine, obtains the triptolide Liposomal formulation.
Embodiment 3: the inhibitory action of a kind of triptolide Liposomal formulation to the nude mice transplanted breast carcinoma
1, laboratory animal and tumor strain
Female BALB/C-nu/nu nude mice, 50, weight 18-20g, purchased from zoopery center, this school.Human breast cancer cell strain MCF-7, purchased from zoopery center, institute of oncology, Jiangsu Province.
2, modeling and experimental technique
50 of BALB/C-nu/nu nude mices, stay 10 negative matched groups in proportion at random, and all the other 40 are carried out modeling.Get the exponential phase MCF-7 Human Breast Cancer Cells of In vitro culture, cell concentration is adjusted into 1 * 10
7/ ml.Under aseptic condition, MCF-7 Human Breast Cancer Cells is inoculated in to BALB/C-nu/nu nude mice back, inoculum concentration is that only (cell number is 2 * 10 to 0.2ml/
6/ only).Whole seeded process must be carried out with sterile working in aseptic cover, completes inoculation in 1h.
Be divided at random 4 groups after inoculation, 10 every group, be respectively tumor model matched group, paclitaxel positive controls, triptolide and 2 test group of triptolide liposome, separately add negative control group, totally 5 groups.After inoculation oncocyte 24h, test group lumbar injection triptolide and triptolide liposome, positive controls lumbar injection paclitaxel, dosage is 8mg/kg, negative control group and tumor model matched group lumbar injection equal-volume injectable drug solvent, each treated animal is all by the 0.2ml lumbar injection, successive administration 3 weeks.Next day after the last administration, observe as follows:
Completely peel off the tumor piece, and the calculating tumor control rate of weighing, tumor control rate=(model control group tumor weight-test of cure group tumor weight)/model control group tumor weight * 100%.
3, experimental result:
The inhibitory action of a kind of triptolide Liposomal formulation to the nude mice transplanted breast carcinoma: 8mg/kg triptolide Liposomal formulation can significantly suppress the growth (P<0.01) of nude mice transplanted breast carcinoma, its anti-breast cancer activity is higher than non-liposome triptolide (P<0.01), and non-liposome triptolide anti-breast cancer activity is again higher than chemotherapeutic paclitaxel (P<0.01).In Table 1.
Table 1 triptolide Liposomal formulation is to the effect of nude mice transplanted breast carcinoma
Embodiment 4: the inhibitory action of a kind of triptolide Liposomal formulation to nude mice transplantability three negative breast cancer
1, laboratory animal and tumor strain
Female BALB/c nude mice, 50, weight 18-20g, purchased from zoopery center, this school.People three negative breast cancer cell strain MDA-MB-231, purchased from zoopery center, institute of oncology, Jiangsu Province.
2, modeling and experimental technique
50 of BALB/c nude mices, stay 10 negative matched groups in proportion at random, and all the other 40 are carried out modeling.Get the exponential phase MCF-7 Human Breast Cancer Cells of In vitro culture, cell concentration is adjusted into 1 * 10
7/ ml.Under aseptic condition, human breast carcinoma MDA-MB-231 cell is inoculated in to BALB/c nude mice right side scapular region subcutaneous, inoculum concentration is that only (cell number is 2 * 10 to 0.2ml/
6/ only).Whole seeded process must be carried out with sterile working in aseptic cover, completes inoculation in 1h.
Be divided at random 4 groups after inoculation, 10 every group, be respectively tumor model matched group, cisplatin positive controls, triptolide and 2 test group of triptolide liposome, separately add negative control group, totally 5 groups.After inoculation oncocyte 24h, test group lumbar injection triptolide and triptolide liposome, positive controls lumbar injection cisplatin, dosage is 8mg/kg, negative control group and tumor model matched group lumbar injection equal-volume injectable drug solvent, each treated animal is all by the 0.2ml lumbar injection, successive administration 3 weeks.Next day after the last administration, observe as follows:
Completely peel off the tumor piece, and the calculating tumor control rate of weighing, tumor control rate=(model control group tumor weight-test of cure group tumor weight)/model control group tumor weight * 100%.
3, experimental result:
The inhibitory action of a kind of triptolide Liposomal formulation to the nude mice transplanted breast carcinoma: 8mg/kg triptolide Liposomal formulation can significantly suppress the growth (P<0.01) of nude mice transplanted breast carcinoma, its anti-breast cancer activity is higher than non-liposome triptolide (P<0.01), and non-liposome triptolide anti-breast cancer activity is again higher than chemotherapeutic cisplatin (P<0.01).In Table 2.
