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Development of a method to quantify total and free irinotecan and 7-ethyl-10-hydroxycamptothecin(SN-38) for pharmacokinetic and bio-distribution studies after administration of irinotecan liposomal formulation

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Asian Journal of Pharmaceutical Sciences 2019年第6期14卷 687-697页

作者： Wenqian Yang Zimeng Yang Jieru Liu Dan Liu Yongjun Wang Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China Key Laboratory of Structure-Based Drugs Design&Discovery of Ministry of Education Shenyang Pharmaceutical UniversityShenyang 110016China

In 2015,liposomal formulation of irinotecan(ONIVYDE)has been approved by FDA and widely applied in the treatment of pancreatic cancer.ONIVYDE is a novel liposome formulation,entrapping CPT-11 in the aqueous core of vesicles using a modified gradient loading method.Due to toxicity concerns,it is essential to explore a rapid and reliable method to effectively isolate and quantify the non-liposomal,namely,free CPT-11and total CPT-11 in plasma.This study focuses on separation of non-liposomal CPT-11,evaluation of the pharmacokinetics of free CPT-11 and total CPT-11 and bio-distribution after intravenous administration of CPT-11 liposome.Free CPT-11 in plasma was separated by solid-phase extraction(SPE).The amount of total CPT-11 and main metabolite 7-ethyl-10-hydroxycamptothecin(SN-38)in plasma was quantified by ultra-performance liquid chromatography–MS/MS.The calibration curves fitted well and lower limit of quantitation for SN-38,free CPT-11,total CPT-11 and CPT-11 in tissue and were 5 ng/ml,10 ng/ml,4.44 ng/ml and 25 ng/ml respectively.The recoveries,precision and accuracy of the method appear satisfactory.Using this method,the pharmacokinetics and bio-distribution of CPT-11 liposome formulation after an intravenous dose of 2.5 mg/kg were then investigated.

关键词： Irinotecan Liposome UPLC-MS-MS SPE Pharmacokinetics bio-distribution

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Toxicity and bio-distribution of carbon dots after single inhalation exposure in vivo

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Chinese Chemical Letters 2018年第6期29卷 895-898页

作者： Yue Yang Xiangling Ren Zhenning Sun Changhui Fu Tianlong Liu Xianwei Meng Zili Wang College of Animal Science and Technology Southwest University Chongqing 400716 China Laboratory of Controllable Preparation and Application of Nanomaterials CAS Key Laboratory of Cryogenics Technical Institute of Physics and Chemistry Chinese Academy of Sciences Beijing 100190 China College of Veterinary Medicine China Agricultural University Beijing 100193 China

Because of the advantages of excellent light stability, carbon dots（CDs） are considered to be a promising agent in the bio-marker application. Nevertheless, there are many unresolved issues with the toxicity of CDs in vitro and in vivo. In the study, CDs were synthesized by citric acid and ethylenediamine into deionized water, then the inhalation toxicity and bio-distribution of CDs in vivo were systematically assessed. The results showed that CDs caused animals death at higher dosages and induced injury in the lung and liver including inflammation and necrosis after single inhalation exposure at 5, 2 and 1 mg/kg dosages of the CDs. We also found that the injury increase with a dose-dependent and time-dependent manner. Fluorescent examination and TEM results showed that CDs mainly located at the lung and liver.And the fluorescent intensity increase with a time-dependent manner. This study provides a theoretical basis of the respiratory toxicity of CDs, and provides a basis for the use of CDs as a bio-marker.

关键词： Carbon dots Toxicity bio-distribution Inhalation Fluorescent intensity

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Effect of Kupffer cells depletion on ABC phenomenon induced by Kupffer cells-targeted liposomes

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Asian Journal of Pharmaceutical Sciences 2019年第4期14卷 455-464页

作者： Chaoyang Lai Cong Li Mengyang Liu Qiujun Qiu Xiang Luo Xinrong Liu Ling Hu Yihui Deng Yanzhi Song Shenyang Pharmaceutical University

