白及多糖凝胶对黄藤素纳米柔性脂质体性质的影响
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摘要
以天然高分子白及多糖(BSP)为凝胶基质,制备了载黄藤素纳米柔性脂质体(1-FNL)凝胶剂,并考察BSP凝胶对脂质体性质(包封率、体外释放、平均粒径、?电位、酸度值和过氧化值)和人阴道上皮细胞(HVEC)毒性的影响。结果表明,BSP浓度为0.5%~2%时能增大1-FNL的包封率,最大值为83.7%,继续增加BSP浓度至2.5%,包封率反而下降。BSP浓度在0.5%~2.5%范围内能减慢凝胶剂中1-FNL的体外释药速率,且具有浓度依赖性。相较于1-FNL,1-FNL凝胶在30 d内的平均粒径和?电位变化程度小,提示BSP与1-FNL相容性较好。同时,在4、25和40℃贮存30 d期间,凝胶剂的酸度值和过氧化值均低于1-FNL,提示BSP提高了1-FNL的化学稳定性。MTT法及碘化丙啶(PI)荧光染色法表明,BSP能降低1-FNL对HVEC的毒性作用,并减弱1-FNL对细胞膜完整性的影响。
The gels containing palmatine flexible nano-liposomes(1-FNL) with Bletilla striata polysaccharide(BSP) as the matrix were prepared.The effect of BSP gels on properties of 1-FNL(encapsulation efficiency,in vitro release,average particle size,? potential,acidity value and peroxide value) and cytotoxicity against human vaginal epithelial cells(HVEC) were investigated.The results showed that the encapsulation efficiency increased with the increasing of BSP concentration in the range of 0.5%—2%,and the maximum value was 83.7%.But the encapsulation efficiency obviously decreased when the BSP concentration increased to 2.5%.The in vitro drug release from the gels with different BSP concentrations(from 0.5% to 2.5%) decreased in a concentration-dependent manner.The changes of average particle size and ? potential of the gels within 30 d were smaller than those of 1-FNL,indicating a good compatibility of BSP with 1-FNL.Meanwhile,the acidity values and peroxide values of the gels stored at 4,25 and 40 ℃for 30 d were lower than those of 1-FNL,which indicated the chemical stability of 1-FNL was also improved by BSP.The results of MTT assay and propidium iodide(PI) staining showed that BSP could weaken both the cell cytotoxicity and destruction of cell membrane integrity of 1-FNL against HVEC.
The gels containing palmatine flexible nano-liposomes(1-FNL) with Bletilla striata polysaccharide(BSP) as the matrix were prepared.The effect of BSP gels on properties of 1-FNL(encapsulation efficiency,in vitro release,average particle size,? potential,acidity value and peroxide value) and cytotoxicity against human vaginal epithelial cells(HVEC) were investigated.The results showed that the encapsulation efficiency increased with the increasing of BSP concentration in the range of 0.5%—2%,and the maximum value was 83.7%.But the encapsulation efficiency obviously decreased when the BSP concentration increased to 2.5%.The in vitro drug release from the gels with different BSP concentrations(from 0.5% to 2.5%) decreased in a concentration-dependent manner.The changes of average particle size and ? potential of the gels within 30 d were smaller than those of 1-FNL,indicating a good compatibility of BSP with 1-FNL.Meanwhile,the acidity values and peroxide values of the gels stored at 4,25 and 40 ℃for 30 d were lower than those of 1-FNL,which indicated the chemical stability of 1-FNL was also improved by BSP.The results of MTT assay and propidium iodide(PI) staining showed that BSP could weaken both the cell cytotoxicity and destruction of cell membrane integrity of 1-FNL against HVEC.
引文
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[20]Lee TW,Kim JC,Hwang SJ.Hydrogel patches containing triclosan for acne treatment[J].Eur J Pharm Biopharm,2003,56(3):407—412.
