姜黄素-明胶纳米复合物改善药物水溶性和稳定性的研究
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摘要
[目的]制备明胶-姜黄素纳米复合物,考察复合物对姜黄素水溶性和稳定性的影响。[方法]采用碱溶酸中和的方法,以明胶为载体,制备姜黄素-明胶纳米复合物,对复合物的粒径、溶解度、物理稳定性等进行测定;以姜黄素水溶液作为对照,考察复合物中姜黄素在模拟胃肠道p H环境、光照、紫外线、高温条件下的稳定性。[结果]姜黄素-明胶纳米复合物的平均粒径为117.2 nm,PDI为0.112;具有较好的物理稳定性;随着姜黄素浓度的增加载药量升高;复合物中姜黄素的水中溶解度相比原药增加1 500倍;光谱学研究表明姜黄素与明胶疏水区域通过相互作用结合;在模拟胃肠道p H、光照、紫外线、高温条件下,姜黄素-明胶纳米复合物中姜黄素的降解远低于姜黄素原药,明胶与姜黄素的复合可提高姜黄素化学稳定性。[结论]采用碱溶酸中和法制备的姜黄素-明胶纳米复合物可显著提高姜黄素的水溶性和稳定性。
[Objective]Nanocomplexes of curcumin with gelatin were prepared, and the improvement on the solubility and stability of curcumin were investigated.[Methods]Curcumin-gelatin nanocomplexes was prepared using gelatin as a carrier,curcumin was deprotonated and dissolved under alkaline conditions, then complexation with gelatin after acidification. The particle size, solubility and physical stability of the nanocomplexes were detected. The chemical stability of the nanocomplex in simulated gastrointestinal p H environment, light, ultraviolet radiation and high temperature were investigated and curcumin in water was used as a control.[Results]The average particle size, polydispersion parameter of the nanocomplex were 117. 2 nm,0.112, respectively. Nanocomplex has good physical stability. Drug-loading rate of nanocomplex was increased while the concentration of curcumin increased. The solubility of curcumin in water was enhanced by the nanocomplex about 1 500 folds compared to the original curcumin. Spectroscopic studies indicated the binding between gelatin and curcumin; The degradation rate of curcumin-gelatin nanocomplexes was significantly lower than original curcumin under different conditions.The complexation of gelatin and curcumin can improve the chemical stability of curcumin.[Conclusion]The solubility and stability of curcumin can be improvement by nanocomplexation with gelatin with the p H-driven method.
[Objective]Nanocomplexes of curcumin with gelatin were prepared, and the improvement on the solubility and stability of curcumin were investigated.[Methods]Curcumin-gelatin nanocomplexes was prepared using gelatin as a carrier,curcumin was deprotonated and dissolved under alkaline conditions, then complexation with gelatin after acidification. The particle size, solubility and physical stability of the nanocomplexes were detected. The chemical stability of the nanocomplex in simulated gastrointestinal p H environment, light, ultraviolet radiation and high temperature were investigated and curcumin in water was used as a control.[Results]The average particle size, polydispersion parameter of the nanocomplex were 117. 2 nm,0.112, respectively. Nanocomplex has good physical stability. Drug-loading rate of nanocomplex was increased while the concentration of curcumin increased. The solubility of curcumin in water was enhanced by the nanocomplex about 1 500 folds compared to the original curcumin. Spectroscopic studies indicated the binding between gelatin and curcumin; The degradation rate of curcumin-gelatin nanocomplexes was significantly lower than original curcumin under different conditions.The complexation of gelatin and curcumin can improve the chemical stability of curcumin.[Conclusion]The solubility and stability of curcumin can be improvement by nanocomplexation with gelatin with the p H-driven method.
引文
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[15]王雪梅,陈利华,施文婷.姜黄素类化合物的光稳定性研究.[J].安徽大学学报(自然科学版),2012,36(3):73-78.
[2]SIVIERO A,GALLO E,MAGGINI V. Curcumin,a golden spice with a low bioavailability.[J]. Journal of Herbal Medicine,2015,5(5):57-70.
[3]MAHMOOD K,ZIA K M,ZUBER M,et al. Recent developments in curcumin and curcumin based polymeric materials for biomedical applications:A review. International Journal of Biological Macromolecules.[J]. Int J Biol Macromol,2015(81):877-890.
[4]TARHINI M,GREIGEGERGES H,ELAISSARI A. Protein-based nanoparticles:From preparation to encapsulation of active molecules.[J]. International Journal of Pharmaceutics,2017,522(1-2):172.
[5] ELZOGHBY A O. Gelatin-based nanoparticles as drug and gene delivery systems:reviewing three decades of research.[J]. Journal of Controlled Release,2013,172(3):1075-1091.
[6] CHANG C,WANG T,HU Q. Pectin coating improves physicochemical properties of caseinate/zein nanoparticles as oral delivery vehicles for curcumin.[J]. Food Hydrocolloids,2017(70):143-151.
[7]WANG Y H,WANG J M,YANG X Q. Amphiphilic zein hydrolysate as a novel nano-delivery vehicle for curcumin.[J]. Food&Function,2015,6(8):2636-2645.
[8]CHENG C,CHENG C,PENG S. Improved bioavailability of curcumin in liposomes prepared using a p H-driven,organic solvent-free,easily scalable process.[J]. Rsc Advances,2017,7(42):25978-25986.
[9]FENG J,WU S,WANG H. Improved bioavailability of curcumin in ovalbumin-dextran nanogels prepared by Maillard reaction[J]. Journal of Functional Foods,2016(27):55-68.
[10]PRIYADARAINI K I. Photochemistry and photobiology of curcumin:Studies from organic solutions,bio-mimetics and living cells.[J]. Journal of Photochemistry&Photobiology C Photochemistry Reviews,2009,10(2):81–95.
[11]SHEN X C,LIU X Y,LIANG H. Spectroscopic studies of interaction between bovine hemoglobin and Ag nanoparticles[J]. Acta Chimica Sinica,2006,64(6):469-474.
[12]CHEN L,BAI G,YANG S. Encapsulation of curcumin in recombinant human H-chain ferritin increases its water-solubility and stability.[J]. Food Research International,2014,62(8):1147-1153.
[13]LAKOWICZ J R,WEBER G. Quenching of protein fluorescence by oxygen. Detection of structural fluctuations in proteins on the nanosecond time scale[J]. Biochemistry,1973,12(21):4171-4179.
[14]TAPAL A,TIKU P K. Complexation of curcumin with soy protein isolate and its implications on solubility and stability of curcumin.[J]. Food Chemistry,2012,130(4):960-965.
[15]王雪梅,陈利华,施文婷.姜黄素类化合物的光稳定性研究.[J].安徽大学学报(自然科学版),2012,36(3):73-78.