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Synthesis and evaluation of cationic polymeric micelles as carriers of lumbrokinase for targeted thrombolysis

Asian Journal of Pharmaceutical Sciences 2019年第2期14卷 144-153页

作者： Yang Pan Xiahui Wang Zongning Yin Key Laboratory of Drug Targeting and Drug Delivery Systems West China School of Pharmacy Sichuan University

To achieve targeted thrombolysis, a targeted delivery system of lumbrokinase(LK) was constructed using RGDfk-conjugated hybrid micelles. Based on the specific affinity of RGDfk to glycoprotein complex of GP Ⅱ b/Ⅲ a expressed on the surface of membrane of activated platelet, LK loaded targeted micelles(LKTM) can be delivered to thrombus. The hybrid micelles were composed of polycaprolactone-block-poly(2-(dimethylamino) ethyl methacrylate)(PCL-PDMAEMA), methoxy polyethylene glycol-block-polycaprolactone(mPEG-PCL)and RGDfk conjugated polycaprolactone-block-polyethylene glycol(PCL-PEG-RGDfk). PCLPDMAEMA was synthesized via ring open polymerization(ROP) and atom transfer radical polymerization(ATRP). PCL-PEG-RGDfk was synthesized via ROP and carbodiimide chemistry. The prepared LKTM was characterized by dynamic light scattering(DLS) and transmission electron microscope(TEM). Colloidal stability assay showed the prepared LKTM was stable. Biocompatibility assay was performed to determine the safe concentration range of polymer. The assay of fluorescent distribution in vivo demonstrated that LKTM can be efficiently delivered to thrombi in vivo. Thrombolysis in vivo indicated the thrombolytic potency of LKTM was optimal in all groups. Notably, the laboratory mice treated with LKTM exhibited a significantly shorter tail bleeding time compared to those treated with LK or LK-loaded micelles without RGDfk, which suggested that the targeted delivery of LK using RGDfk-conjugated hybrid micelles effectively reduced the bleeding risk.

关键词： Targeted thrombolysis lumbrokinase Polymeric micelles ATRP ROP

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Preparation of pegylated lumbrokinase and an evaluation of its thrombolytic activity both in vitro and in vivo

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Acta Pharmaceutica Sinica B 2013年第2期3卷 123-129页

作者： Mingji Jin Wei Chen Wei Huang Long Rong Zhonggao Gao State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Beijing Key Laboratory of Drug Delivery Technology and Novel FormulationsInstitute of Materia MedicaChinese Academy of Medical SciencesBeijing 100050China Beijing University of Aeronautics and Astronautics Beijing 100191China

lumbrokinase(LK)is a group of serine proteases with strong fibrinolytic and thrombolytic *** clinical practice,LK can only be administered orally because of its antigenicity,iinmunogenicity and potential to produce anaphylactic reactions after ***,many useful drugs such as interferon,insulin,erythropoietin and interleukin have been modified with polyethylene glycol(PEG)to prepare injectable *** this study,LK was modified with methoxy PEG succinimidyl carbonate(mPEG-SC)with molecular weights of 5000,10,000 and 20,000 and the pegylatcd products were isolated and purified using the Akta protein purification *** extent of pegylation was detennined by *** activities of pegylatcd and unmodified LK were measured both in vitro against urokinase on fibrin plates and in vivo using a mouse carageenan black tail *** pegylation was obtainal using mPEG-SC_(5000) in a buffer pH 8.0 with a reaction time of 5 h,reaction temperature of 0℃ and LK:mPEG-SC molar ratio of 1:*** results show that mPEG modified LK has strong fibrinolytic and thrombolytic activities both in vitro and in *** is suggested that the pegylatcd LK is a promising injectable thrombolytic agent for the treatment of thrombotic diseases in clinical practice.

关键词： lumbrokinase Methoxy polyethylene glycol succinimidyl carbonate Pegylation Fibrinolytic activity

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高活性蚓激酶提取工艺研究

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宁夏科技 2001年第6期 44-45页

作者：王东鹏孙贵宝

1.蚓激酶原料药开发的意义1983年日本的美原恒(Mihara)等应用现代手段从蚯蚓蛋白粗提物中分离到多组具有纤溶酶活性的蛋白质,并首次命名为蚓激酶'(lumbrokinase)蚯蚓蛋白提取物蚓激酶无论静脉注射或口服给药,均具有溶栓作用,是目前最有... 详细信息

1.蚓激酶原料药开发的意义1983年日本的美原恒(Mihara)等应用现代手段从蚯蚓蛋白粗提物中分离到多组具有纤溶酶活性的蛋白质,并首次命名为蚓激酶'(lumbrokinase)蚯蚓蛋白提取物蚓激酶无论静脉注射或口服给药,均具有溶栓作用,是目前最有开发前景的纤溶药物之一.我院研制的蚓激酶冻干粉是配制蚓激酶胶囊的原料药,具有高活性、高纯度、低价格等特点,它富含蛋白质、氨基酸、微量元素、酶、激素等多种活性物质,可广泛应用于医药、食品、保健品、化妆品等行业.

关键词：高活性蚓激酶提取工艺 lumbrokinase

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