收稿日期: 2019-10-23
网络出版日期: 2020-07-07
Research progress on new formulations of albendazole against echinococcosis
Received date: 2019-10-23
Online published: 2020-07-07
抗棘球蚴病的首选药物为阿苯达唑,其新型制剂有固体分散体、脂质体、自微乳、前体胶束、微球、纳米药物等。其中阿苯达唑脂质体的研究起步较早,制备工艺较为成熟,在人类临床中已开始使用,但其载体修饰、药物贮存工艺等方面存在不足,还在不断改进中;阿苯达唑纳米药物的研究热度逐年上升,应用前景较为广泛;其他新型制剂尚处于实验室研究阶段。阿苯达唑的一些新型制剂明显提高了原药的靶向性与生物利用度,有望在减小原药不良反应和提高原药生物利用度与临床疗效等方面发挥重要作用。本文就阿苯达唑新型制剂近10年的研究进展作一综述。
杨林川 , 田易江 , 曾竺琳 , 曾仁权 . 阿苯达唑抗棘球蚴病新型制剂的研究进展[J]. 中国寄生虫学与寄生虫病杂志, 2020 , 38(3) : 383 -389 . DOI: 10.12140/j.issn.1000-7423.2020.03.020
Albendazole is the first-option drug for treatment of echinococcosis, with various new formulations including solid dispersion, liposomes, self-microemulsifying, precursor micelles, microspheres and nanodrug. Albendazole liposome formulations have been studied earlier, with its preparation technique being matured, and the formulation have commenced clinical application, however, the shortcomings in carrier modification and drug storage are being improved. Albendazole nanoformulation has wide application prospect, and the reaches in this regard have been growing year by year. Other new formulations of albendazole remain at the laboratory study stage. To be noted, some new albendazole formulations can largely improve the targeting property and bioavailability of the crude drug, and thus expectedly, the new formulations could play important role in reducing adverse effects and improving the bioavailability and therapeutic efficacy of the original crude drug. This review summarizes the researches in recent 10 years on new formulations of albendazole.
| [1] | Yan HB. Epidemic status of echinococcosis and research progress on prevention and control technology[J]. Vet Orientat, 2015,20(17):27-29. (in Chinese) |
| [1] | ( 闫鸿斌. 棘球蚴病的流行现状与防控技术研究进展[J]. 兽医导刊, 2015,20(17):27-29.) |
| [2] | Pawlowski Z, Eckert J, Vuitton DA, et al. Echinococcosis in humans: clinical aspects, diagnosis and treatment[M] //Eckert J, Gemmell MA, Meslin FX, et al. WHO/OIE Manual on Echinococcosis in Humans and Animals. Paris: Office International des épizooties, 2001: 104-106. |
| [3] | Morris DL, Jourdan JL, Pourgholami MH. Pilot study of albendazole in patients with advanced malignancy. Effect on serum tumor markers/high incidence of neutropenia[J]. Oncology, 2001,61(1):42-46. |
| [4] | Velík J, Baliharová V, Skálová L, et al. Stereospecific biotransformation of albendazole in mouflon and rat-isolated hepatocytes[J]. J Vet Pharmacol Ther, 2003,26(4):297-302. |
| [5] | Lanchote VL, Marques MP, Takayanagui OM, et al. Simultaneous determination of albendazole sulfoxide enantiomers and albendazole sulfone in plasma[J]. J Chromatogr B Biomed Sci Appl, 1998,709(2):273-279. |
| [6] | John H. Albendazole for the treatment of echinococcosis[J]. Fundam Clin Pharmacol, 2003,17(2):205-212. |
