本文關(guān)鍵詞：姜黃素超微粉體的制備及生物活性評價　出處：《中南林業(yè)科技大學(xué)》2015年碩士論文　論文類型：學(xué)位論文

  更多相關(guān)文章： 姜黃素 高壓均質(zhì) 超臨界二氧化碳反溶劑 超微粉體 理化性質(zhì) 體外抗腫瘤

【摘要】：姜黃素是從姜科姜黃屬植物根莖中提取出來的一種天然色素,具有抗病毒、抗菌、抗腫瘤、抗炎、抗氧化、降血脂等有廣泛的藥理活性。但姜黃素本身難溶于水,其水溶液在中性至堿性條件下不穩(wěn)定,代謝過快,極大地限制了其生物活性。因此,有必要增加姜黃素在水中的溶解度、提高其體外溶出速率。國內(nèi)外學(xué)者研究并改進(jìn)了多種姜黃素的新劑型,減小姜黃素顆粒的粒徑是實現(xiàn)上述目的技術(shù)手段之一。本論文采用高壓均質(zhì)技術(shù)和超臨界二氧化碳反溶劑技術(shù)制備了姜黃素超微粉體,優(yōu)化了姜黃素超微粉體的制備工藝；對姜黃素超微粉體進(jìn)行了理化性質(zhì)、化學(xué)結(jié)構(gòu)、體外溶出度測試與表征,并開展了姜黃素超微粉體的體外抗腫瘤活性研究。(1)建立姜黃素含量分析方法采用高效液相色譜分析姜黃素含量,方法學(xué)考察結(jié)果表明：姜黃素在濃度范圍1～60μg/ml線性關(guān)系良好,含量測定方法的日內(nèi)和日間精密度、穩(wěn)定性、以及回收率均符合方法學(xué)考察的要求。(2)高壓均質(zhì)法制備姜黃素超微粉體采用高壓均質(zhì)法制備姜黃素納米混懸劑,優(yōu)化了姜黃素超微粉體(粉體A)的制備工藝；結(jié)果表明,均值壓力1000 bar,循環(huán)次數(shù)30次,姜黃素納米混懸劑的平均粒徑為(171.0±8.56)nm,一致性系數(shù)為(0.6940±0.05)；凍干保護(hù)劑適宜工藝條件為：甘露醇濃度為4%(W/W),加入方式為內(nèi)加法,預(yù)凍溫度為-20℃,預(yù)凍時間為24h。IR,UV, XRD和HPLC顯示,姜黃素超微粉體化學(xué)結(jié)構(gòu)未見改變,與姜黃素原粉相比,姜黃素超微粉體在水中的溶解度有大幅度提高；姜黃素超微粉體外溶出速率也明顯提高,120 min時,溶出度已達(dá)80%。高壓均質(zhì)法是一種適用于姜黃素超微粉體的制備方法。(3)超臨界二氧化碳反溶劑制備姜黃素超微粉體采用超臨界二氧化碳反溶劑法制備姜黃素超微粉體(粉體B),以丙酮為溶劑,以微粒粒徑為指標(biāo),考察了結(jié)晶壓力,結(jié)晶溫度,溶液流速,溶液濃度等工藝參數(shù)。確定適宜工藝條件為：結(jié)晶壓力30 Mpa,結(jié)晶溫度53℃,溶液濃度12.5mg/mL,溶液流速9 mL/min,所制備的姜黃素顆粒平均粒徑為450～550 nm。IR,UV表明姜黃素超微粉體化學(xué)結(jié)構(gòu)未見改變；XRD表明姜黃素超微粉體結(jié)晶化程度低于姜黃素原粉,結(jié)晶程度越低,水溶性越好；TG/DTG和DSC表明超微化后姜黃素穩(wěn)定性沒有改變,但姜黃素超微粉體熔化所需能量低于姜黃素原粉。水溶性實驗表明,姜黃素超微粉體在水中的溶解度隨顆粒粒徑的減小而增大。(4)姜黃素超微粉體體外抗腫瘤活性研究采用MTT方法,研究了姜黃素超微粉體(粉體A和粉體B)對HepG2、HCT116兩種細(xì)胞生長的抑制作用。結(jié)果顯示：HepG2、HCT116細(xì)胞生長明顯受抑制,隨著姜黃素超微粉體濃度的增加其抑制作用增強(qiáng)。姜黃素超微粉體粉體A和粉體B以及姜黃素原粉對HepG2細(xì)胞的IC50值分別為11.95μg/mL、12.76μg/mL和24.14μg/mL;對HCT116的IC50值分別為10.87μg/mL、11.24μg/mL和24.14μg/mL。研究結(jié)果表明減小姜黃素顆粒的粒徑,能增強(qiáng)姜黃素的體外抗腫瘤活性,因而也可進(jìn)一步提高其生物利用度。
[Abstract]:Curcumin is a kind of natural pigment extracted from Curcuma in antiviral, antibacterial, antitumor, anti-inflammatory, antioxidant, hypolipidemic and has extensive pharmacological activity. But curcumin is insoluble in water, its water solution is not stable in neutral to alkaline conditions, rapid metabolism, great to limit its biological activity. Therefore, it is necessary to increase the solubility of curcumin, improve the dissolution rate. Domestic and foreign scholars and many new forms of curcumin improved, curcumin reduced particle size is one of the means of achieving these goals. In this paper, and the supercritical carbon dioxide anti solvent preparation technology the curcumin ultrafine powder by high pressure homogenization technology, optimize the preparation process of curcumin ultrafine powder; ultrafine powder of curcumin on physicochemical properties, chemical structure, test and characterization of in vitro dissolution, and The superfine powder of curcumin antitumor activity in vitro. (1) analysis method was established by HPLC analysis of the content of curcumin content of curcumin, the methodological study results show that curcumin in the concentration range of 1 ~ 60 g/ml good linear relationship, a method for the determination of the intra day and inter day precision, stability and recovery. Rate are consistent with the methodological study. (2) high