In vitro permeability analysis, pharmacokinetic and brain distribution study in mice of imperatorin, isoimperatorin and cnidilin in Radix Angelicae Dahuricae

Fitoterapia ◽  
2013 ◽  
Vol 85 ◽  
pp. 144-153 ◽  
Author(s):  
Wan Lili ◽  
Sun Yehong ◽  
Yu Qi ◽  
Huo Yan ◽  
Zhu Jinhui ◽  
...  
Keyword(s):  
Brain Distribution ◽  
Distribution Study

scholarly journals Fabrication and Characterization of Paclitaxel and Resveratrol Loaded Soluplus Polymeric Nanoparticles for Improved BBB Penetration for Glioma Management

Polymers ◽  
2021 ◽  
Vol 13 (19) ◽  
pp. 3210
Author(s):  
Talib Hussain ◽  
Sathishbabu Paranthaman ◽  
Syed Mohd Danish Rizvi ◽  
Afrasim Moin ◽  
Devegowda Vishakante Gowda ◽  
...  
Keyword(s):  
Polymeric Nanoparticles ◽  
C6 Glioma Cells ◽  
Brain Distribution ◽  
Distribution Study ◽  
Therapeutic Modalities ◽  
The Central Nervous System ◽  
Distribution Studies

Gliomas are one of the prominent cancers of the central nervous system with limited therapeutic modalities. The present investigation evaluated the synergistic effect of paclitaxel (PAX) and resveratrol (RESV)-loaded Soluplus polymeric nanoparticles (PNPs) against glioma cell lines along with in vivo pharmacokinetics and brain distribution study. PAX-RESV-loaded PNPs were prepared by the thin film hydration technique and optimized for different dependent and independent variables by using DoE (Design-Expert) software. The in vitro physiochemical characterization of prepared PAX-RESV-loaded PNPs exhibited appropriate particle size, PDI and % encapsulation efficiency. Cytotoxicity assay revealed that PTX-RESV loaded PNPs had a synergistic antitumor efficacy against C6 glioma cells compared with single and combined pure drugs. Finally, the pharmacokinetic and brain distribution studies in mice demonstrated that the PNPs significantly enhanced the bioavailability of PTX-RESV PNPs than pure PAX and RESV. Thus, the study concluded that PAX-RESV PNPs combination could significantly enhance anti-glioma activity, and this could be developed into a potential glioma treatment strategy.

Pharmacokinetic and brain distribution study of an anti‐glioblastoma agent in mice by HPLC‐MS/MS

2022 ◽  
Author(s):  
Yaxin Li ◽  
Raina Dano ◽  
Cathy Li ◽  
Wenjing Zhang ◽  
Justin D. Lathia ◽  
...  
Keyword(s):  
Brain Distribution ◽  
Distribution Study

DEVELOPMENT, CHARACTERIZATION AND BRAIN DISTRIBUTION STUDIES OF NANOSTRUCTURED LIPID CARRIER CONTAINING SAQUINAVIR MESYLATE FOR NASAL ADMINISTRATION

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (09) ◽  
pp. 38-47
Author(s):  
H. S. Mahajan ◽  
◽  
M. I. Patel
Keyword(s):  
Adverse Effect ◽  
Targeted Delivery ◽  
Entrapment Efficiency ◽  
Nasal Administration ◽  
Nanostructured Lipid Carrier ◽  
Brain Distribution ◽  
Scanning Calorimetry ◽  
Distribution Studies

The aim of the present study was to formulate saquinavir mesylate loaded nanostructured lipid carriers (SQVM-NLC) and evaluate its brain distribution after nasal administration. NLCs reveal some advantages for drug therapy over conventional carriers, including increased solubility, the ability to enhance storage stability, improved permeability and bioavailability, reduced adverse effect, prolonged half-life, and tissue-targeted delivery. SQVM-NLCs were prepared by hot high pressure homogenization and subsequent stabilization by lyophilization. QVM- NLC developed showed a particle with the size of 124.4 nm, polydispersity index of 0.267, entrapment efficiency of 73% and the zeta potential of -24.9 mV. The results from Scanning Electron Microscopy (SEM), powder X-ray diffraction (XRD)and differential scanning calorimetry (DSC) demonstrated that SQVM was present in NLC in an encapsulated molecule form. Mucosal toxicity study on sheep nasal mucosa showed no significant adverse effect of SQVMloaded NLC. SQVM-NLC showed slower release compared with saquinavir mesylate suspension in vitro. In vivo brain distribution studies demonstrated desired drug concentration in brain after intra nasal administration of SQVM-NLC than PDS. The results of the study also suggest that SQVM-NLC could be a promising drug delivery system for antiretroviral therapy.

scholarly journals Development and Validation of a Sensitive UHPLC-MS/MS Method for the Measurement of Gardneramine in Rat Plasma and Tissues and its Application to Pharmacokinetics and Tissue Distribution Study

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3953 ◽  
Author(s):  
Zhao ◽  
Tan ◽  
Chen ◽  
Sun ◽  
Wang ◽  
...  
Keyword(s):  
Multiple Reaction Monitoring ◽  
Indole Alkaloid ◽  
Internal Standard ◽  
Gradient Elution ◽  
Rat Plasma ◽  
Limit Of Quantification ◽  
Tissue Samples ◽  
Distribution Study