Accelerated blood clearance(ABC) phenomenon is common in many PEGylated nanocarriers, whose mechanism has not been completely elucidated yet. In this study, the correlation between Kupffer cells(KCs) and ABC phenomenon has been studied by KCs-targeted liposomes inducing ABC phenomenon and KCs depletion. In other words, the 4-aminophenyl-α-D-mannopyranoside(APM) lipid derivative DSPE-PEG 2000-APM(DPM), and 4-aminophenyl-β-L-fucopyranoside(APF) lipid derivative DSPE-PEG 2000-APF(DPF) were conjugated and modified on alendronate sodium(AD) liposomes to specifically target and deplete KCs. The dualligand modified PEGylated liposomes(MFPL) showed stronger ability to damage KCs in vitro and in vivo, which also could indirectly illustrate that dual-ligand modification could better target KCs. Besides, the hepatic biodistribution and pharmacokinetics could directly prove that MFPL had a stronger targeting ability to KCs. In addition, in depletion rats, plasma concentration and splenic biodistribution of MFPL and PEGylated liposomes(PL) were significantly elevated and hepatic biodistribution was significantly reduced, which demonstrated that KCs played an important role on elimination of nanoparticles. What’s more, ABC phenomenon of the secondary injection of PL was stronger in KCs depletion rats than that in normal rats, which indicated that depletion of KCs prolonged the circulation of PL in the first injection repeatedly stimulating B-cells in the marginal region of the spleen and causing it to secrete more IgM antibodies. This could also illustrate that anti-PEG IgM takes up a major station compared with KCs. Most important of all, KCs-targeted liposomes could induce a stronger ABC phenomenon than PL in normal rats, which declared that based on the same IgM concentration, the more the KCs were stimulated, the stronger ABC phenomenon was induced. However, in depletion rats, this difference of ABC phenomenon between PL and MFPL could no more exist, further demonstrating that KCs could participate and play a certain role

关键词： Accelerated blood clearance (ABC) phenomenon Kupffer cells Depletion Liposomes bio-distribution

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bio-distribution research of a novel 188Re-TPPS4 in mice

Bio-distribution research of a novel 188Re-TPPS4 in mice

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首届全国分子核医学暨分子影像学学术交流会

作者： JIA Zhiyun, DENG Houfu, PU Manfey l.Dept. of Nuclear Medicine, West China Hospital. Sichuan University, Sichuan Chengdu 610041, China Institute of Nuclear Physics and Chemistry, China Academy of Engineering Physics, Sichuan Mianyang 621900

Objective To evaluate biological behaviors of a novel 188Re-TPPS4 porphyrin derivative in normal mice and tumor nude mice. Methods TPPS4 (meso-tetrakis4-sulfophenyl) porphyrin) was synthesized and characterized with improving methods. 188ReO4- was acquired from an 188W/188Re generator. The labelling of TPPS4 with 188ReO4- were optimized and achieved by varying reaction conditions. Neoplasm transplantation model of nude mice bearing melanoma or hepatoma were set up and divided randomly into 2 groups, each contains 5 animals;Normal Kunming mice were randomly divided into 10 groups, 10 animals in each group.188Re-TPPS4 were injected respectively into nude mice and Kunming mice via tail veins , SPECT imaging of the nude mice were carried out at different time and the mice were killed with radioactivity of major organs or tumour determined accordingly. Results It showed that the complexation yield was more than>98% as estimated by paper chromatography in acetone and in saline, with the specific activity up to 16.9GBq (mol.T3,4CPP)-1.188Re-TPPS4 did not significantly decrease during the period of 48h after the derivative formation with the preparation containing lOmg.L-1 Vc (Vitamin C) and via dilution ratio of 188Re-TPPS4 preparation within the range of 5 to 15 using physiological saline. It proved that Vc could increase stability of the derivative in vivo;and 188Re-TPPS4 had biological property of fast blood clearance(-90% 24h post-injection), certain uptake in kidney and liver, lower activity in other tissues and major renal clearance with its metabolites. At 8h post-injection, the uptake of 188Re-TPPS4 was up to 5.7% and 4.4%(%ID.g-1) in liver tumor and melanoma, respectively;tumour/blood and tumour/muscle ratios in hepatoma-bearing and melanomas-bearing mice were observed to be 3.8、26.0 and 2.6、21.0, respectively. This uptake in the tumour was retained until 24h post-injection with major activity showing renal clearance, no significant activity was present in other organs. The results of SPECT imaging confirmed th

关键词： 188Re porphyrin derivative bio-distribution mice tumor-bearing nude mice

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