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Hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration in mice

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Acta Pharmacologica Sinica 2004年第7期25卷 120-126页

作者： Zheng-hong WU, Qi-neng PING2, Yi WEI, Jia-ming LAI Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China Department of Pharmaceutics China Pharmaceutical University Nanjing 210009 China

AIM: To evaluate the hypoglycemic efficacy of insulin liposomes coated by chitosan with different molecular weights and concentrations after oral administration in mice. METHODS: Insulin-liposomes were prepared by reversed-phase evaporation. Chitosan coating was carried out by incubation of the liposomal suspensions with the chitosan solution. The hypoglycemic efficacies of chitosan-coated insulin liposomes were investigated by monitor- ing the blood glucose level using the glucose oxidase method after oral administration to healthy mice. RESULTS: In all the insulin liposomes, the insulin liposomes coated by 0.2 % chitosan (Mr 1000 kDa) showed a better hypogly- cemic efficacy as compared with the other liposomes coated by chitosan. The minimum blood glucose level was 15.1 %±6.0 % of the initial (n=6). The hypoglycemic efficacy lasted for 4 h after oral administration to mice. CONCLUSION: Chitosan-coated liposomes could reduce tryptic digestion on insulin, and enhance enteral absorp- tion of insulin. The molecular weights and concentrations of chitosan had significant effects on hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration to healthy mice.

关键词： chitin chitosan insulin liposomes blood glucose oral administration

A practical method to trace intracellular and transcellular transport pathways of gold nanoparticles via oral administration

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Journal of Chinese Pharmaceutical Sciences 2016年第10期25卷 737-746页

作者：刘德春杨丹何冰代文兵张华王学清袁兰张强唐星沈阳药科大学药学院辽宁沈阳110016 北京大学医学部药学院天然药物及仿生药物国家重点实验室北京100191 北京大学医学部医药卫生分析中心北京100191

oral nanoparticles play an important role in improving the bioavailability of poorly water-soluble drug. It is necessary to investigate the interaction of nanoparticles with intestinal epithelial cells. In general, nano-carriers labeled with fluorescent probes are always chosen. However, fluorescent dye via physical loading may leak in complex biological environment and lose its function to trace the transport behavior ofnanoparticles. Fluorescent probes chemically coupled on the nanoparticles may alter the properties of nanoparticles. Therefore, a facile and exact detection method is required to trace intracellular and transcellular pathways of oral nano-medicines. In our study, gold nanoparticles were selected as nano-carriers owing to their unique characteristics of light scattering. The feasibility of gold nanoparticle detection through reflected light signal was tested in different situations, including gold nanoparticle solution, cell and animal level As a result, high resolution image of gold nanoparticles could be detected through reflection mode by confocal laser scanning microscope （CLSM） when excited at a wavelength of 633 nm. The reflected light signal of gold nanoparticles could be clearly shown in different intestinal epithelial cells no matter when they were in fixed or in living state, and the intracellular trafficking and distribution of gold nanoparticles were clearly shown in three-dimensional image. Meanwhile, this method was also applied to rat small intestine in vivo. In conclusion, we believed that this technique was a convenient and precise way to explore the transport behavior of gold nanoparticles via oral administration without fluorescent dye.

关键词： Gold nanoparticles Reflected light signal CLSM oral administration Intracellular and transcellular pathways In vivo

Pharmacokinetics of Milbemycin Oxime in Dogs Following Its Intravenous and oral administration

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Journal of Northeast Agricultural University(English Edition) 2018年第1期25卷 47-54页

作者： Lu Yi-tong Qi Lian-wen Xu Qian-qian Ding Liang-jun Wang Bo Liu Hai-rui Li Ji-chang State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 211198China College of Veterinary Medicine Northeast Agricultural UniversityHarbin 150030China Shandong Binzhou Animal Science and Veterinary Medicine Academy Binzhou 256600ShandongChina

