Nasal timosaponin BII dually sensitive in situ hydrogels for the prevention of Alzheimer's disease induced by lipopolysaccharides.


:Alzheimer's disease (AD) is a common and severe brain disease with a high mortality among the elders, but no highly efficient medications are currently available. For example, timosaponin BII, an efficient anti-AD agent, has low oral bioavailability. Here, timosaponin BII was formulated in a temperature/ion-sensitive in situ hydrogel (ISG) that was well transformed into gels in the nasal environment. Timosaponin BII protected the PC12 cells injured by lipopolysaccharides (LPS) by decreasing TNF-α and IL-1β and stabilizing F-actin. Timosaponin BII ISGs were intranasally administered to the mice every day for 38 days. On Day 36, LPS was injected to the mice to establish an AD model. Morris water maze experiments showed that the number of the animals that were able to cross the platform returned to normal and the total distance over which the animals moved in the open field also increased, which demonstrated that the spatial memory and spontaneous behavior were improved after treatment compared to the model. Moreover, an AD improver, inducible nitric oxide synthase (iNOS) in the brain, was reduced after treatment. High brain targeting effect of timosaponin BII ISGs was confirmed by in vivo fluorescence imaging. The nasal timosaponin BII dually sensitive ISGs can serve as a promising medication for local prevention of AD.


Int J Pharm


Chen W,Li R,Zhu S,Ma J,Pang L,Ma B,Du L,Jin Y




Has Abstract


2020-03-30 00:00:00












  • Diffusion and binding of 5-fluorouracil in non-ionic hydrogels with interpolymer complexation.

    abstract::Hydrogen-bonded interpolymer complexes can be used for development of novel dosage forms. In this study, two types of crosslinked hydrogels, copolymer networks of N-vinyl pyrrolidone and acrylamide (PVP-co-PAM) and interpenetrating polymer networks (IPN) composed of crosslinked PVP-co-PAM and poly(vinyl alcohol) (PVA)...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Zhou W,Lu P,Sun L,Ji C,Dong J

    更新日期:2012-07-15 00:00:00

  • Induction of immunogenic cell death of cancer cells through nanoparticle-mediated dual chemotherapy and photothermal therapy.

    abstract::The use of nanomedicines to induce immunogenic cell death is a new strategy that aims to increase tumor immunogenicity and thereby prime tumors for further immunotherapies. In this study, we developed a nanoparticle formulation for combinatory chemotherapy and photothermal therapy based only on materials previously us...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Heshmati Aghda N,Abdulsahib SM,Severson C,Lara EJ,Torres Hurtado S,Yildiz T,Castillo JA,Tunnell JW,Betancourt T

    更新日期:2020-09-06 00:00:00

  • In-line monitoring of partial and overall solid concentration during solvent-mediated phase transition using Raman spectroscopy.

    abstract::A calibration strategy for the continuous monitoring of solvent-mediated phase transition was developed using in situ Raman spectroscopy. Citric acid which exhibits enantiotropy during its anhydrous/monohydrate phase transition was selected as a model organic product. Using 25 samples in suspension, specific calibrati...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Caillet A,Puel F,Fevotte G

    更新日期:2006-01-13 00:00:00

  • Preparation, characterization, and optimization of asenapine maleate mucoadhesive nanoemulsion using Box-Behnken design: In vitro and in vivo studies for brain targeting.

    abstract::The tight junctions between capillary endothelial cells of the blood-brain barrier (BBB) restricts the entry of therapeutics into the brain. Potential of the intranasal delivery tool has been explored in administering the therapeutics directly to the brain, thus bypassing BBB. The objective of this study was to develo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Kumbhar SA,Kokare CR,Shrivastava B,Gorain B,Choudhury H

    更新日期:2020-08-30 00:00:00

  • Influence of dissolution medium buffer composition on ketoprofen release from ER products and in vitro-in vivo correlation.

    abstract::The purpose of this work was to investigate the influence of dissolution medium composition on the in vitro release of ketoprofen from a series of ER products and the impact of the different buffer media on the in vivo-in vitro (IVIV) relationship. The products investigated were coated micro bead preparations having i...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Corrigan OI,Devlin Y,Butler J

    更新日期:2003-03-26 00:00:00

  • MALDI mass spectrometry imaging as a complementary analytical method for improved skin distribution analysis of drug molecule and excipients.

    abstract::In cutaneous drug delivery, it is widely accepted that the choice of excipients affects the delivery of a drug molecule to the skin. MALDI mass spectrometry imaging (MALDI-MSI) is an imaging technique which enables the simultaneous detection of multiple compounds. MALDI-MSI was applied to study the penetration of tofa...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Handler AM,Fallah M,Just Pedersen A,Pommergaard Pedersen G,Troensegaard Nielsen K,Janfelt C

