龙血竭总黄酮纳米粒的制备工艺研究及其表征
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摘要
目的:制备龙血竭总黄酮纳米粒(Dragon’s blood total flavonoid nanoparticles,DBF-NPs),并优化其处方和制备工艺。方法:结合HPLC与葡聚糖凝胶柱层析法,构建样品包封率测定方法;以包封率,粒径及外观为综合指标,在单因素试验的基础上进行正交试验设计确定最佳处方及工艺。结果:所优选葡聚糖凝胶柱层析条件为:柱规格10 mm×450 mm,洗脱剂为去离子水,上样量1 mL(含龙血竭总黄酮1 mg),流速(6±1)mL·h~(-1);薄膜超声法为最佳制备方法;最优处方为:有机相与水相体积比1∶1,Tween 80浓度为1%,PDLLACOOR 0.7%,龙血竭总黄酮0.1%;制得纳米粒包封率和平均粒径分别为81%±2.6%、(203±12)nm。结论:通过工艺优化,制得DBF-NPs包封率较高,粒径合适,稳定性良好。
OBJECTIVE To prepare Dragon's blood total flavonoid nanoparticles(DBF-NPs) and optimize its formulation and preparation process. METHODS The best formulation and preparation condition were optimized by orthogonal test based on single-factor test and encapsulation rate, particle size and appearance were considered as comprehensive index. The encapsulation rate determination method were established by HPLC combined with Sephadex G-50 column chromatography. RESULTS The optimum conditions of Sephadex column chromatography were as follows: column size 1 cm×45 cm, elution solvent: deionized water, sample volume 1 ml, flow rate(6±1)mL·h~(-1). Thin-film ultrasonic method is the best preparation method and the optimal prescription was: volume ratio of organic phase to aqueous phase 1∶1, Tween 80 1%, PDLLACOOR 0.7%, Dragon's blood total flavonoid 0.1%. The encapsulation rate and the average particle size were 81%±2.6% and(203±12)nm, respectively. CONCLUSION With optimization of the formulation and preparation conditions, the prepared DBF-NPs had high encapsulation rate and good stability.
OBJECTIVE To prepare Dragon's blood total flavonoid nanoparticles(DBF-NPs) and optimize its formulation and preparation process. METHODS The best formulation and preparation condition were optimized by orthogonal test based on single-factor test and encapsulation rate, particle size and appearance were considered as comprehensive index. The encapsulation rate determination method were established by HPLC combined with Sephadex G-50 column chromatography. RESULTS The optimum conditions of Sephadex column chromatography were as follows: column size 1 cm×45 cm, elution solvent: deionized water, sample volume 1 ml, flow rate(6±1)mL·h~(-1). Thin-film ultrasonic method is the best preparation method and the optimal prescription was: volume ratio of organic phase to aqueous phase 1∶1, Tween 80 1%, PDLLACOOR 0.7%, Dragon's blood total flavonoid 0.1%. The encapsulation rate and the average particle size were 81%±2.6% and(203±12)nm, respectively. CONCLUSION With optimization of the formulation and preparation conditions, the prepared DBF-NPs had high encapsulation rate and good stability.
引文
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[2] Chen S,Wu SC,Zeng Y,et al.Anti-inflammatory and Analgesic Effects of Total Flavone Extracted from Dragon’s Blood and Its Analgesic Mechanism Exploration[J].Lishizhen Med Mater Med Res(时珍国医国药),2013,24(5):1030-1032.
[3] Chen FF,Zhen YN,Du WJ,et al.Effect of Sanguis Draxonis Capsules on chronic stasis syndrome[J].Drug Eval Res(药物评价研究),2015,38(3):274-278.
[4] Nie L,Cheng DY,Zhu GY,et al.Effect of the Dragon’s blood on TGF-β 1 mRNA and collagen I expression in lungs of rats with pulmonary fibrosis[J].Hebei J Tradit Chin Med.(河北中医),2010,32(7):1071-1074.
