N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro,in silico and in vivo evaluation

2018 ◽  
Vol 93 (3) ◽  
pp. 364-372 ◽  
Author(s):  
Ajmer Singh Grewal ◽  
Rajeev Kharb ◽  
Deo Nandan Prasad ◽  
Jagdeep Singh Dua ◽  
Viney Lather
Keyword(s):  
In Silico ◽  
In Vivo Evaluation ◽  
Design Synthesis

Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh
Keyword(s):  
Drug Release ◽  
In Silico ◽  
Ex Vivo ◽  
Strong Interactions ◽  
Dissolution Time ◽  
Sem Images ◽  
In Vivo Evaluation ◽  
Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

scholarly journals In vitro and in vivo Evaluation of in silico Predicted Pneumococcal UDPG:PP Inhibitors

2020 ◽  
Vol 11 ◽  
Author(s):  
Freya Cools ◽  
Dhoha Triki ◽  
Nele Geerts ◽  
Peter Delputte ◽  
Denis Fourches ◽  
...  
Keyword(s):  
In Silico ◽  
In Vivo Evaluation

Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents

2020 ◽  
Vol 186 ◽  
pp. 111863 ◽  
Author(s):  
Muhammad Saeed Jan ◽  
Sajjad Ahmad ◽  
Fida Hussain ◽  
Ashfaq Ahmad ◽  
Fawad Mahmood ◽  
...  
Keyword(s):  
In Silico ◽  
Design Synthesis ◽  
In Silico Studies ◽  
Anti Inflammatory

Gastrointestinal transfer: In vivo evaluation and implementation in in vitro and in silico predictive tools

2014 ◽  
Vol 63 ◽  
pp. 233-242 ◽  
Author(s):  
Bart Hens ◽  
Joachim Brouwers ◽  
Bart Anneveld ◽  
Maura Corsetti ◽  
Mira Symillides ◽  
...  
Keyword(s):  
In Silico ◽  
In Vivo Evaluation ◽  
Predictive Tools

scholarly journals Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation ofN-(2-diethylaminoethyl)-4-[18F]fluorobenzamide ([18F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

2009 ◽  
Vol 20 (3) ◽  
pp. 583-590 ◽  
Author(s):  
Sudha Garg ◽  
Kanchan Kothari ◽  
Shankar R. Thopate ◽  
Aniruddha K. Doke ◽  
Pradeep K. Garg
Keyword(s):  
In Vivo Evaluation ◽  
Design Synthesis

In Silico, in Vitro, and in Vivo Evaluation of New Candidates for α-Synuclein PET Imaging

2018 ◽  
Vol 15 (8) ◽  
pp. 3153-3166 ◽  
Author(s):  
Mathieu Verdurand ◽  
Elise Levigoureux ◽  
Wael Zeinyeh ◽  
Laurent Berthier ◽  
Meriem Mendjel-Herda ◽  
...  
Keyword(s):  
Pet Imaging ◽  
In Silico ◽  
In Vivo Evaluation
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