| [7] | Do?er E, H?kelek M, Do?er A. The use of albendazole sulphoxide as a scolicidal agent for the percutaneous treatment in hydatid cysts[J]. Parasitol Int, 1998,47:382. |
| [8] | Jiménez de los Santos CJ, Pérez-Martínez JI, Gómez-Pantoja ME, et al. Enhancement of albendazole dissolution properties using solid dispersions with Gelucire 50/13 and PEG 15000[J]. J Drug Deliv Sci Technol, 2017,42:261-272. |
| [9] | Dong CL, Liu YY, Wang TZ, et al. Preparation and analysis of albendazole solid dispersions[J]. Chin J Animal Vet Sci, 2014,45(6):1018-1023. (in Chinese) |
| [9] | ( 董春柳, 刘艳艳, 王天梓, 等. 阿苯达唑固体分散体的制备及分析[J]. 畜牧兽医学报, 2014,45(6):1018-1023.) |
| [10] | Dong CL, Liu YY, Wang TZ, et al. Preparation and analysis of albendazole solid dispersion using combined carrier[C]// Twelfth Symposium of Veterinary Pharmacology and Toxicology Branch of Chinese Society of Animal Husbandry and Veterinary Medicine, Zhengzhou: Chinese Society of Animal Husbandry and Veterinary Medicine, 2013. (in Chinese) |
| [10] | ( 董春柳, 刘艳艳, 王天梓, 等. 利用联合载体制备阿苯达唑固体分散体及分析[C]//中国畜牧兽医学会兽医药理毒理学分会第十二次学术讨论会论文集, 郑州, 2013. 郑州: 中国畜牧兽医学会, 2013.) |
| [11] | Dong CL. Preparation of albendazole solid dispersion and its pharmacokinetics in dogs[D]. Harbin: Northeast Agricultural University, 2015. (in Chinese) |
| [11] | ( 董春柳. 阿苯达唑固体分散体的制备及其在犬体内药代动力学研究[D]. 哈尔滨: 东北农业大学, 2015.) |
| [12] | Hengsawas Surasarang S, Keen JM, Huang SY, et al. Hot melt extrusion versus spray drying: hot melt extrusion degrades albendazole[J]. Drug Dev Ind Pharm, 2017,43(5):797-811. |
| [13] | Ullio Gamboa GV, Pensel PE, Elissondo MC, et al. Albendazole-lipid nanocapsules: optimization, characterization and chemoprophylactic efficacy in mice infected with Echinococcus granulosus[J]. Exp Parasitol, 2019,198:79-86. |
| [14] | Li J. Isolation and modification of phospholipids and their application in liposome pharmaceutical preparations[D]. Lanzhou: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, 2009. (in Chinese) |
| [14] | ( 李继. 磷脂的分离、 改性及其在脂质体药物制剂中的应用研究[D]. 兰州: 中国科学院兰州化学物理研究所, 2009.) |
| [15] | Nayar R, Hope MJ, Cullis PR. Generation of large unilamellar vesicles from long-chain saturated phosphatidylcholines by extrusion technique[J]. Biochim Et Biophys Acta BBA- Biomembr, 1989,986(2):200-206. |
| [16] | Jiao J, Jiang GP, Deng YH. Summary on liposomes for drug delivery in 50 years development course[J]. J Shenyang Pharm Univ, 2014,31(9):738-754. (in Chinese) |
| [16] | ( 焦姣, 蒋宫平, 邓意辉. 脂质体药物传递系统的50年发展历程概述[J]. 沈阳药科大学学报, 2014,31(9):738-754.) |
| [17] | Yang T. Research progress of new liposomes[J]. Her Med, 2009,28(3):336-338. (in Chinese) |
| [17] | ( 杨彤. 新型脂质体的研究进展[J]. 医药导报, 2009,28(3):336-338.) |