    更新日期:2020-11-30 00:00:00

  • Biomedical potentialities of cationic geminis as modulating agents of liposome in drug delivery across biological barriers and cellular uptake.

    abstract::Hydroxyethyl bearing gemini surfactants, alkanediyl-α,ω-bis(N-hexadecyl-N-2-hydroxyethyl-N-methylammonium bromide), 16-s-16(OH), were used to augment phosphatidylcholine based liposomes to achieve higher stability and enhanced cellular uptake and penetration. The developed liposomes were loaded with rhodamine B, doxor...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Pavlov RV,Gaynanova GA,Kuznetsova DA,Vasileva LA,Zueva IV,Sapunova AS,Buzyurova DN,Babaev VM,Voloshina AD,Lukashenko SS,Rizvanov IK,Petrov KA,Zakharova LY,Sinyashin OG

    更新日期:2020-09-25 00:00:00

  • The modified extended Hansen method to determine partial solubility parameters of drugs containing a single hydrogen bonding group and their sodium derivatives: benzoic acid/Na and ibuprofen/Na.

    abstract::Sodium salts are often used in drug formulation but their partial solubility parameters are not available. Sodium alters the physical properties of the drug and the knowledge of these parameters would help to predict adhesion properties that cannot be estimated using the solubility parameters of the parent acid. This ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Bustamante P,Pena MA,Barra J

    更新日期:2000-01-20 00:00:00

  • Application of a chromatic confocal measurement system as new approach for in-line wet film thickness determination in continuous oral film manufacturing processes.

    abstract::The key parameter of the oral film production process is the wet film thickness since it regulates the active pharmaceutical ingredient (API) content of the finished product. There is no general recommendation on how to adjust the gap height of the coating knife during the film manufacturing process to obtain the targ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Niese S,Quodbach J

    更新日期:2018-11-15 00:00:00

  • Transdermal delivery of naloxone: effect of water, propylene glycol, ethanol and their binary combinations on permeation through rat skin.

    abstract::The effect of the solvent systems water, ethanol (EtOH), propylene glycol (PG) and their binary combinations was studied on the ex vivo permeation profile of the opioid receptor antagonist, naloxone, through rat skin. Fourier transform-infrared (FT-IR) spectroscopic studies were done to investigate the effect of enhan...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Panchagnula R,Salve PS,Thomas NS,Jain AK,Ramarao P

    更新日期:2001-05-21 00:00:00

  • Classification of microcrystalline celluloses via structures of individual particles measured by synchrotron radiation X-ray micro-computed tomography.

    abstract::Microcrystalline cellulose (MCC) is one of the most important excipients due to its outstanding binding and tableting properties. Owing to the absence of high resolution characterization techniques at the single particle scale, 3D (three dimension) microstructure of MCC and its effects on formulation performance remai...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Fang L,Yin X,Wu L,He Y,He Y,Qin W,Meng F,York P,Xu X,Zhang J

    更新日期:2017-10-15 00:00:00

  • Multifunctional TK-VLPs nanocarrier for tumor-targeted delivery.

    abstract::Virus-like particles (VLPs) have been exploited for various biomedical applications, such as the monitoring, prevention, diagnosis and therapy of disease. In this study, a novel multifunctional VLPs nanocarrier (TK-VLPs) was prepared and used for tumor-targeted delivery. The SPR and cell uptake results indicated that ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Ren Y,Mu Y,Jiang L,Yu H,Yang S,Zhang Y,Wang J,Zhang H,Sun H,Xiao C,Peng H,Zhou Y,Lu W

    更新日期:2016-04-11 00:00:00

  • A novel particle engineering technology: spray-freezing into liquid.

    abstract::Spray-freezing into liquid (SFL) is a novel particle engineering technology where a feed solution containing an active pharmaceutical ingredient (API) and pharmaceutical excipient(s) is atomized beneath the surface of a cryogenic liquid, such as liquid nitrogen. Intense atomization results from the impingement that oc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Rogers TL,Hu J,Yu Z,Johnston KP,Williams RO 3rd

    更新日期:2002-08-21 00:00:00

  • Peptide ligand-mediated liposome distribution and targeting to EGFR expressing tumor in vivo.

    abstract::Epidermal growth factor receptor (EGFR) is an important anti-cancer therapy target that is applicable to many cancer types. We had previously reported the screening and discovery of a novel peptide ligand against EGFR named GE11. It was shown to bind to EGFR competitively with EGF and mediate gene delivery to cancer c...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Song S,Liu D,Peng J,Sun Y,Li Z,Gu JR,Xu Y