[21]雷震,常明泉,陈黎,等.白及的临床应用研究进展[J].中国药师,2013,16(8):1240—1242.
[2]Li W,Zhou Y,Zhao N,et al.Pharmacokinetic behavior and effi ciency of acetylcholinesterase inhibition in rat brain after intranasal administration of galanthamine hydrobromide loaded flexible liposomes[J].Environ Toxicol Pharmacol,2012,34(2):272—279.
[3]Kim A,Lee EH,Choi SH,et al.In vitro and in vivo transfection efficiency of a novel ultradeformable cationic liposome[J].Biomaterials,2004,25(2):305—313.
[4]Gupta PN,Mishra V,Singh P,et al.Tetanus toxoid-loaded transfersomes for topical immunization[J].J Pharm Pharmacol,2005,57(3):295—301.
[5]Godin B,Touitou E.Mechanism of bacitracin permeation enhancement through the skin and cellular membranes from an ethosomal carrier[J].J Controlled Release,2004,94(2/3):365—379.
[6]Elsayed MM,Abdallah OY,Naggar VF,et al.Lipid vesicles for skin delivery of drugs:reviewing three decades of research[J].Int J Pharm,2007,332(1-2):1—16.
[7]Elsayed MM,Abdallah OY,Naggar VF,et al.Deformable liposomes and ethosomes:mechanism of enhanced skin delivery[J].Int J Pharm,2006,322(1-2):60—66.
[8]Paveli?Z,Skalko-Basnet N,Filipovi?-Grci?J,et al.Development and in vitro evaluation of a liposomal vaginal delivery system for acyclovir[J].J Controlled Release,2005,106(1-2):34—43.
[9]程安媛.新型胃粘附材料——白芨多糖的制备及膜粘附性体内外评价[D].重庆:重庆医科大学硕士学位论文,2008.
[10]徐花荣.白芨多糖的提取分离及其在中药水凝胶巴布剂型中的应用[D].西安:西北大学硕士学位论文,2006.
[11]李玉先.阿莫西林白芨胶生物粘附缓释胶囊的研制[D].重庆:重庆医科大学硕士学位论文,2005.
[12]孙维彤,黄桂华,叶杰胜,等.鱼精蛋白凝聚法测定脂质体和纳米脂质体包封率[J].中国药学杂志,2006,41(22):1716—1720.
[13]李伟泽,赵宁,闫菁华,等.阴道用苦参柔性脂质体泡沫气雾剂的制备研究[J].中成药,2012,34(1):42—45.
[14]石富成,周景春,张慧岩,等.测定大豆磷脂酸值的方法改进[J].药物分析杂志,1997,17(6):414—415.
[15]孙珊珊,王慧云,陆爱华.全反式维甲酸前体脂质体的制备及磷脂过氧化值的测定[J].中国当代医药,2010,17(14):114.
[16]孙达锋,史劲松,张卫明,等.白及多糖胶研究进展[J].食品科学,2009,30(3):296—298.
[17]梅正平,王俊杰,王刚,等.“瑰及”乳膏中白及不同提取部位活血化瘀作用的实验研究[J].中国医药导报,2010,12(7):1207—1208.
[18]Verma DD,Verma S,Blume G,et al.Liposomes increase skin penetration of entrapped and non-entrapped hydrophilic substances into human skin:a skin penetration and confocal laser scanning microscopy study[J].Eur J Pharm Biopharm,2003,55(3):271—277.
[19]Barichello JM,Handa H,Kisyuku M,et al.Inducing effect of liposomalization on the transdermal delivery of hydrocortisone:creation of a drug supersaturated state[J].J Controlled Release,2006,115(1):94—102.
[20]Lee TW,Kim JC,Hwang SJ.Hydrogel patches containing triclosan for acne treatment[J].Eur J Pharm Biopharm,2003,56(3):407—412.
[21]雷震,常明泉,陈黎,等.白及的临床应用研究进展[J].中国药师,2013,16(8):1240—1242.