| [18] | Li HT, Bai L, Zhao JM, et al. Clinical observation of liposmal albendazole for treating complex liver alveolar echinococcosis[J]. J Xinjiang Med Univ, 2010,33(9):1089-1092. (in Chinese) |
| [18] | ( 李海涛, 白磊, 赵晋明, 等. 阿苯达唑脂质体治疗复杂肝泡型包虫病的初期临床观察[J]. 新疆医科大学学报, 2010,33(9):1089-1092.) |
| [19] | Li HT, Song T, Shao YM. Clinical efficacy evaluation for two types of albendazole in treating cystic echinococcosis by logistic regression equation[J]. Xinjiang Med J, 2015,45(3):281-285. (in Chinese) |
| [19] | ( 李海涛, 宋涛, 邵英梅, 等. Logistic回归方程对阿苯达唑两种剂型药物治疗囊性包虫病的临床疗效评价[J]. 新疆医学, 2015,45(3):281-285.) |
| [20] | Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems[J]. Eur J Pharm Sci, 2000,11(Suppl 2):S93-S98. |
| [21] | Kommuru TR, Gurley B, Khan MA, et al. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment[J]. Int J Pharm, 2001,212(2):233-246. |
| [22] | Zhang YJ, Wang KY, Fan LL, et al. Preparation and preliminary stability evaluation of albendazole self-microemulsifying drug delivery systems[J]. J Shihezi Univ Nat Sci, 2009,27(1):65-69. (in Chinese) |
| [22] | ( 张永军, 王科燕, 樊莲莲, 等. 阿苯达唑自微乳的研制及稳定性分析[J]. 石河子大学学报(自然科学版), 2009,27(1):65-69.) |
| [23] | Wei LH, Zhang YJ, Chen WJ, et al. Pharmacokinetics of self-microemulsifyingdrug delivery system albendazole in rat[J]. Agric Reclam Med, 2011,33(2):125-129. (in Chinese) |
| [23] | ( 魏丽红, 张永军, 陈卫军, 等. 阿苯达唑自微乳化释药系统大鼠体内药代动力学的研究[J]. 农垦医学, 2011,33(2):125-129.) |
| [24] | Wei LH, Zhang YJ, Zhu YT, et al. Tissue distribution of self-microemulsifying drug delivery system of albendazole in rats[J]. Chin J Hosp Pharm, 2011,31(16):1348-1351. (in Chinese) |
| [24] | ( 魏丽红, 张永军, 朱雅婷, 等. 阿苯达唑自微乳释药系统在大鼠体内组织分布[J]. 中国医院药学杂志, 2011,31(16):1348-1351.) |
| [25] | Zhang LN, Zhang YJ, Chen WJ, et al. Pharmacodynamic study of albendazole-SMEDDS against in vitro-culture of Echinococcus multilocularis metacestodes[J]. Chin J Hosp Pharm, 2012,32(16):1255-1259. (in Chinese) |
| [25] | ( 张丽娜, 张永军, 陈卫军, 等. 阿苯达唑自微乳体外抗泡球蚴药效学研究[J]. 中国医院药学杂志, 2012,32(16):1255-1259.) |
| [26] | Zhang YJ, Wei LH, Zhang LN, et al. Absorption mechanism of albendazole microemulsion across Caco-2 monolayer model[J]. Chin J Hosp Pharm, 2013,33(21):1757-1762. (in Chinese) |
| [26] | ( 张永军, 魏丽红, 张丽娜, 等. 阿苯达唑自微乳在Caco-2细胞上的吸收机制[J]. 中国医院药学杂志, 2013,33(21):1757-1762.) |
| [27] | Zheng Z, Hu JH. Physical and chemical principles of surfactants[M]. Guangzhou: South China University of Technology Press, 1995: 88-112. (in Chinese) |
| [27] | ( 郑忠, 胡纪华. 表面活性剂的物理化学原理[M]. 广州: 华南理工大学出版社, 1995: 88-112.) |
| [28] | Yasugi K, Nagasaki Y, Kato M, et al. Preparation and characterization of polymer micelles from poly(ethylene glycol)-poly(D, L-lactide) block copolymers as potential drug carrier[J]. J Control Release, 1999,62(1/2):89-100. |
| [29] | Kwon GS, Kataoka K. Block copolymer micelles as long-circulating drug vehicles[J]. Adv Drug Deliv Rev, 2012,64:237-245. |
