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Drug brain distribution following intranasal administration of Huperzine A in situ gel in rats

Acta Pharmacologica Sinica 2007年第2期28卷 273-278页

作者： Yan ZHAO Peng YUE Tao TAO~2 Qing-hua CHEN Shanghai Institute of Pharmaceutical Industry,Shanghai 200040,China Shanghai Institute of Pharmaceutical Industry Shanghai China

Aim:To determine the uptake extent of Huperzine A(Hup A)into the brain afterintranasal administration of Hup A in situ gel to rats,and to compare the pharma-cokinetic parameters between intranasal administration and iv and ***:Hup A was administered to male Sprague-Dawley rats via nasal,iv and oral routesat the dose of 166.7,166.7,and 500 μg/kg,*** and brain tissuesamples including the cerebrum,hippocampus,cerebellum and olfactory bulbwere collected,and the concentrations of Hup A in the samples were assayed *** area under the concentration-time curve(AUC0→6 h)and the ratio ofthe AUCbrain to the AUCplasma(drug targeting efficiency,DTE)were calculated toevaluate the brain targeting efficiency of the drug via 3 administration ***:The AUC0→6 h of the drug in the cerebrum,hippocampus,cerebellum,left olfactory bulb and right olfactory bulb after intranasal administration of theHup A in situ gel were 1.5,1.3,1.0,1.2,and 1.0 times of those after iv administrationof the injection,and 2.7,2.2,1.9,3.1,and 2.6 times of those after administration ofthe oral *** AUCbrain0→6 h/AUCplasma0→6 h of HupAin the cerebrum,hippocampus and left olfactory bulb following the intranasal administration dosewere significantly higher(P<0.05)than the iv ***:Intranasal deliv-ery showed a viable,non-invasive strategy for delivering the drug into brain.

关键词： Huperzine A in situ gel brain distribution intranasal administration

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Doxorubicin-loaded zein in situ gel for interstitial chemotherapy of colorectal cancer

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Acta Pharmaceutica Sinica B 2012年第6期2卷 610-614页

作者： Ning Shen Jie Hu Linan Zhang Li Zhang Yongjun Sun Yinghua Xie Shaomei Wu Lei Liu Zibin Gao Department of Pharmacy Hebei University of Science and TechnologyShijiazhuang 050018China Department of Immunology Hebei Medical UniversityShijiazhuang 050017China Department of Pharmaceutics New Drug Research and Development CenterNorth China Pharmaceutical Group CorporationShijiazhuang 050015China

The aim of this research was to evaluate doxorubicin(DOX)-loaded zein in situ gels,a new drug delivery system in which a liquid state drug can be transformed into semi-solid after intratumoral *** vitro release of DOX-loaded zein was investigated and the pharmacokinetics,biodistribution and therapeutic efficacy of these DOX-loaded zein formulations were investigated using BAI B/c nude tumor-bearing *** vitro release of DOX from the gels extended up to 7 *** accumulation of DOX in the tumor with lower drug concentration in blood and normal organs was obtained resulting in effective inhibition of tumor growth and fewer off-target side *** conclusion,a DOX-loaded in situ gel was developed with sustained release,enhanced anti-cancer efficacy for colorectal cancer in vivo,and especially with reduced off-target side effects.

关键词： Doxorubicin Zein in situ gel Tumor Intratumoral injection

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A stepwise optimization strategy to formulate in situ gelling formulations comprising fluconazole-hydroxypropyl-beta-cyclodextrin complex loaded niosomal vesicles and Eudragit nanoparticles for enhanced antifungal activity and prolonged ocular delivery

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Asian Journal of Pharmaceutical Sciences 2020年第5期15卷 617-636页

作者： Heba Elmotasem Ghada E.A.Awad Pharmaceutical Technology Department National Research CentreCairo 12622Egypt Chemistry of Natural and Microbial Product Department National Research CentreCairo 12622Egypt

Fungal keratitis and endopthalmitis are serious eye ***(FL)is indicated for their treatment,but suffers from poor topical ocular *** study was intended to improve and prolong its ocular *** niosomal vesicles were prepared using span ***,polymeric nanoparticles were prepared using cationic Eudragit RS100 and Eudragit *** investigated particles had adequate entrapment efficiency(EE%),nanoscale particle size and high zeta ***,formulations were optimized using full factorial ***-HP-β-CD complex was encapsulated in selected Eudragit nanoprticles(FL-CD-ERS1)and niosmal *** niosomes were further coated with cationic and bioadhesive chitosan(FL-CD-Nios-ch).EE%for FL-CD-ERS1 and FL-CD-Niosch formulations were 76.4%and 61.7%;particle sizes were 151.1 and 392 nm;also,they exhibited satisfactory zeta potential+40.1 and+28.5 m *** situ gels were prepared by poloxamer P407,HPMC and chitosan and evaluated for gelling capacity,rheological behavior and gelling *** increase the precorneal residence time,free drug and selected nano-formulations were incorporated in the selected in situ *** study revealed sustained release within 24 *** through excised rabbits corneas demonstrated enhanced drug flux and large AUC0-6 h in comparison to plain *** permeation of selected formulations labeled with Rhodamine B was visualized by Confocal laser *** study and in vivo tolerance test evidenced *** vivo susceptibility test using Candida albicans depicted enhanced growth inhibition and sustained *** this study the adopted stepwise optimization strategy combined cylodextrin complexation,drug nano-encapsulation and loading within thermosenstive in situ ***,the developed innovated formulations displayed boosted corneal permeation,enhanced antifungal activity and prolonged action.

关键词： Fluconazole Ocular Eudragit nanoparticles Cyclodextrin Niosomes in situ gel

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