CN105560193A - Applications of curcumin submicron powder in preparation of anti-cancer drugs - Google Patents
Applications of curcumin submicron powder in preparation of anti-cancer drugs Download PDFInfo
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- CN105560193A CN105560193A CN201410527906.9A CN201410527906A CN105560193A CN 105560193 A CN105560193 A CN 105560193A CN 201410527906 A CN201410527906 A CN 201410527906A CN 105560193 A CN105560193 A CN 105560193A
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Abstract
The present invention discloses applications of curcumin submicron powder in preparation of anti-cancer drugs, wherein curcumin is subjected to an ultrasonic treatment, the treated curcumin is subjected to high pressure homogenization in a high pressure homogenizer, and freeze drying is performed to obtain the curcumin submicron powder with a particle size of 100-1000 nm.
Description
Technical field
The invention belongs to medical art, be specifically related to curcumin sub-micro powder and preparing the application in cancer therapy drug.
Background technology
Generally acknowledge that 0.1 ~ 100nm is nanometer-scale spatial in the world, 100 ~ 1000nm is submicron system, and being less than 1nm is elementide.At art of pharmacy generally by the size definitions of nanoparticle at 1 ~ 1000nm, this scope obviously includes the submicron particle of size at more than 100nm.Nanometer formulation can improve the oral absorption of insoluble drug.Under surfactant and water etc. exist, directly medicine is ground into nano suspension, is suitable for comprising the administrations such as oral, injection and absorbs or targeting to improve.In addition, the chemical composition of submicronized (micronization) also may show some new character.
High pressure homogenize is a kind of method preparing medicament nano powder body, at camptothecine
[2], dyestuff
[3]etc. aspect have many application.High pressure homogenize technique mainly relies on high pressure homogenizer to complete.High pressure homogenizer is made up of high-pressure pump and homogenizing valve two parts, action principle is that raw material is imported the homogenizing valve of expanding slot by high-pressure pump, the material of instantaneous loss of pressure sprays with high flow velocity, collision is on the collision ring of one of valve module, produce shearing, clash into and 3 kinds, hole effect, reach the effect of refinement and homogenizing.
Along with the fast development of China's economy, aged tendency of population is constantly aggravated, industrialization, urbanization and living-pattern preservation, the burden of China's Chronic Non-Communicable Diseases increases the weight of day by day, and death rate caused by it has accounted for 82.45% of disease death, and wherein malignant tumor accounts for All death 22.32%
[5].Infer according to world's cancer report in 2008, current China annual malignant tumor neopathy number of cases is about 2,820,000 examples, expects 2015, and morbidity will reach 341.1 ten thousand examples
[6].Malignant tumor has become one of Etiological of harm humans health.
Curcumin is from Zingiberaceae Curcuma (curcumal) plant Rhizoma Curcumae Longae, a kind of phenoloid extracted in the rhizome of Radix Curcumae etc., is also wherein most important active component.Modern pharmacology shows, the various active such as curcumin has stronger antioxidation, antitumor, antiinflammatory, protect the liver.Especially at anti-tumor aspect, curcumin can affect each stage of tumorigenesis, and the transfer of anticancer, propagation particularly have good inhibitory action to hepatocarcinoma
[7].
The dissolubility of curcumin is poor, not yet has bibliographical information high pressure homogenization technical finesse curcumin nano powder body.
[1] its energy flat. the present and the future [J] of nano-drug preparation. Chinese pharmacists, 2002,5 (7): 421-423.
[2] Sun Baihe, Wang Zhichao, Zhao Xiuhua, etc. anti-solvent-high pressure homogenization method prepares hydroxycamptothecin nano grain technique and character research [J] thereof. modern agriculture science and technology, 2013 (8): 138-139.
[3] Shen Weiqing, Xiang Bin, Gao Jianrong, etc. high pressure homogenize technique prepares the research [J] of superfine disperse dye. dyestuff and dyeing, 2007,44 (2): 43-45.
[4] Ai Xiujuan, Chen Jianhai, flat deep pool, etc. the application [J] of high pressure homogenization technique in nanometer formulation preparation. medical Leader, 2007,26 (9): 1055-1058.
[5] Chen Zhu. whole nation third time cause of the death Retrospect spot-check report. Beijing: publishing house of China Concord Medical Science University, 2008.
[6]FerlayJ,ShinHR,BrayF,etal.Estimatesofworldwideburdenofcancerin2008:
GLOBOCAN2008[J].Internationaljournalofcancer,2010,127(12):2893-2917.
[7] Tan Jun, Guo Hui. curcumin is to the inhibitory action experimentation [J] of hepatocarcinoma. Guangdong pharmacy, 2002,12 (4): 55-57.
Summary of the invention
The present invention aims to provide a kind of curcumin sub-micro powder, and this curcumin sub-micro powder demonstrates the active anticancer stronger than the former powder of curcumin, is therefore intended to protect described curcumin sub-micro powder preparing the application in cancer therapy drug.
Curcumin sub-micro powder is preparing the application in cancer therapy drug, and described curcumin sub-micro powder in high pressure homogenizer, carries out high pressure homogenize by after curcumin supersound process, more obtained particle diameter is the sub-micro powder of 100-1000nm after lyophilization.
Described curcumin sub-micro powder is prepared as follows: take curcumin 150-250mg, adds ultrasonic 3-12min in 200-300mL water; Then join in high pressure homogenizer, respectively at the circulated under pressure 3-6 times of 200,400,600,800Bar, then at the circulated under pressure 30 ~ 40 times of 800 ~ 1500Bar; After discharging, discharging is freezing, then put into lyophilizing, obtain curcumin sub-micro powder.
