体外透皮递送SPE的CMC/CS/Ca^(2+)复合水凝胶及其抗氧化活性研究  

Study on CMC/CS/Ca2+Composite Hydrogel for Transdermal Delivery of SPE in vitro and Its Antioxidant Activity

作　　者：叶君[1] 刘禄莹 黄卓生 熊犍[3] YE Jun;LIU Luying;HUANG Zhuosheng;XIONG Jian(State Key Laboratory of Pulp and Paper Engineering,South China University of Technology,Guangzhou 510640,Guangdong,China;Yiruian Food Ingredients Co.,Ltd.,Shanghai 201600,China;School of Food Science and Engineering,South China University of Technology,Guangzhou 510640,Guangdong,China)

机构地区：[1]华南理工大学制浆造纸工程国家重点实验室,广东广州510640 [2]宜瑞安食品配料有限公司,上海201600 [3]华南理工大学食品科学与工程学院,广东广州510640

出　　处：《华南理工大学学报（自然科学版）》2023年第1期51-60,共10页Journal of South China University of Technology(Natural Science Edition)

基　　金：国家自然科学基金资助项目(22178128,31270617)。

摘　　要：像大豆肽(SPE)这样的肽类物质在药物靶向治疗和诊断等方面有着重要作用,但它们难以抵抗胃部极低的pH环境以及离子障碍,因此难以通过口服的方式进行递送。透皮递送系统可避免胃液的障碍,将药物递送到血液中。文中通过冻融循环成功制备了负载SPE的羧甲基纤维素/阳离子淀粉/Ca^(2+)(CMC/CS/Ca^(2+))复合水凝胶,以克服透皮递送过程中皮肤角质层对水溶性SPE渗透的障碍。颗粒电荷分析(PCD)、傅里叶变换红外光谱(FT-IR)以及流变结果表明,CMC、CS及Ca^(2+)之间产生了化学和物理交联作用,形成了稳定的复合水凝胶,且SPE与CS、Ca^(2+)间产生的相互作用使其力学性能可满足透皮递送的要求;扫描电子显微镜(SEM)和比表面积测试(BET)结果表明,这些复合水凝胶内部具有多孔洞的三维网络结构。复合水凝胶的含水率均高于95.63%,在25℃下持续25 min后其保湿率仍在97.34%以上,所有复合水凝胶均在120 min内快速溶胀,在720 min时平衡溶胀分数可达636.23%,说明该复合水凝胶对水具有高度的亲和性,这是SPE透皮递送效率提高的根本原因。体外释放结果表明,SPE从复合水凝胶中的释放为溶胀控释型,且其最大DPPH自由基和ABTS自由基清除率分别可达47.07%和72.16%。3种复合水凝胶中SPE的单位面积累积渗透量分别为0.55、0.70和0.60 mg/cm^(2),其累积渗透百分比分别达到84.13%、92.93%和92.57%。复合水凝胶的外观以及pH值、耐热性、耐寒性均符合QB/T 2872—2017的规定。文中制备的复合水凝胶不仅有望在透皮递送肽及蛋白质类药物上得以应用,在皮肤抗氧化护理方面也具有潜在的应用价值。Peptides,such as soybean peptide(SPE),play an important part in drugs targeted therapy and diagnosis.However,their intolerance for the extremely low pH and ionic barriers of the stomach makes them hard to be delivered orally.Transdermal delivery system can deliver drugs to the blood avoiding the obstacles of the gastric.In this paper,carboxymethyl cellulose/cationic starch/Ca^(2+)(CMC/CS/Ca^(2+))composite hydrogel was successfully prepared by freeze-thaw cycle,and it can overcome the barrier of penetration of water-soluble SPE in the stratum corneum during transdermal delivery.The results of particle charge detector(PCD),Fourier transform infrared spectroscopy(FT-IR)and rheology show that chemical and physical cross-linking occurs among CMC,CS and Ca^(2+),forming a stable hydrogel.Moreover,the interaction among SPE,CS and Ca^(2+)makes its mechanical properties meet the requirements of transdermal delivery.The results of scanning electron microscope(SEM)and specific surface area measurement(BET)illustrate that there is a porous 3D network structure in those composite hydrogels.The moisture content of the composite hydrogel is higher than 95.63%and remains above 97.34%after 25 min at 25℃.All composite hydrogels swell rapidly within 120 min,and the equilibrium swelling fraction can reach up to 636.23%at720 min.Moreover,it is also indicated that the composite hydrogels have high affinity for water,which is the fundamental reason for improving the transdermal delivery efficiency of SPE.The results of in vitro release show that the release type of SPE releasing from hydrogel belongs to swelling controlled release type,and the maximum scavenging rates of DPPH radical and ABTS radical are 47.07%and 72.16%,respectively.The cumulative permeation per unit area of SPE is 0.55,0.70 and 0.60 mg/cm~2,separately,and the cumulative penetration percentage is84.13%,92.93%and 92.57%,respectively.The appearance and pH value,thermostability and cold endurance of the hydrogel all meet the standards of QB/T 2872—2017.Therefore,these

关 键 词：羧甲基纤维素 阳离子淀粉 大豆肽 透皮递送 抗氧化活性 

分 类 号：O636.1[理学—高分子化学]