| [30] | Allen C, Maysinger D, Eisenberg A. Nano-engineering block copolymer aggregates for drug delivery[J]. Colloids Surf B Biointerfaces, 1999,16(1-4):3-27. |
| [31] | Chen J. The preparation and study of oral premicelle albendazole[D]. Urumqi: Xinjiang Medical University, 2007. (in Chinese) |
| [31] | ( 陈迹. 阿苯达唑前体胶束的研制[D]. 乌鲁木齐: 新疆医科大学, 2007.) |
| [32] | Zhang GY, Yan Y, Ni J, et al. Studies on preparation and quality evaluation of albendazole loaded-chitosan microspheres[J]. Anti-Infect Pharm, 2012,9(2):108-114. (in Chinese) |
| [32] | ( 张光宇, 晏语, 倪进, 等. 阿苯达唑-壳聚糖微球的制备及其质量指标的考察[J]. 抗感染药学, 2012,9(2):108-114.) |
| [33] | Qiao L, Abulaihaiti ·M, Wang XC, et al. Variation of Th1/Th2 cytokines in sera from mice infected with alveolar echinococcosis as an indication of the curative effects of treatment with albendazole chitosan microspheres[J]. J Pathog Biol, 2014,9(12):1079-1083. (in Chinese) |
| [33] | ( 乔雷, 阿卜来海提·麦提色依提, 王新春, 等. ABZ-CS-MPs治疗泡球蚴小鼠血清Th1/Th2细胞因子的变化及意义[J]. 中国病原生物学杂志, 2014,9(12):1079-1083.) |
| [34] | Qiao L. A preliminary study on the efficacy and immunological mechanism of albendazole chitosan microspheres in anti-foaming mice[D]. Shihezi: Shihezi University, 2015. (in Chinese) |
| [34] | ( 乔雷. 阿苯达唑壳聚糖微球抗泡球蚴小鼠疗效及免疫学机制初步探讨[D]. 石河子: 石河子大学, 2015.) |
| [35] | Abulaihaiti M, Wu XW, Qiao L, et al. Efficacy of albendazole-chitosan microsphere-based treatment for alveolar echinococcosis in mice[J]. PLoS Negl Trop Dis, 2015,9(9):e0003950. |
| [36] | Nishioka Y, Yoshino H. Lymphatic targeting with nanoparticulate system[J]. Adv Drug Deliv Rev, 2001,47(1):55-64. |
| [37] | Gao HJ, Chen B, Zhang HB, et al. Pharmacokinetics and liver targeting of lyophilized albendazole nanoliposomes in rats[J]. Chin J Hosp Pharm, 2017,37(8):702-706. (in Chinese) |
| [37] | ( 高惠静, 陈蓓, 张海波, 等. 阿苯达唑纳米脂质体冻干粉在大鼠体内药动学及肝靶向研究[J]. 中国医院药学杂志, 2017,37(8):702-706.) |
| [38] | Zhang XN, Zhang Q, Wen H, et al. Studies on preparation of albendazole polybutycyanocrylate nanoparticles and its stability[J]. Chin Pharm J, 2003,38(5):357-359. (in Chinese) |
| [38] | ( 张学农, 张强, 温浩, 等. 乳化聚合法制备阿苯达唑聚氰基丙烯酸酯纳米球的方法比较及稳定性考察[J]. 中国药学杂志, 2003,38(5):357-359.) |
| [39] | Paredes AJ, Litterio N, Dib A, et al. A nanocrystal-based formulation improves the pharmacokinetic performance and therapeutic response of albendazole in dogs[J]. J Pharm Pharmacol, 2018,70(1):51-58. |
| [40] | Paredes AJ, Bruni SS, Allemandi D, et al. Albendazole nanocrystals with improved pharmacokinetic performance in mice[J]. Ther Deliv, 2018,9(2):89-97. |
| [41] | Ma YF, Wang JH, Chen J, et al. Pharmacokinetics study of albendazole nano-powder in rats[J]. China Pharm, 2016,27(34):4797-4799. (in Chinese) |
| [41] | ( 马运芳, 王建华, 陈迹, 等. 阿苯达唑纳米微粉在大鼠体内的药动学研究[J]. 中国药房, 2016,27(34):4797-4799.) |