    更新日期:2008-11-03 00:00:00

  • Nanoparticles based on natural, engineered or synthetic proteins and polypeptides for drug delivery applications.

    abstract::Medicine formulations at the nanoscale, referred to as nanomedicines, have managed to overcome key challenges encountered during the development of new medical treatments and entered clinical practice, but considerable improvement in terms of local efficacy and reduced toxicity still need to be achieved. Currently, th...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Georgilis E,Abdelghani M,Pille J,Aydinlioglu E,van Hest JCM,Lecommandoux S,Garanger E

    更新日期:2020-08-30 00:00:00

  • The solubility, permeability and the dose as key factors in formulation development for oral lipophilic drugs: Maximizing the bioavailability of carbamazepine with a cosolvent-based formulation.

    abstract::The purpose of this research was to investigate drug dose, solubility, permeability, and their interplay, as key factors in oral formulation development for lipophilic drugs. A PEG400-based formulation was studied for five doses of the lipophilic drug carbamazepine, accounting for biorelevant dissolution of the dose i...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Fine-Shamir N,Beig A,Miller JM,Dahan A

    更新日期:2020-05-30 00:00:00

  • Production of salbutamol sulfate for inhalation by high-gravity controlled antisolvent precipitation.

    abstract::The purpose of this study was to produce salbutamol sulfate (SS) as a model anti-asthmatic drug using high-gravity controlled precipitation (HGCP) through antisolvent crystallisation. An aqueous solution of SS was passed through a HGCP reactor with isopropanol as antisolvent to induce precipitation. Spray drying was e...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Chiou H,Li L,Hu T,Chan HK,Chen JF,Yun J

    更新日期:2007-02-22 00:00:00

  • Interaction of solutions containing phenothiazines exposed to laser radiation with materials surfaces, in view of biomedical applications.

    abstract::Phenothiazine drugs - chlorpromazine (CPZ), promazine (PZ) and promethazine (PMZ) - were exposed to 266 nm (fourth harmonic of the Nd:YAG pulsed laser radiation) in order to be modified at molecular level and to produce an enhancement of their antibacterial activity. The irradiated samples were analysed by several met...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Simon A,Alexandru T,Boni M,Damian V,Stoicu A,Dutschk V,Pascu ML

    更新日期:2014-11-20 00:00:00

  • Biological activity of heterologous murine interleukin-10 and preliminary studies on the use of a dextrin nanogel as a delivery system.

    abstract::Interleukin-10 (IL-10) is an anti-inflammatory cytokine, which active form is a non-covalent homodimer with two intramolecular disulphide bonds essential for its biological activity. A mutated form of murine IL-10 was successfully expressed in E. coli, recovered and purified from inclusion bodies. Its ability to reduc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Carvalho V,Castanheira P,Faria TQ,Gonçalves C,Madureira P,Faro C,Domingues L,Brito RM,Vilanova M,Gama M

    更新日期:2010-11-15 00:00:00

  • Liposomes encapsulating native and cyclodextrin enclosed paclitaxel: Enhanced loading efficiency and its pharmacokinetic evaluation.

    abstract::Combination strategy involving cyclodextrin (CD) complexation and liposomal system was investigated for Paclitaxel (PTX) to improve loading. Complexation was done using 2,6-di-O-methylbetacyclodextrin (DMβCD). Sterically stabilized double loaded PEGylated liposomes (DLPLs) containing PTX and PTX-DMβCD complex were pre...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Bhatt P,Lalani R,Vhora I,Patil S,Amrutiya J,Misra A,Mashru R

    更新日期:2018-01-30 00:00:00

  • Effects of drying technique on extrusion-spheronisation granules and tablet properties.

    abstract::Extrusion-spheronisation was used to generate smooth, highly spherical granules of a microcrystalline cellulose/propyl gallate/water paste. Freeze-drying retained the shape and size of the granules, whereas oven-drying produced roughened granules due to the uneven shrinkage of the wet powders. Compaction of one size f...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Song B,Rough SL,Wilson DI

    更新日期:2007-03-06 00:00:00

  • Impact of implant composition of twin-screw extruded lipid implants on the release behavior.

    abstract::The development of vaccine delivery systems that will remove or reduce the need for repeated dosing has led to the investigation of sustained release systems. In this context, the duration of antigen release is of great importance as is the requirement for concomitant adjuvant release. In this work, lipid implants con...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Even MP,Bobbala S,Kooi KL,Hook S,Winter G,Engert J

