麦冬多糖多囊脂质体的制备及其抗2型糖尿病活性的研究
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摘要
目的:制备麦冬多糖多囊脂质体,并考察其对2型糖尿病模型小鼠的治疗效果。方法:以复乳化溶剂蒸发法制备麦冬多糖多囊脂质体,Box-Behnken响应面设计法优化处方,评价麦冬多糖多囊脂质体的外观形态、粒径、Zeta电位、包封率、储存稳定性等特性。采用高脂饲料联合链脲佐菌素注射建立2型糖尿病小鼠模型,造模小鼠随机分组灌胃给药,28天后测定血糖指数。结果:优选的制备处方组成为麦冬多糖24 mg,维生素E 5 mg,二油酰基卵磷脂(DOPC) 20 mg,磷脂酰甘油(DPPG) 4 mg,胆固醇16 mg,三油酸甘油酯10 mg,吐温80 10 mg。制得的麦冬多糖多囊脂质体多室结构清晰可见,包封率较高(81. 24±2. 11)%,平均粒径为15. 37μm,Zeta电位为(38. 38±3. 26) m V,稳定性良好;麦冬多糖多囊脂质体的抗2型糖尿病活性优于麦冬多糖(P <0. 05)。结论:麦冬多糖多囊脂质体能有效包载麦冬多糖,增强其抗2型糖尿病活性,可作为新型天然多糖的药物传递系统。
To prepare ophiopogon japonicus polysaccharide( OJP)-loaded multivesicular liposomes and to evaluate its therapeutic effect on type 2 diabetic mice. Methods: The multivesicular liposomes were prepared by multiple emulsion method and optimized by Box-Behnken response surface design. The morphology,particle size,Zeta potential,encapsulation efficiency,stability and anti-type 2 diabetes effects of the liposomes were evaluated. The models of type 2 diabetic mice was established by high fat diet combined with Streptozotocin injection. The model mice were administrated with the corresponding medication. Blood glucose indexes were determined after 28 days. Results: The optimized prescription were OJP 24 mg,vitamin E 5 mg,DOPC20 mg,DPPG 4 mg,cholesterol 16 mg,triolein 10 mg and Tween 80 10 mg. The prepared liposomes were multi-chamber structure,high entrapment efficiency( 81. 24 ± 2. 11) %,suitable mean particle diameter(15. 37 μm) and stable Zeta potential(38. 38 ± 3. 26) m V. Furthermore,the anti-type 2 diabetes effects of multivesicular liposomes were superior to OJP. Conclusion: The multivesicular liposomes could deliver OJP and enhance the anti-type 2 diabetes activities effectively,which can serve as a novel drug delivery system for natural polysaccharides.
To prepare ophiopogon japonicus polysaccharide( OJP)-loaded multivesicular liposomes and to evaluate its therapeutic effect on type 2 diabetic mice. Methods: The multivesicular liposomes were prepared by multiple emulsion method and optimized by Box-Behnken response surface design. The morphology,particle size,Zeta potential,encapsulation efficiency,stability and anti-type 2 diabetes effects of the liposomes were evaluated. The models of type 2 diabetic mice was established by high fat diet combined with Streptozotocin injection. The model mice were administrated with the corresponding medication. Blood glucose indexes were determined after 28 days. Results: The optimized prescription were OJP 24 mg,vitamin E 5 mg,DOPC20 mg,DPPG 4 mg,cholesterol 16 mg,triolein 10 mg and Tween 80 10 mg. The prepared liposomes were multi-chamber structure,high entrapment efficiency( 81. 24 ± 2. 11) %,suitable mean particle diameter(15. 37 μm) and stable Zeta potential(38. 38 ± 3. 26) m V. Furthermore,the anti-type 2 diabetes effects of multivesicular liposomes were superior to OJP. Conclusion: The multivesicular liposomes could deliver OJP and enhance the anti-type 2 diabetes activities effectively,which can serve as a novel drug delivery system for natural polysaccharides.
引文
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[6]张然然,孙艳冬,赵源,等.处方及工艺因素对多囊脂质体质量影响的研究进展[J].中国医药工业杂志,2016,47(7):929-933.
[7] LI H,AN J H,PARK J S,et al. Multivesicular liposomes for oral delivery of recombinant human epidermal growth factor[J]. Archives of Pharmacal Research,2005,28(8):988-994.
[8] JAIN S K,JAIN R K,CHOURASIA M K,et al. Design and development of multivesicular liposomal depot delivery system for controlled systemic delivery of acyclovir sodium[J]. Aaps Pharmscitech,2005,6(1):E35-E41.
[9]赵玉萍,陈晓旺,沈鹏伟. Box-Behnken实验设计及响应面分析优化锰过氧化物酶培养基条件[J].食品工业科技,2013,34(4):207-211.
[2]张小平,孙润广,王小梅,等.化学修饰水提麦冬多糖WPOJ的抗肿瘤活性研究[J].食品与生物技术学报,2014,33(4):368-373.
[3] XU D,YI F,ZHOU Y,et al. Active components of polysaccharide of Ophiopogon Japonicus on acute myocardial ischemia[J]. Chinese Traditional Patent Medicine,2004:26.
[4] FAN S R,WANG J J,MAO Y G,et al. Characterization and antioxidant properties of OJP2,a polysaccharide isolated from Ophiopogon japonicus[J]. Advances in Bioscience&Biotechnology,2015,6(8):517-525.
[5]曹爽,付绍智,王永多,等.麦冬多糖药理作用研究进展[J].安徽农业科学,2015,43(28):63.
[6]张然然,孙艳冬,赵源,等.处方及工艺因素对多囊脂质体质量影响的研究进展[J].中国医药工业杂志,2016,47(7):929-933.
[7] LI H,AN J H,PARK J S,et al. Multivesicular liposomes for oral delivery of recombinant human epidermal growth factor[J]. Archives of Pharmacal Research,2005,28(8):988-994.
[8] JAIN S K,JAIN R K,CHOURASIA M K,et al. Design and development of multivesicular liposomal depot delivery system for controlled systemic delivery of acyclovir sodium[J]. Aaps Pharmscitech,2005,6(1):E35-E41.
[9]赵玉萍,陈晓旺,沈鹏伟. Box-Behnken实验设计及响应面分析优化锰过氧化物酶培养基条件[J].食品工业科技,2013,34(4):207-211.