The pharmacokinetics of milbemycin oxime was investigated in dogs following oral(per os, PO) and intravenous(IV) administration. Three groups of dogs received milbemycin oxime tablets as a single PO dose equal to 0.25, 0.5 and 1.0 mg · kg-1 of milbemycin oxime, respectively, another group received a single IV dose of 0.5 mg · kg-1. Blood samples were collected at predetermined times after drug administration and the milbemycin oxime concentrations in plasma were determined by LC-MS/MS. The drug protein binding in dog plasma in vitro was determined by equilibrium dialysis at concentrations spanning the range of values observed in vivo in dog plasma. After PO administration at doses of 0.25, 0.5 and 1.0 mg · kg-1, milbemycin oxime was slowly absorbed and eliminated, the time to reach the maximum plasma concentration(Tmax) was 4.14±0.20, 4.27±0.14 and 4.06±0.13 h, the mean absorption time(MAT) was 19.06, 13.67 and 11.77 h, the terminal rate half-life(t1/2λz) was 15.06±0.37, 11.09±0.54 and 9.76±0.89 h and the total body clearance(Cl) was 1.15±0.05, 1.18±0.03 and 1.17±0.07 m L · min-1 · kg-1, respectively. The maximum plasma concentration(Cmax, 36.50±1.40, 76.11±2.77 and 182.05±7.20 ng · m L-1, respectively) and the area under the first-moment curve(AUC-10→∞, 985.83±49.46, 1 663.12±51.42 and 3 558.04±197.88 mg · h · L, respectively) increased accordingly to the administered dose rates; the oral bioavailabilities were estimated to be 88.61%, 74.75% and 79.96%, respectively. The values of fu were 0.12%, 0.14% and 0.13% in dog plasma, respectively. In conclusion, the pharmacokinetics of milbemycin oxime in dogs following oral administration revealed its higher oral bioavailability and advantageous pharmacokinetic properties, such as its lower total body clearance and longer elimination half-life, and indicated that the single oral dose of 0.50 mg · kg-1 of milbemycin oxime which was recommended in all the parasitological efficacy studies allowed an adequate concentration of

关键词： pharmacokinetic macrolide milbemycin oxime oral administration dog

Pharmacokinetics of diclazuril after oral administration of clinical doses to rabbits

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Journal of Chinese Pharmaceutical Sciences 2009年第3期18卷 273-277页

作者：胡连栋刘慈徐文河北大学药学院河北保定071002 第二军医大学长征医院药学部上海200003

The purpose of this study was to evaluate the pharmacokinetic parameters and bioavailability of the solid dispersion formulation of diclazuril after oral administration in rabbits in comparison with its known premix form with feed *** concentrations were determined by high-performance liquid chromatography（HPLC）.The areas under the plasma concentration curves（AUC0-∞） of diclazuril in solid dispersion and premix were 247.8±18.1μg/h/mL and 145.4±12.6μg/h/mL,respectively. The Cmax of diclazuril in solid dispersion and premix were 33.72±4.75 μg/mL and 10.42±3.4μg/mL, respectively, The t1/2 were 9.53±1.37 and 9.23±1.20 min, respectively. The oral bioavailability of drug solid dispersion was 1.7-fold higher than that of premix. From these data we concluded that diclazuril solid dispersion may be used as a potential anticoccidial preparation.

关键词： Diclazuril Rabbits Pharmacokinetics oral administration High-performance liquid chromatography

Pharmacokinetics of oxytetracycline in yellow catfish (Pelteobagrus fulbvidraco) with a single and multiple-dose oral administration

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Pharmacokinetics of oxytetracycline in yellow catfish (Pelte...