[5] Chen S,Wu SC,Zeng Y,et al.Anti-inflammatory and Analgesic Effects of Total Flavone Extracted from Dragon’s Blood and Its Analgesic Mechanism Exploration[J].Lishizhen Med Mater Med Res(时珍国医国药),2013,24(5):1030-1032.
[6] Liu P,Jiang ZJ,Zhang JX,et al.Optimization on preparation of glycyrrhetinic acid modified PEG-pep-PEI-PLGA nanoparticles loaded with hydroxycamptothecin by central composite design-response surface method[J].J Guangdong Pharm Univ(广东药科大学学报),2018,34(1):1-6.
[7] Ye F,Lou XF,Du YZ.Determination of Loureirin A in Solid Lipid Nanoparticles Encapsulating Resina Draconis by HPLC[J].Chin J Mod Appl Pharm(中国现代应用药学),2013,30(1):69-72.
[8] Chen JP,Fang YC,Shen L.Process Research and Characterization of Ursolic Acid-PLGA Nanoparticles[J].J Chin Med Mater(中药材),2016,39(10):2315-2317.
[9] Qiu YX,Shi L,Liu YL,et al.Determination of Drug Content and Entrapment Efficiency of Ezetimibe and Simvastation Nanoparticles by HPLC[J].Contemp Chem Ind(当代化工),2017,46(4):613-615.
[10] Lin HX,Dai DB,Ding D,et al.Simultaneous determination of content and entrapment efficiency of doxorubixin and curcumin loaded nanoparticles by HPLC[J].Zhejiang Med J(浙江医学),2015,37(10):836-839.
[11] Zhang SC,Chen K,Liu LY.Preparation and evaluation of self-assembled lecithin/chitosan nanoparticles for berberine hydrochloride delivery[J].J Tianjin Agric Univ (天津农学院学报),2018,25(1):59-63.
[12] Richa J,Krishna KT,Raghvenda G.Role of Solid Lipid Nanoparticles in Augmentation of Carcinoma Therapy:An in-vitro Study[J].People’s J Sci Res,2017,10(2):70.
[13] Wu XY,Shi L,Zhou TT,et al.Research on Determination Method for Encapsulation Efficiency of Ciclesonide Nanoparticles[J].Chin Pharm(中国药业),2013,22(12):100-102.
[14] Tan Q,Liu WD,Guo CY et al.Preparation and evaluation of quercetin-loaded lecithin-chitosan nanoparticles for topical delivery[J].Int J Nanomed,2011,6:1621-1630.
[15] ChenR,Wu QZ,Ping QN.Current Progressin Microparticles for Pulmonary Drug Delivery[J].Prog Pharm Sci (药学进展),2008,32(11):499-504.
[16] Liu NN,Jiang FS,Yu TT,et al.Preparation of curcumin-(oleic acid)2 loaded mPEG5000-PLGA nanoparticles by modified solvent evaporation method[J].Chin Tradit Herbal Drugs(中草药),2013,44(16):2223-2229.
[17] Liu MX,Ma L,Liu YQ,et al.Preparatio n and Characteriztio n of Biodegradable Poly(lactic acid) Nano particles[J].Chem World(化学世界),2003,2 (10):78-80.
[18] Guo JY,Wang P,Hu M,et al.Excipient Formula Research of Nicotinate-Curcumin nanoparticles Prepared by Film Ultrasonic Method[J].Chin Pharm J(中国药学杂志),2017,52(06):462-467.
[19] Zhang L.The development and quality research on Mometasone furoate nasal spray[D].Hubei University of Chinese Medicine(湖北中医药大学),2014.
[20] Ding YN,Kang B,Wang J.Preparation and in vitro Evaluation of Budesonide Inhalation Nanosuspension[J].Chin J Pharm (中国心血管杂志),2017,48(8):1131-1135.