| [42] | Zhang MH. Experimental study of albendazole nanoparticles via the portal vein administration in the treatment of Echinococcus multilocularis in liver[D]. Urumqi: Xinjiang Medical University, 2011. (in Chinese) |
| [42] | ( 张明星. 经门静脉灌注阿苯达唑纳米微球治疗肝泡状棘球蚴病的实验研究[D]. 乌鲁木齐: 新疆医科大学, 2011.) |
| [43] | Fan YX. Experimental study of albendazole microspheres via the hepatic artery infusion on hepatic alveolar echinococcosis in rats[D]. Urumqi: Xinjiang Medical University, 2012. (in Chinese) |
| [43] | ( 樊玉祥. 经肝动脉灌注阿苯达唑纳米微球治疗大鼠肝泡状棘球蚴病的实验研究[D]. 乌鲁木齐: 新疆医科大学, 2012.) |
| [44] | Fakhar M, Chabra A, Rahimi-Esboei B, et al. In vitro protoscolicidal effects of fungal chitosan isolated from Penicillium waksmanii and Penicillium citrinum[J]. J Parasit Dis, 2015,39(2):162-167. |
| [45] | Song C, Fei ZH. Application of polymer materials in nano drug delivery system[J]. J Chifeng Univ Nat Sci Ed, 2008,24(1):126-128. (in Chinese) |
| [45] | ( 宋春风, 费志宏. 高分子材料在纳米给药系统中的应用[J]. 赤峰学院学报(自然科学版), 2008,24(1):126-128.) |
| [46] | Pensel P, Paredes A, Albani CM, et al. Albendazole nanocrystals in experimental alveolar echinococcosis: Enhanced chemoprophylactic and clinical efficacy in infected mice[J]. Vet Parasitol, 2018,251:78-84. |
| [47] | Chen J, Ma YF, Wang JH. On technology of Using liquid phase precipitation method to make albendazole nano powder[J]. J Xinjiang Med Univ, 2014,37(1):40-43. (in Chinese) |
| [47] | ( 陈迹, 马运芳, 王建华. 阿苯达唑纳米微粉制备工艺研究[J]. 新疆医科大学学报, 2014,37(1):40-43.) |
| [48] | Naseri M, Akbarzadeh A, Spotin A, et al. Scolicidal and apoptotic activities of albendazole sulfoxide and albendazole sulfoxide-loaded PLGA-PEG as a novel nanopolymeric particle against Echinococcus granulosus protoscoleces[J]. Parasitol Res, 2016,115(12):4595-4603. |
| [49] | Torabi N, Dobakhti F, Faghihzadeh S, et al. In vitro and in vivo effects of chitosan-praziquantel and chitosan-albendazole nanoparticles on Echinococcus granulosus metacestodes[J]. Parasitol Res, 2018,117(7):2015-2023. |
| [50] | Wang XQ, Gu ZL, Yuan MY, et al. Preparation of albendazole-chitosan nanoparticles and its characteristics in vivo and in vitro[J]. Chin J New Drugs, 2013,22(7):755-761. (in Chinese) |
| [50] | ( 王晓青, 顾宗林, 袁明月, 等. 阿苯达唑-壳聚糖纳米粒的制备及体内外评价[J]. 中国新药杂志, 2013(7):755-761.) |
| [51] | Ren JR, Ma YF, Wang JH, et al. Optimization of freeze-drying technology of albendazole nanosuspension[J]. China Pharm, 2015,26(25):3575-3577. (in Chinese) |
| [51] | ( 任洁如, 马运芳, 王建华, 等. 阿苯达唑纳米混悬液的冻干工艺优化[J]. 中国药房, 2015,26(25):3575-3577.) |
| [52] | Ren JR. Studies on the freeze-drying technology, bioavailability and preliminary toxicity of albendazole nano powder[D]. Urumqi: Xinjiang Medical University, 2016. (in Chinese) |
| [52] | ( 任洁如. 阿苯达唑纳米微粉的冻干工艺、生物利用度及毒性初步研究[D]. 乌鲁木齐: 新疆医科大学, 2016.) |
/
| 〈 |
|
〉 |