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A Stable Irinotecan Liposome with Enhanced Antitumor Activity in a Range of Tumor Models

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机构： [1]Sichuan Kelun Pharmaceutical Research Institute Co. Ltd., Chengdu, 611130, China. [2]Hunan Kelun Pharmaceutical Institute Co. Ltd., Yueyang, 414199, China. [3]Department of Pharmacy, Chengdu Women's and Children's Central Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 611731, China. [4]Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd., Chengdu, 611130, China

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关键词： antitumor efficacy irinotecan liposome pharmacokinetics tissue distribution

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This study aimed to prepare a stable irinotecan liposome (CPT-11 liposome) and evaluate its antitumor efficacy in a range of tumor models.CPT-11 liposome was prepared with a Z-average particle size of 110 ~ 120 nm and high entrapment efficiency (> 95%) and had a good stability within 18 months. Then the antitumor efficacy was studied in human colon (Ls-174t), gastric (NCI-N87), pancreatic (BxPC-3) and small cell lung (NCI-H526) cancer xenograft models. The toxicity of high-dose CPT-11 liposome was also evaluated in Beagle dogs.The results showed that the anti-tumor effects of CPT-11 liposome were markedly superior (at least 10 times higher) to those of the CPT-11 injection group in all four xenograft models. The tissue distribution test in the Ls-174t model further demonstrated that the CPT-11 liposome could alter the plasma and tissue distribution of CPT-11, increase the exposure level of its active metabolite SN-38 in tumor, and ultimately improve antitumor efficiency. Meanwhile, CPT-11 liposome showed a much less toxicity than CPT-11 injection in beagle dogs.Overall, the CPT-11 liposome may be developed as a new clinical alternative for the cancer patients.© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.

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大类 | 3 区医学

小类 | 3 区化学：综合 3 区药学

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大类 | 3 区医学

小类 | 3 区化学：综合 3 区药学

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第一作者机构： [1]Sichuan Kelun Pharmaceutical Research Institute Co. Ltd., Chengdu, 611130, China. [2]Hunan Kelun Pharmaceutical Institute Co. Ltd., Yueyang, 414199, China.

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