Box-Behnken效应面法优化隐丹参酮纳米粒制备工艺
|
摘要
目的:制备隐丹参酮聚乙二醇-聚乳酸/羟基乙酸共聚物(PEG-PLGA)载药纳米粒,并优化其处方和制备工艺。方法:采用纳米沉淀法制备隐丹参酮PEG-PLGA载药纳米粒。分别以PEG-PLGA在有机相中质量浓度、隐丹参酮和PEG-PLGA质量比、水相和有机相体积比为考察因素,以包封率为考察指标,采用Box-Behnken效应面法优化纳米粒的处方和工艺。结果:隐丹参酮PEG-PLGA纳米粒的最佳处方工艺条件为:PEG-PLGA在有机相中质量浓度为13.78mg·mL-1,隐丹参酮和PEG-PLGA的质量比0.9∶10,水相和有机相的体积比为9.66∶1,平均包封率为70.40%。结论:Box-Behnken效应面法简便可行,可用于优化隐丹参酮载药纳米粒的制备工艺。
Objective: To prepare cryptotanshinone PEG-PLGA nanoparticles and to optimize the prescription and preparation of cryptotanshinone PEG-PLGA nanoparticles. Methods: The nanoprecipitation method was employed to prepare cryptotanshinone PEG-PLGA nanoparticles. The influence factors included the concentration of PEG-PLGA in organic phase, the mass ratio of PEG-PLGA to drug and the volume ratio of water phase to organic phase. The drug loading process was optimized by Box-Behnken response surface method with the entrapment efficiency as the evaluation parameters. Results: The optimal formulation and process parameters were as follows: the concentration of PEG-PLGA in organic phase was13.78 mg·mL-1, the mass ratio of cryptotanshinone to PEG-PLGA was 0.9∶10,and the volume ratio of water phase to organic phase was 9.66∶1. The average encapsulation efficiency was70.40 %. Conclusion: The Box-Behnken response surface method is simple and feasible and can be used for drug loading process optimization of cryptotanshinone PEG-PLGA nanoparticles.
Objective: To prepare cryptotanshinone PEG-PLGA nanoparticles and to optimize the prescription and preparation of cryptotanshinone PEG-PLGA nanoparticles. Methods: The nanoprecipitation method was employed to prepare cryptotanshinone PEG-PLGA nanoparticles. The influence factors included the concentration of PEG-PLGA in organic phase, the mass ratio of PEG-PLGA to drug and the volume ratio of water phase to organic phase. The drug loading process was optimized by Box-Behnken response surface method with the entrapment efficiency as the evaluation parameters. Results: The optimal formulation and process parameters were as follows: the concentration of PEG-PLGA in organic phase was13.78 mg·mL-1, the mass ratio of cryptotanshinone to PEG-PLGA was 0.9∶10,and the volume ratio of water phase to organic phase was 9.66∶1. The average encapsulation efficiency was70.40 %. Conclusion: The Box-Behnken response surface method is simple and feasible and can be used for drug loading process optimization of cryptotanshinone PEG-PLGA nanoparticles.
引文
[7]Garinot M,Virginie Fiévez,Pourcelle V,et al.PEGylated PLGA-based nanoparticles targeting M cells for oral vaccination[J].Journal of Controlled Release,2007,120(3):195-204.
[8]陈刚,李玉民,刘涛,等.PEG-PLGA纳米颗粒载体药物靶向治疗肿瘤的研究进展[J].国际外科学杂志,2010,37(6):417-419.
[9]李艳,罗成,周婕.纳米沉淀法及其在纳米载体领域的研究进展[J].中国生物医学工程学报,2017,36(4):483-489.
[10]李莎,曾迎春,张志荣.醋酸地塞米松PEG-PLGA纳米粒的制备及表征[J].华西药学杂志,2017,32(2):124-126.
