环孢素A微乳巴布膏眼贴的制备及体外透皮实验  

Preparation and in vitro transdermal permeation of cyclosporin A microemulsion papua cream eye patch

作　　者：陈敏[1] 许丽疆[1] 翁景宁[2] 上官晓辉[3] 严俊[4] 黄金棋[5,6,7] 陈丹娜 Chen Min;Xu Li-jiang;Weng Jing-ning;Shangguan Xiao-hui;Yan Jun;Huang Jin-qi;Chen Dan-na(Department of Ophthalmology,Affiliated Hospital(Group)of Putian University,Putian 351100,Fujian Province,China;Department of Ophthalmology,Union Hospital of Fujian Medical University,Fuzhou 350000,Fujian Province,China;Department of Blood Rheumatology,Longyan First Hospital of Fujian Medical University,Longyan 364000,Fujian Province,China;Department of Blood Reheumatology,Affiliated Hospital(Group)of Putian University,Putian 351100,Fujian Province,China;Department of Hematology,Affiliated Hospital(Group)of Putian University,Putian 351100,Fujian Province,China;Translational Medicine Center,School of Pharmacy,Xiamen University,Xiamen 361102,Fujian Province,China;Cell and Genetic Engineering Institute,Putian University,Putian 351100,Fujian Province,China)

机构地区：[1]莆田学院附属医院,眼科,福建省莆田市351100 [2]福建医科大学附属协和医院眼科,福建省福州市350000 [3]福建医科大学附属龙岩市第一医院血液风湿科,福建省龙岩市364000 [4]莆田学院附属医院,血液风湿科,福建省莆田市351100 [5]莆田学院附属医院,血液内科,福建省莆田市351100 [6]厦门大学药学院转化医学中心,福建省厦门市361102 [7]莆田学院细胞与基因工程研究所,福建省莆田市351100

出　　处：《中国组织工程研究》2018年第10期1553-1558,共6页Chinese Journal of Tissue Engineering Research

基　　金：莆田学院校级课题(2014034);莆田市科技局课题(2014S06(2))

摘　　要：背景:免疫性眼病如甲亢性突眼、葡萄膜炎等疾病严重危害患者的眼健康,是眼科的常见病和疑难病,目前最常见的治疗方法为口服激素和免疫抑制剂,疗效不佳、反复发作、预后差同时全身不良反应很大。此类疾病多有淋巴细胞直接或间接参与。尝试把免疫抑制剂制作成巴布膏眼贴,通过局部外用使药物进入体内,利用环孢素A微乳的淋巴靶向性能,使环孢素A作用在睑周淋巴结,从而达到治疗或控制睑周淋巴结参与反应的免疫性眼病。这种方法为局部外用,不用全身用药,针对性强,药物剂量小,如果治疗效果好,可以有效治疗免疫性眼病并规避原有药物全身应用及长期应用的不良反应。目的:制备环孢素A微乳巴布膏眼贴,研究环孢素A微乳巴布膏眼贴体外透皮吸收特性。方法:将环孢素A微乳与聚丙烯酸钠、聚乙烯醇、聚乙烯吡络烷酮、明胶、桃胶、羧甲基纤维素钠、羟丙基纤维素等的水溶性高分子材料混合物以1 mg∶1 mL的比例充分混匀,涂布于无纺布上制备成巴布膏。Franz扩散池法测定该巴布膏在ICR小鼠腹部皮肤的通透性。高效液相色谱分析法检测环孢素A浓度,并进行皮肤刺激性和过敏性实验。结果与结论:实验成功制备了粘性适宜、透气透水性能良好、敷贴舒适、无皮肤刺激性和过敏反应的环孢素A微乳巴布膏,环孢素A含量为10 mg/片,质量浓度为1 g/L。环孢素A微乳透皮的浓度随着时间的增加而增加,具有较好的透皮效果。证实将环孢素A微乳制备成巴布膏眼贴是可行的。其在透皮性能、黏附能力、皮肤舒适方面表现良好。BACKGROUND:Immune eye diseases such as hyperthyroidism exophthalmos and uveitis seriously endanger the eye health of patients,which are common and difficult eye diseases.Current treatments for these diseases include oral administration of hormones and immunosuppressive agents,with poor efficacy,recurrent attacks and poor prognosis.Meanwhile,these treatments can induce systemic adverse reactions.Lymphocytes are directly or indirectly involved in these diseases.Therefore,we try to make papua eye patch carrying immunosuppressant,and deliver the drug through the topical use.Cyclosporin A microemulsion targeting lymphocytes can treat or control palpebral lymph nodes involved in the immune eye diseases.It is a topical method rather than the systemic medication,which is targeted and has small doses of drugs.If possible,this treatment can effectively treat immune eye diseases and avoid systemic drug adverse reactions and long-term adverse reactions induced by original drugs.OBJECTIVE:To study the preparation of cyclosporin A microemulsion papua cream eye patch,and its transdermal absorption characteristics in vitro.METHODS:Cyclosporine A microemulsion was fully mixed with water-soluble polymer materials at a ratio of 1 mg:1 mL,including sodium polyacrylate,polyvinyl alcohol,polyvinylpyrrolidone,gelatin,peach gum,sodium carboxymethylcellulose,hydroxypropylcellulose,and then coated onto the non-woven fabric to prepare Babu cream.Permeability of the Babu cream on the abdominal skin of ICR mice was determined by Franz diffusion cell method.High-performance liquid chromatography was used to detect the concentration of cyclosporine A,and skin irritation and anaphylaxis were also measured.RESULTS AND CONCLUSION:Cyclosporin A microemulsion papua cream eye patch was successfully prepared with appropriate viscosity,good permeability,good permeability,comfortable application,no skin irritation and allergic reaction.The content of cyclosporine A was 10 mg/tablet,and the concentration was 1 g/L.The concentration of cyclosporine A mic

关 键 词：环孢素A微乳 巴布膏 眼贴 工艺研究 体外透皮 免疫性眼病 甲状腺相关眼病 局部给药 生物材料 亲环素类 免疫抑制剂 免疫毒素类 组织工程 

分 类 号：R318[医药卫生—生物医学工程]