A　Study　on　Early　Biological　Effects　of　oral　administration　of　Terephthalic　Acid　in　Rats

中国水产学会鱼病专业委员会2013年学术研讨会

作者： Juan Yuan Ru-Qin Li Yan Shi Xiao-Yun Peng Xiao-Xuan Chen Zhi-Xin Wu Department of Aquatic Animal Medicine College of Fisheries Huazhong Agricultural University/Key Lab of Freshwater Animal Breeding Ministry of Agriculture/Freshwater Aquaculture Collaborative Innovation Center of Hubei Province

A pharmacokinetic study of oxytetracycline(OTC)following a single(100 mg/kg)or amulti-dose(100 mg/kg for 5 days)oral administration was carried out in yellow catfish,Pelteobagrus *** oral administration at 25℃,a one-compartment model *** absorption half-life(t1/2(ka))was 3.92,1.44,2.75 and 3.34 h in plasma,muscle,liver,and kidney after the single dose,and 0.35,0.22,0.42,0.32 h after the multi-dose,*** order of peak concentration(Cmax)was liver>kidney>plasma>muscle,at 3.48μg/g,2.90μg/g,1.46μg/ml,and 1.39μg/g after the single dose,and 14.02μg/g,8.51μg/g,4.17μg/ml,and 3.84μg/g after the multi-dose,*** elimination half-lives(t1/2(ke))of OTCin plasma,muscle,liver,and kidney were calculated to be 7.67,26.29,19.08 and 10.61 h after thesingle dose,and 47.54,70.99,49.87 and 47.73 h after the multi-dose,*** resultssuggest that OTC was absorbed faster after the multi-dose than after the single dose,suggestingthat OTC could be more efficacious after the multi-dose and more effective to control the bacterialdiseases in aquaculture,with a side effect of longer withdrawal periods.

关键词： pharmacokinetic oxytetracycline(OTC) oral administration yellow catfish

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The Journal of Biomedical Research 1994年第1期18卷 74-74页

作者： Qiu Qing, et al. ACTA ACADEMIAE MEDICINAF,NANJING,1994,14(2):131-133

Rats were fed with foods containing various doses of terephthalic (TPA) for 8 weeks. General status was observed and biological indices(including urine,serum and bone) were determined after 1, 3 and 8 week *** in urine calcium, ammonia, PH and serum albumin between the treat groups and the control were significant. Marked correlation was found in these indices. No Change in N-acetyl-β-D-glucosaminidase (NAG),serum calcium,bone calcium, alkaline phosphatase and alanine transaminase was noted in the treat *** suggests that change of urine ammonium concentration may serve as a protective level in setting the TPA exposure limit.

关键词： terphthalic acid oral administration biological effect rat

Double-layer probiotic encapsulation for enhanced bacteriotherapy against inflammatory bowel disease

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Nano Research 2024年第10期17卷 9103-9110页

作者： Yixin Wang Jun Liu Sichen Yuan Yawen You Quanyin Hu Pharmaceutical Sciences Division School of PharmacyUniversity of Wisconsin-MadisonMadisonWI 53705USA Carbone Cancer Center School of Medicine and Public HealthUniversity of Wisconsin-MadisonMadisonWI 53705USA Wisconsin Center for NanoBioSystems School of PharmacyUniversity of Wisconsin-MadisonMadisonWI 53705USA

Inflammatory bowel disease(IBD)is inflammatory intestinal disorders associated with dysregulated gut *** that leverages bacteria as therapeutics has shown tremendous promise in resolving gut dysbiosis and reducing inflammatory mediators to treat *** delivered probiotics,such as Escherichia coli Nissle 1917(EcN),can produce beneficial ingredients,competitively inhibit the proliferation of pathogens,and promote the restoration of gut microbiome ***,environmental stresses(such as gastric acids)in the gastrointestinal(GI)tract pose an enormous challenge to the probiotics following oral administration,leading to decreases in viability and activity of ***,the inferior mucoadhesive capability of probiotics results in low colonization efficacy,further compromising their therapeutic *** probiotics with functional biomaterials may protect them from elimination and prolong their retention in the GI ***,we developed a facile double-layer electrostatic assembly technique to encapsulate EcN bacteria in protective layers of mucoadhesive chitosan(CS)and immunomodulatory hyaluronic acid(HA)to generate *** biomaterials confer the coated EcN resistance to environmental assault and enhanced mucoadhesion in the GI *** probiotics equipped with the multifunctional shield can thus suppress inflammation and reshape the intestinal microenvironment to enhance therapeutic efficacy for the prevention and treatment of ***,this study presents a novel probiotic coating strategy to augment the outcome of bacteriotherapy to combat IBD.