    更新日期:2015-09-30 00:00:00

  • Long-circulating non-toxic blood pool imaging agent based on hyperbranched polyglycerols.

    abstract:PURPOSE:Currently, in vivo or in vitro(99m)Tc-radiolabelled red blood cells are the standard blood pool imaging agents. Due to risks associated with handling of blood and the problems with the current (99m)Tc shortage, we were interested in a long-circulating biocompatible synthetic macromolecule that would be simple t...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Saatchi K,Gelder N,Gershkovich P,Sivak O,Wasan KM,Kainthan RK,Brooks DE,Häfeli UO

    更新日期:2012-01-17 00:00:00

  • Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery.

    abstract::The purpose of this study was to construct isotretinoin-loaded SLN (IT-SLN) formulation with skin targeting for topical delivery of isotretinoin. PRECIROL ATO 5 was selected as the lipid of SLN. Tween 80 and soybean lecithin were used as the surfactants to stabilize SLN. The hot homogenization method was performed to ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Liu J,Hu W,Chen H,Ni Q,Xu H,Yang X

    更新日期:2007-01-10 00:00:00

  • Type of pH sensitive linker reveals different time-dependent intracellular localization, in vitro and in vivo efficiency in alpha-fetoprotein receptor targeted doxorubicin conjugate.

    abstract::Despite the presence of a variety of modern anticancer drugs at the market, doxorubicin (Dox) is still widely used in antineoplastic therapy, although its administration causes severe side effects. To enhance specific activity of such molecules, various approaches have been exploited: targeted moieties like monoclonal...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Mollaev M,Gorokhovets N,Nikolskaya E,Faustova M,Zabolotsky A,Zhunina O,Sokol M,Zamulaeva I,Severin E,Yabbarov N

    更新日期:2019-03-25 00:00:00

  • A prototype 'Infucon' device for continuous infusion of microbubbles in vivo.

    abstract::A device for continuous infusion of microbubbles (MBs) 'Infucon' has been designed, constructed and tested on rabbits. The device prevents MBs from flotation and accumulation in the layer directly below the surface in the syringe injection during i.v. application. Homogenous i.v. application of MBs was tested on 16 ma...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Kauerová Z,Lukáč R,Kohout P,Mašek J,Koudelka Š,Plocková J,Vašíčková M,Vlašín M,Turánek J

    更新日期:2013-01-30 00:00:00

  • Correlation of solid dosage porosity and tensile strength with acoustically extracted mechanical properties.

    abstract::Currently, the compressed tablet and its oral administration is the most popular drug delivery modality in medicine. The accurate porosity and tensile strength characterization of a tablet design is vital for predicting its performance such as disintegration, dissolution, and drug-release efficiency upon administratio...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Xu X,Mack C,Cleland ZJ,Vallabh CKP,Dave VS,Cetinkaya C

    更新日期:2018-05-05 00:00:00

  • 3D printed drug products: Non-destructive dose verification using a rapid point-and-shoot approach.

    abstract::Three-dimensional printing (3DP) has the potential to cause a paradigm shift in the manufacture of pharmaceuticals, enabling personalised medicines to be produced on-demand. To facilitate integration into healthcare, non-destructive characterisation techniques are required to ensure final product quality. Here, the us...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Trenfield SJ,Goyanes A,Telford R,Wilsdon D,Rowland M,Gaisford S,Basit AW

    更新日期:2018-10-05 00:00:00

  • Dependency of cyclosporine tissue distribution and metabolism on the age and gender of rats after a single intravenous dose.

    abstract::In a previous study we demonstrated the dependency of cyclosporine (CyA) pharmacokinetics on the age and gender of Wistar rats given 10 mg/kg intravenously. The present study has been conducted under the same experimental conditions (10 mg/kg as a single intravenous dose) to identify the mechanisms behind such differe...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Molpeceres J,Chacón M,Guzmán M,Aberturas MR,Berges L

    更新日期:2000-03-20 00:00:00

  • Development of enteric-coated fixed dose combinations of amorphous solid dispersions of ezetimibe and lovastatin: Investigation of formulation and process parameters.

    abstract::Enteric-coated fixed-dose combinations of ezetimibe and lovastatin were prepared by fluid bed coating aiming to avoid the acidic conversion of lovastatin to its hydroxyacid derivative. In a two-step process, sucrose beads were layered with a glass solution of ezetimibe, lovastatin and Soluplus®, top-coated with an ent...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章


    authors: Riekes MK,Dereymaker A,Berben P,Augustijns P,Stulzer HK,Van den Mooter G

    更新日期:2017-03-30 00:00:00