As a novel monoterpenoid indole alkaloid, gardneramine has been confirmed to possess excellent nervous depressive effects. However, there have been no reports about the measurement of gardneramine in vitro and in vivo. The motivation of this study was to establish and validate a specific, sensitive, and robust analytical method based on UHPLC-MS/MS for quantification of gardneramine in rat plasma and various tissues after intravenous administration. The analyte was extracted from plasma and tissue samples by protein precipitation with methanol using theophylline as an internal standard (I.S.). The analytes were separated on an Agilent ZORBAX Eclipse Plus C18 column using a gradient elution of acetonitrile and 0.1% formic acid in water at a flow rate of 0.3 mL/min. Gardneramine and I.S. were detected and quantified using positive electrospray ionization in multiple reaction monitoring (MRM) mode with transitions of m/z 413.1→217.9 for gardneramine and m/z 181.2→124.1 for I.S.. Perfect linearity range was 1–2000 ng/mL with a correlation coefficient (r2) of ≥0.990. The lower limit of quantification (LLOQ) of 1.0 ng/mL was adequate for application to different preclinical studies. The method was successfully applied for determination of gardneramine in bio-samples.

UPLC-MS/MS method for determination of schisandrin in rat plasma and brain microdialysates: application to a comparative pharmacokinetic and brain distribution study in normal and Alzheimer’s disease rats

2017 ◽  
Vol 9 (32) ◽  
pp. 4740-4746 ◽  
Author(s):  
BinBin Wei ◽  
Mingyan Liu ◽  
Zaixing Chen ◽  
Minjie Wei
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Rat Plasma ◽  
Brain Distribution ◽  
Comparative Pharmacokinetic ◽  
Distribution Study

An efficient UPLC-MS/MS method for determining schisandrin in rat plasma and brain microdialysates has been developed and validated.

Transnasomucosal mucoadhesive microemulsion of zaltoprofen: A comparative brain distribution study

2017 ◽  
Vol 39 ◽  
pp. 237-246
Author(s):  
Surjyanarayan Mandal ◽  
Snigdha Das Mandal ◽  
Krishna Chuttani ◽  
Abhay Dharamsi ◽  
Bharat bhushan Subudhi
Keyword(s):  
Brain Distribution ◽  
Distribution Study

In vitro and in vivo investigations on fluoroquinolones; effects of the P-glycoprotein efflux transporter on brain distribution of sparfloxacin

2000 ◽  
Vol 12 (2) ◽  
pp. 85-93 ◽  
Author(s):  
Elizabeth C.M. de Lange ◽  
Sandrine Marchand ◽  
Dirk-Jan van den Berg ◽  
Inez C.J. van der Sandt ◽  
Albertus G. de Boer ◽  
...  
Keyword(s):  
Brain Distribution ◽  
Efflux Transporter ◽  
P Glycoprotein

scholarly journals Evaluation of recombinant Brachyspira pilosicoli oligopeptide-binding proteins as vaccine candidates in a mouse model of intestinal spirochaetosis

2010 ◽  
Vol 59 (3) ◽  
pp. 353-359 ◽  
Author(s):  
Abdolreza Movahedi ◽  
David J. Hampson
Keyword(s):  
Mouse Model ◽  
Binding Proteins ◽  
Control Group ◽  
Cumulative Number ◽  
Igg Antibody ◽  
Brachyspira Pilosicoli ◽  
Distribution Study ◽  
Different Strains

The anaerobic intestinal spirochaete Brachyspira pilosicoli colonizes the large intestine of humans, and various species of animals and birds, in which it may induce a mild colitis and diarrhoea. The aim of the current study was to evaluate the use of putative oligopeptide-binding proteins of B. pilosicoli as vaccine components. A partial genome sequence of B. pilosicoli porcine strain 95/1000 was subjected to bioinformatics analysis, and six genes predicted to encode oligopeptide-binding proteins were selected. Following a PCR-based distribution study of the genes across different strains of the spirochaete, they were amplified from B. pilosicoli human strain WesB and cloned in Escherichia coli. The recombinant histidine-tagged proteins were purified and subjected to in vitro and in vivo immunogenicity analysis. Recombinant products (P-1 and P-3) from two genes that were immunogenic and recognized by sera from pigs that had recovered from B. pilosicoli infections were tested in a mouse model of intestinal spirochaetosis. For each recombinant protein, groups of 12 C3H/HeJ mice were vaccinated subcutaneously with 100 μg protein emulsified in Freund's incomplete adjuvant, twice with a 2 week interval. Two weeks later the vaccinated and non-vaccinated control animals were challenged orally with B. pilosicoli strain WesB. Both proteins induced systemic and local colonic IgG antibody responses, and, following experimental infection, the cumulative number of colonization days was significantly (P<0.001) less in both groups of vaccinated mice compared to the control mice. There were significantly (P=0.012) fewer mice colonized in the group vaccinated with P-1 than in the non-vaccinated control group. The results suggest that oligopeptide-binding proteins may have potential for use as components of vaccines for B. pilosicoli.

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