[11]王婴,李木生,吴瑞婵,等.星点设计-效应面法优化青藤碱聚乳酸-羟基乙酸纳米粒的制备工艺[J].中药新药与临床药理,2017(2):232-237.
[12]柳阳,朱艳华,孙佳琳,等.聚乙二醇-聚乳酸-羟基乙酸嵌段共聚物载药纳米粒制备方法的研究进展[J].中国药房,2017,28(16):2274-2276.
[13]邵红霞,奉建芳,龙晓英.脂质体包封率的测定方法[J].中南药学,2009,7(3):212-215,6.
[1]曾金,张志荣,缪萍,等.隐丹参酮的药理作用研究进展[J].中成药,2015,37(6):1309-1313.
[2]叶因涛,王晨,宋晓坤,等.隐丹参酮对肝癌H22荷瘤小鼠放射增敏作用的影响[J].中国癌症杂志,2014,24(1):29-34.
[3]邓凤春,杨钰,赵红晔,等.隐丹参酮抑制人胃癌SGC-7901细胞增殖的实验研究[J].中外医疗,2014,35(5):49-50.
[4]叶欢,阮君山,王少明.隐丹参酮抑制A549细胞复发转移的机制[J].海峡药学,2014,26(12):238-241.
[5]王加茹,徐宛婷,朴仙姬,等.隐丹参酮诱导人食管癌HCE-4细胞凋亡的机制[J].肿瘤防治研究,2018,45(8):533-539.
[6]Zhang J.A Mechanistic Study of the Intestinal Absorption of Cryptotanshinone,the Major Active Constituent of Salvia miltiorrhiza[J].Journal of Pharmacology and Experimental Therapeutics,2006,317(3):1285-1294.
[8]陈刚,李玉民,刘涛,等.PEG-PLGA纳米颗粒载体药物靶向治疗肿瘤的研究进展[J].国际外科学杂志,2010,37(6):417-419.
[9]李艳,罗成,周婕.纳米沉淀法及其在纳米载体领域的研究进展[J].中国生物医学工程学报,2017,36(4):483-489.
[10]李莎,曾迎春,张志荣.醋酸地塞米松PEG-PLGA纳米粒的制备及表征[J].华西药学杂志,2017,32(2):124-126.
[11]王婴,李木生,吴瑞婵,等.星点设计-效应面法优化青藤碱聚乳酸-羟基乙酸纳米粒的制备工艺[J].中药新药与临床药理,2017(2):232-237.
[12]柳阳,朱艳华,孙佳琳,等.聚乙二醇-聚乳酸-羟基乙酸嵌段共聚物载药纳米粒制备方法的研究进展[J].中国药房,2017,28(16):2274-2276.
[13]邵红霞,奉建芳,龙晓英.脂质体包封率的测定方法[J].中南药学,2009,7(3):212-215,6.
[1]曾金,张志荣,缪萍,等.隐丹参酮的药理作用研究进展[J].中成药,2015,37(6):1309-1313.
[2]叶因涛,王晨,宋晓坤,等.隐丹参酮对肝癌H22荷瘤小鼠放射增敏作用的影响[J].中国癌症杂志,2014,24(1):29-34.
[3]邓凤春,杨钰,赵红晔,等.隐丹参酮抑制人胃癌SGC-7901细胞增殖的实验研究[J].中外医疗,2014,35(5):49-50.
[4]叶欢,阮君山,王少明.隐丹参酮抑制A549细胞复发转移的机制[J].海峡药学,2014,26(12):238-241.
[5]王加茹,徐宛婷,朴仙姬,等.隐丹参酮诱导人食管癌HCE-4细胞凋亡的机制[J].肿瘤防治研究,2018,45(8):533-539.
[6]Zhang J.A Mechanistic Study of the Intestinal Absorption of Cryptotanshinone,the Major Active Constituent of Salvia miltiorrhiza[J].Journal of Pharmacology and Experimental Therapeutics,2006,317(3):1285-1294.