Literature DB >> 17604872

High throughput solubility measurement in drug discovery and development.

Jochem Alsenz1, Manfred Kansy.   

Abstract

Measurement of drug solubility in various solvents is one of the key elements of compound characterization during the whole discovery and development process. This review summarizes current experimental approaches and addresses recent advances in the experimental methods used to determine drug solubility in drug discovery and early development. This paper focuses on high throughput methods designed to determine kinetic and thermodynamic (equilibrium) solubility but traditional methods are also presented. The focus, positioning, experimental setup, pros and cons, and limitations of individual assays are discussed and differences in solubility studies in discovery and development environments are highlighted. Finally, future needs and trends in solubility assay development designed to overcome current bottlenecks and trade-offs between speed and quality/quantity of measurements are addressed.

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Year:  2007        PMID: 17604872     DOI: 10.1016/j.addr.2007.05.007

Source DB:  PubMed          Journal:  Adv Drug Deliv Rev        ISSN: 0169-409X            Impact factor:   15.470


  32 in total

1.  Solubility at the molecular level: development of a critical aggregation concentration (CAC) assay for estimating compound monomer solubility.

Authors:  Jie Wang; Edmund Matayoshi
Journal:  Pharm Res       Date:  2012-03-16       Impact factor: 4.200

2.  A three-stage biophysical screening cascade for fragment-based drug discovery.

Authors:  Ellene H Mashalidis; Paweł Śledź; Steffen Lang; Chris Abell
Journal:  Nat Protoc       Date:  2013-10-24       Impact factor: 13.491

3.  Investigations on the 4-quinolone-3-carboxylic acid motif part 5: modulation of the physicochemical profile of a set of potent and selective cannabinoid-2 receptor ligands through a bioisosteric approach.

Authors:  Claudia Mugnaini; Stefania Nocerino; Valentina Pedani; Serena Pasquini; Andrea Tafi; Maria De Chiaro; Luca Bellucci; Massimo Valoti; Francesca Guida; Livio Luongo; Stefania Dragoni; Alessia Ligresti; Avraham Rosenberg; Daniele Bolognini; Maria Grazia Cascio; Roger G Pertwee; Ruin Moaddel; Sabatino Maione; Vincenzo Di Marzo; Federico Corelli
Journal:  ChemMedChem       Date:  2012-03-02       Impact factor: 3.466

4.  Solvent Selection for Insoluble Ligands, a Challenge for Biological Assay Development: A TNF-α/SPD304 Study.

Authors:  Christos P Papaneophytou; Anthi K Mettou; Vagelis Rinotas; Eleni Douni; George A Kontopidis
Journal:  ACS Med Chem Lett       Date:  2012-11-29       Impact factor: 4.345

Review 5.  Preclinical formulations: insight, strategies, and practical considerations.

Authors:  Sanket M Shah; Ankitkumar S Jain; Ritu Kaushik; Mangal S Nagarsenker; Maneesh J Nerurkar
Journal:  AAPS PharmSciTech       Date:  2014-06-12       Impact factor: 3.246

6.  Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.

Authors:  Javier de Vicente; Parcharee Tivitmahaisoon; Pamela Berry; David R Bolin; Daisy Carvajal; Wei He; Kuo-Sen Huang; Cheryl Janson; Lena Liang; Christine Lukacs; Ann Petersen; Hong Qian; Lin Yi; Yong Zhuang; Johannes C Hermann
Journal:  ACS Med Chem Lett       Date:  2015-08-04       Impact factor: 4.345

7.  Exploratory analysis of kinetic solubility measurements of a small molecule library.

Authors:  Rajarshi Guha; Thomas S Dexheimer; Aimee N Kestranek; Ajit Jadhav; Andrew M Chervenak; Michael G Ford; Anton Simeonov; Gregory P Roth; Craig J Thomas
Journal:  Bioorg Med Chem       Date:  2011-05-13       Impact factor: 3.641

8.  Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors.

Authors:  Giulia Vignaroli; Claudio Zamperini; Elena Dreassi; Marco Radi; Adriano Angelucci; Patrizia Sanità; Emmanuele Crespan; Miroslava Kissova; Giovanni Maga; Silvia Schenone; Francesca Musumeci; Maurizio Botta
Journal:  ACS Med Chem Lett       Date:  2013-05-20       Impact factor: 4.345

9.  Biomimetic Design of Protein Nanomaterials for Hydrophobic Molecular Transport.

Authors:  Dongmei Ren; Mercè Dalmau; Arlo Randall; Matthew M Shindel; Pierre Baldi; Szu-Wen Wang
Journal:  Adv Funct Mater       Date:  2012-04-23       Impact factor: 18.808

10.  Polymeric nanoparticles loaded with the 3,5,3'-triiodothyroacetic acid (Triac), a thyroid hormone: factorial design, characterization, and release kinetics.

Authors:  Karen C Dos Santos; Maria Fatima Gf da Silva; Edenir R Pereira-Filho; Joao B Fernandes; Igor Polikarpov; Moacir R Forim
Journal:  Nanotechnol Sci Appl       Date:  2012-07-19
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