pressure homogenization preparation of curcumin ultrafine powders prepared by the high pressure homogenization method of curcumin nano suspension, optimization of the curcumin superfine powder (A powder) in the preparation process; the results show that the mean pressure of 1000 bar, 30 cycles, the average particle of curcumin nanoparticles suspension of the diameter of (171 + 8.56) nm, consistency coefficient (0.6940 + 0.05); cryoprotector suitable conditions: the mannitol concentration was 4% (W/W), joined the way in law, pre freezing temperature of -20, pre Freezing time is 24h.IR, UV, XRD and HPLC showed that curcumin ultrafine powder chemical structure was not changed, compared with the original powder of curcumin, curcumin ultrafine powder has greatly improved solubility in water; rate also obviously improve the dissolution of curcumin powder in vitro, 120 min, dissolution rate has reached 80%. high pressure homogenization method is a kind of method is suitable for preparation of curcumin ultrafine powder. (3) carbon dioxide supercritical anti solvent preparation of supercritical carbon dioxide anti solvent preparation of curcumin ultrafine powder using curcumin superfine powder (B powder), using acetone as the solvent, with the particle size as indexes, the influences of crystallization pressure, crystallization temperature, solution flow rate, solution concentration and other parameters. To determine the optimum conditions for crystallization pressure of 30 Mpa, the crystallization temperature of 53 DEG C, the concentration of 12.5mg/mL solution, the flow rate of 9 mL/min, the particles prepared by curcumin with an average diameter of 450 ~ 550 nm.IR UV, show that curcumin ultrafine powder did not alter the chemical structure of XRD ultrafine powder; curcumin crystallization degree is lower than that of curcumin powder, the crystallization degree is low, the water soluble TG/DTG and DSC showed better; after ultramicronization stability of curcumin has not changed, but the curcumin ultrafine powder required for melting energy less than the original powder water soluble curcumin. Experiments show that curcumin ultrafine powder increases the solubility in water increases with the decrease of particle size. (4) using curcumin superfine powder in vitro antitumor activity of MTT and curcumin superfine powder (A powder and B powder) on HepG2 growth inhibition effect of HCT116 two cells. The results showed that HepG2, HCT116 cell growth was significantly inhibited, with the increase of the concentration of curcumin powder is enhanced. The inhibitory effect of curcumin IC50 superfine powder, A powder and B powder and powder of curcumin on HepG2 cells Values were 11.95 g/mL, 12.76 g/mL and 24.14 g/mL; the HCT116 IC50 values were 10.87 g/mL, 11.24 g/mL and 24.14 g/mL. the results of the study show that curcumin decreased the particle size, can enhance the antitumor activity of curcumin in vitro, which can further improve its bioavailability.

【學(xué)位授予單位】：中南林業(yè)科技大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2015
【分類號】：TQ28;TB383.3

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