Described curcumin sub-micro Powder Particle Size more preferably 100-200nm.
The present invention, by high pressure homogenize process to curcumin, is prepared into the nano-powder of curcumin, but we find that its dissolubility in water reduces on the contrary.We compared for the curcumin powder body before and after high pressure homogenize further, find that the more untreated curcumin powder body of the growth inhibited effect of the Rhizoma Curcumae Longae nano-powder after high pressure homogenize process to hepatoma Hep G 2 cells is obviously strengthened.Because nanocurcumin dissolubility does not increase, therefore, curcumin causes the reason that the inhibitory action of external cancer cell not improves bioavailability, and we think that this is a kind of beyond thought result.So we propose patent protection to the purposes of the curcumin of this nanometered disposal.
Preferably, curcumin sub-micro powder of the present invention is prepared as follows: take curcumin 150-250mg, preferred 200mg, adds 200-300mL, ultrasonic 8-12min in preferred 250mL water, preferred 10min; Then join in high pressure homogenizer, respectively 200,400,600, the circulated under pressure of 800Bar 3-6 times, preferably 5 times, the circulated under pressure of 1000Bar 30-40 times, preferably 35 times; After discharging, discharging is freezing at ultra cold storage freezer, then put into freezer dryer lyophilizing; Obtain curcumin sub-micro powder.
Detailed description of the invention
Embodiment 1
1, the preparation process of curcumin sub-micro powder:
Take curcumin 200mg, add ultrasonic 10min in 250mL water; Then join in high pressure homogenizer, respectively 200,400, the circulated under pressure of 600Bar 5 times, the circulated under pressure of 1000Bar 35 times; After discharging, discharging is freezing at ultra cold storage freezer, then put into freezer dryer lyophilizing; Obtain curcumin submicron powder, laser particle analyzer detects this curcumin submicron powder granularity between 100nm-171nm.
The 2 submicronized front and back of curcumin are on the impact of hepatoma Hep G 2 cells growth curve
The growth curve of mtt assay to hepatoma Hep G 2 cells is adopted to observe.
MTT reagent full name is 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide, Chinese chemistry 3-(4 by name, 5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide bromine salt, trade name: tetrazolium bromide.It is a kind of dyestuff of yellow color.
MTT colorimetry is a kind of method detecting cell survival and growth.Its Cleaning Principle is that the succinate dehydrogenase in living cells mitochondrion can make exogenous MTT be reduced to water-insoluble bluish violet crystallization first a ceremonial jade-ladle, used in libation (Formazan) and be deposited in cell, and dead cell is without this function.Dimethyl sulfoxide (DMSO) can first a ceremonial jade-ladle, used in libation in dissolved cell, measures its absorbance value, can indirectly reflect living cells quantity with enzyme-linked immunosorbent assay instrument 490nm wavelength place (also useful 570nm wavelength).Within the scope of certain cell number, the amount that MTT crystallization is formed is directly proportional to cell number.The method has been widely used in Activity determination, large-scale screening anti-tumor medicine, cell toxicity test and the tumor radiosensitivity mensuration etc. of some bioactie agents.Its feature is highly sensitive, economical.
In table 1, result is through statistical computation, and under 12.5 μ g/ml and 25 μ g/ml concentration, curcumin sub-micro powder is on the growth inhibiting impact of hepatoma Hep G 2 cells much larger than former powder, proves that the submicronized rear anticancer effect of curcumin is better than former powder.
The former powder of table 1 variable concentrations curcumin and sub-micro powder are on the growth inhibiting impact of hepatoma Hep G 2 cells
* significant difference.
Claims (3)
1. curcumin sub-micro powder is preparing the application in cancer therapy drug, and described curcumin sub-micro powder in high pressure homogenizer, carries out high pressure homogenize by after curcumin supersound process, more obtained particle diameter is the sub-micro powder of 100-1000nm after lyophilization.
2. apply as claimed in claim 1, it is characterized in that, described curcumin sub-micro powder is prepared as follows:
Take curcumin 150-250mg, add ultrasonic 3-12min in 200-300mL water; Then join in high pressure homogenizer, respectively at the circulated under pressure 3-6 times of 200,400,600,800Bar, then at the circulated under pressure 30 ~ 40 times of 800 ~ 1500Bar; After discharging, discharging is freezing, then put into lyophilizing, obtain curcumin sub-micro powder.
3. apply as claimed in claim 1 or 2, it is characterized in that, described curcumin sub-micro Powder Particle Size is 100-200nm.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116763724A (en) * | 2023-07-20 | 2023-09-19 | 江苏创健医疗科技股份有限公司 | Preparation method of recombinant collagen hydrogel loaded with curcumin and application of recombinant collagen hydrogel in uterine cavity adhesion treatment |
-
2014
- 2014-10-09 CN CN201410527906.9A patent/CN105560193A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116763724A (en) * | 2023-07-20 | 2023-09-19 | 江苏创健医疗科技股份有限公司 | Preparation method of recombinant collagen hydrogel loaded with curcumin and application of recombinant collagen hydrogel in uterine cavity adhesion treatment |
| CN116763724B (en) * | 2023-07-20 | 2023-11-21 | 江苏创健医疗科技股份有限公司 | Preparation method of recombinant collagen hydrogel loaded with curcumin and application of recombinant collagen hydrogel in uterine cavity adhesion treatment |
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Application publication date: 20160511 |
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| WD01 | Invention patent application deemed withdrawn after publication |