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A novel long-circulating DOX liposome: formulation and pharmacokinetics studies.

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机构: [1]College of Pharmacy and Chemistry, Dali University, Dali 671000, Yunnan Province, People’s Republic ofChina [2]Institute of Regulatory Science for Medical Devices, National Engineering Research Center for Biomaterials,Sichuan University, No. 29, Wangjiang Road, Chengdu 610064, P. R. China [3]Mianyang Hospitalof T.C.M., No 14, Fucheng Road, Miangyang, Sichuan, P.R. China [4]Beibei Traditional Chinese MedicalHospital, No 380, Jiangjun Road, Chongqing, 400700, P.R. China
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关键词: DOX liposome drug loading entrapment efficiency Kolliphor HS15 particle size pharmacokinetics

摘要:
Doxorubicin (DOX) is a leading chemotherapeutic in cancer treatment, because of its high potency and broad spectrum. Liposomal doxorubicin (Doxil®) is the first FDA-approved PEG-liposomes of DOX for the treatment of over 600.000 cancer patients, and it can overcome doxorubicin-induced cardiomyopathy and other side effects and prolong life span. The addition of MPEG2000-DSPE could elevate the total cost of the cancer treatment.We intended to prepare a novel DOX liposome that was prepared with inexpensive materials egg yolk lecithin and Kolliphor HS15, thus allowing it to be much cheaper for clinical application.DOX liposomes were prepared using the combination of thin-film dispersion ultrasonic method and ammonium sulfate gradient method and the factors that influenced formulation quality were optimized. After formulation, particle size, entrapment efficiency, drug loading, stability, and pharmacokinetics were determined.DOX liposomes was near-spherical morphology with the average size of 90 nm and polydispersity index (PDI) of less than 0.30. The drug loading was up to 7.5%, and the entrapment efficiency was over 80%. The pharmacokinetic studies showed that free DOX could be easily removed and the blood concentration of free DOX group was significantly lower than that of DOX liposomes, which indicated that the novel DOX liposome had a certain sustained-release effect.In summary, DOX liposome is economical and easy-prepared with prolonged circulation time.

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第一作者机构: [1]College of Pharmacy and Chemistry, Dali University, Dali 671000, Yunnan Province, People’s Republic ofChina [2]Institute of Regulatory Science for Medical Devices, National Engineering Research Center for Biomaterials,Sichuan University, No. 29, Wangjiang Road, Chengdu 610064, P. R. China
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通讯作者:
通讯机构: [2]Institute of Regulatory Science for Medical Devices, National Engineering Research Center for Biomaterials,Sichuan University, No. 29, Wangjiang Road, Chengdu 610064, P. R. China [4]Beibei Traditional Chinese MedicalHospital, No 380, Jiangjun Road, Chongqing, 400700, P.R. China [*1]Institute of Regulatory Science for Medical Devices, National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, P.R. China and Beibei Traditional Chinese Medical Hospital, Chongqing, P. R. China
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