Table 2 triptolide Liposomal formulation is to the three negative breast cancer effects of nude mice transplantability
Claims (6)
1. a triptolide Liposomal formulation for the treatment of breast carcinoma is characterized in that it is made by triptolide and the liposome of following quality proportioning:
Triptolide: liposome is 1:30; Wherein, the proportioning raw materials of liposome is: the mass ratio of lecithin and amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine is 10:1, and the mass ratio of lecithin and cholesterol is 10:1.
2. a triptolide Liposomal formulation for preparing treatment breast carcinoma claimed in claim 1 is characterized in that the preparation process of said preparation is as follows:
(1) proportioning raw materials for preparing liposome is: the mass ratio of lecithin and amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine is 10:1, and the mass ratio of lecithin and cholesterol is 10:1;
(2) preparation method of triptolide liposome adopts the alcohol injection preparation: get the PBS buffer of pH7.4 in eggplant type bottle, in 50～55 ℃ of preheating 30～35 min of water bath with thermostatic control;
(3) liposome of getting step 1 proportioning in beaker, the triptolide that to add with the liposome mass ratio be 1:30, then add appropriate dehydrated alcohol to make its dissolving;
(4) after all dissolving, triptolide is injected into rapidly in the eggplant type bottle that buffer solution is housed of step 2 constant temperature preheating, obtain the milky liposome turbid liquor, continue to stir aquation 1～1.2 h, evacuation is except ethanol, 800 P cross 10～12 circulations of high pressure dispersing emulsification machine, obtain the triptolide Liposomal formulation.
3. the application of triptolide Liposomal formulation as claimed in claim 1 in preparation treatment breast cancer medicines.
4. the application of triptolide liposome as claimed in claim 1 in preparation treatment three negative breast cancer medicines.
5. triptolide Liposomal formulation as claimed in claim 1 has obvious inhibitory action to the growth of breast carcinoma, three negative breast cancer in vivo, and its active anticancer is respectively apparently higher than chemotherapeutic paclitaxel and cisplatin.
6. the inhibitory action to breast carcinoma, three negative breast cancer growths is higher than the non-Liposomal formulation of triptolide in vivo for triptolide Liposomal formulation as claimed in claim 1.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105125493A (en) * | 2015-09-11 | 2015-12-09 | 华侨大学 | Preparation method for triptolide nano-liposome |
| CN105233292A (en) * | 2015-10-19 | 2016-01-13 | 中国科学院北京基因组研究所 | Application of ORY-1001 to treatment of triple negative breast cancer through combined radiotherapy and chemotherapy |
| CN108186574A (en) * | 2018-03-01 | 2018-06-22 | 燕山大学 | A kind of triptolide liposome of platinum-gold nano ball shell cladding and preparation method thereof |
| CN113143985A (en) * | 2021-01-25 | 2021-07-23 | 河南中医药大学 | Application of liposome of radix Tripterygii Wilfordii extract in preparing medicine for preventing and treating behavior cognitive disorder induced by lipopolysaccharide by nasal administration |
Citations (1)
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| CN102600180A (en) * | 2012-02-15 | 2012-07-25 | 南京中医药大学 | Chinese medicinal active ingredient compound preparation for treating breast cancer and lung cancer and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102600180A (en) * | 2012-02-15 | 2012-07-25 | 南京中医药大学 | Chinese medicinal active ingredient compound preparation for treating breast cancer and lung cancer and preparation method thereof |
Non-Patent Citations (1)
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| 汪少娟等: "雷公藤内酯醇单独及与华蟾素联合对人乳腺癌MCF-7细胞生长影响的实验研究", 《现代中西医结合杂志》 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105125493A (en) * | 2015-09-11 | 2015-12-09 | 华侨大学 | Preparation method for triptolide nano-liposome |
| CN105233292A (en) * | 2015-10-19 | 2016-01-13 | 中国科学院北京基因组研究所 | Application of ORY-1001 to treatment of triple negative breast cancer through combined radiotherapy and chemotherapy |
| CN105233292B (en) * | 2015-10-19 | 2018-03-13 | 中国科学院北京基因组研究所 | The combined radiotherapies of ORY 1001 and chemotherapy are used for the purposes for treating people's triple negative breast cancer |
| CN108186574A (en) * | 2018-03-01 | 2018-06-22 | 燕山大学 | A kind of triptolide liposome of platinum-gold nano ball shell cladding and preparation method thereof |
| CN108186574B (en) * | 2018-03-01 | 2019-08-27 | 燕山大学 | A kind of triptolide liposome and preparation method thereof of platinum-gold nano ball shell cladding |
| CN113143985A (en) * | 2021-01-25 | 2021-07-23 | 河南中医药大学 | Application of liposome of radix Tripterygii Wilfordii extract in preparing medicine for preventing and treating behavior cognitive disorder induced by lipopolysaccharide by nasal administration |
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Application publication date: 20131225 |