关键词： probiotics biomaterial coating inflammatory bowel disease mucoadhesion oral administration

Microenvironment responsive pod-structured astaxanthin nanocarrier for ameliorating inflammatory bowel disease

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Chinese Chemical Letters 2024年第7期35卷 360-366页

作者： Jingting Wang Yuanyuan Chen Linlin Han Shasha Xia Xingyao Zhang Peng Xue Yuejun Kang Jian Ming Zhigang Xu Key Laboratory of Luminescence Analysis and Molecular Sensing Ministry of EducationSchool of Materials and Energy&Chongqing Engineering Research Center for Micro-Nano Biomedical Materials and DevicesSouthwest UniversityChongqing 400715China College of Food Science Southwest UniversityChongqing 400715China State Key Laboratory of Chemo/Biosensing and Chemometrics Hunan UniversityChangsha 410082China

Anti-inflammatory drugs targeting inflammatory bowel disease(IBD)have attracted considerable attention but still face low therapeutic outcomes and frequent side ***(ATX),a natural ketone,possesses potent antioxidant and anti-inflammatory ***,it faces problems such as poor water solubility,photothermal instability,and low ***,we employed a supramolecular encapsulation strategy to create a nanoscale oral delivery system for ATX(referred to as FC-ATX NPs)by coupling fucoidan(FUC)with chitosan oligosaccharides(COS).The obtained FC-ATX NPs exhibited a particular“bean pod”structure with uniform size,good encapsulation efficiency,excellent physical and chemical stability,pH-triggered intestinal targeted slow-release properties,and potent antioxidant *** vitro cell culture experiments showed that FC-ATX NPs promoted cellular uptake and scavenged excessive intracellular reactive oxygen species(ROS).In mouse models of colitis,FC-ATX NPs enhanced the drug absorption of intestinal epithelial cells and effectively accumulated at the site of *** work provides an efficient approach to enhance the bioavailability of ATX and has excellent application potential as an oral targeted delivery system for colitis therapy.

关键词： oral administration Astaxanthin Nanocarrier Anti-oxidant activity Colon targeting

Arsenic toxicity in mice and its possible amelioration

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Journal of Environmental Sciences 2004年第3期16卷 447-453页

作者： R.J.Verma Archana Vasu Abdul Alim Saiyed Department of Zoology Department of ZoologyDepartment of Zoology University School of SciencesGujarat UniversityAhmedabad 380009IndiaUniversity School of SciencesGujarat UniversityAhmedabad 380009IndiaUniversity School of SciencesGujarat UniversityAhmedabad 380009India

oral administration of arsenic trioxide(3 and 6 mg/kg body weight/d) for 30 d caused, as compared with vehicle control, dose dependent significant reductions in body weight, absolute weight, protein, glycogen, as well as, total, dehydro and reduced ascorbic acid contents both in the liver and kidney of arsenic treated mice. Succinic dehydrogenase(SDH) and phosphorylase only in the liver activities were significantly reduced in a dose dependent manner. Acid phosphatase activity was significantly decreased in the liver of low dose arsenic treated animals; however, significant rise in its activity was observed in high dose group. As compared with vehicle control, treatment also caused significant dose dependent reductions in SDH, alkaline phosphatase and acid phosphatase activities in the kidney of mice. Vitamin E cotreatment as well as, 30 d withdrawal of arsenic trioxide treatment with or without vitamin E caused significant amelioration in arsenic induced toxicity in mice. administration of vitamin E during withdrawal of treatment also caused significant amelioration as compared from only withdrawal of the treatment. It is concluded that vitamin E ameliorates arsenic induced toxicities in the liver and kidney of mice.

关键词： arsenic toxicity mice oral administration amelioration