Abstract
Physicochemical properties of drug molecules impact many aspects of both in vivo and in vitro behavior. Poor physicochemical properties can often create a significant impediment to establishing reliable SAR, establishing proof of principle type studies using in vivo models, and eventually leading to added performance variability and costs throughout the development life cycle; in the worst case scenario, even preventing execution of the desired development plan. Understanding the fundamental physicochemical properties provides the basis to dissect and deconvolute experimental observations in such a way that modification or mitigation of poor molecular properties can be impacted at the design phase, insuring design and selection of a molecule which has a high probability of making it through the arduous development cycle. This review will discuss the key physicochemical properties and how they can be assessed and how they are implicated in both discovery enablement and in final product developability of the selected candidate.
Keywords: Preformulation, solubility, stability, high throughput screening, lipophilicity, pharmacokinetics, absorption, formulation, solubilization
Combinatorial Chemistry & High Throughput Screening
Title: Preformulation Designed to Enable Discovery and Assess Developability
Volume: 13 Issue: 2
Author(s): Michael J. Hageman
Affiliation:
Keywords: Preformulation, solubility, stability, high throughput screening, lipophilicity, pharmacokinetics, absorption, formulation, solubilization
Abstract: Physicochemical properties of drug molecules impact many aspects of both in vivo and in vitro behavior. Poor physicochemical properties can often create a significant impediment to establishing reliable SAR, establishing proof of principle type studies using in vivo models, and eventually leading to added performance variability and costs throughout the development life cycle; in the worst case scenario, even preventing execution of the desired development plan. Understanding the fundamental physicochemical properties provides the basis to dissect and deconvolute experimental observations in such a way that modification or mitigation of poor molecular properties can be impacted at the design phase, insuring design and selection of a molecule which has a high probability of making it through the arduous development cycle. This review will discuss the key physicochemical properties and how they can be assessed and how they are implicated in both discovery enablement and in final product developability of the selected candidate.
Export Options
About this article
Cite this article as:
Hageman J. Michael, Preformulation Designed to Enable Discovery and Assess Developability, Combinatorial Chemistry & High Throughput Screening 2010; 13 (2) . https://dx.doi.org/10.2174/138620710790596781
DOI https://dx.doi.org/10.2174/138620710790596781 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...read more
Integrating Network Pharmacology and Traditional Medicine: A New Perspective in Drug Mechanism Research
Network pharmacology is a network construction and network topology analysis strategy that combines pharmacology and pharmacodynamics. In recent years, network pharmacology has emerged as a powerful tool that can be integrated with pharmacology. Natural products commonly function in multicomponent, multitarget, and multipathway systems. Some examples encompass Ayurveda, traditional Chinese medicines ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
A Role for Milk Proteins and their Peptides in Cancer Prevention
Current Pharmaceutical Design Synthesis and In Vitro Antiproliferative Activity of Diphenyl(piperidin-4- yl)thioamide Methanol Derivatives
Letters in Drug Design & Discovery Cyclic Opioid Peptides
Current Medicinal Chemistry Mining PeptideAtlas for Biomarkers and Therapeutics in Human Disease
Current Pharmaceutical Design Detection of Biothiols Using Some Novel Chemosensors: An Overview
Mini-Reviews in Organic Chemistry Quantitative Analysis of Salicylic Acid and its Derivatives in Primulae radix by High Performance Liquid Chromatography-Diode Array Detection- Electrospray Ionization Mass Spectrometry (HPLC-DAD-ESI-MS) and Simultaneous Determination of Total Polyphenol Content (TPC)
Current Analytical Chemistry Recent Insights into COVID-19 in Children and Clinical Recommendations
Current Pediatric Reviews A New Synthesis of Poly Heterocyclic Compounds Containing [1,2,4]triazolo and [1,2,3,4]tetrazolo Moieties and their DFT Study as Expected Anti-cancer Reagents
Current Organic Synthesis Regioselective Amination of 3-Bromoindolylmaleimide with Amines
Letters in Organic Chemistry MicroRNAs as Biomarkers for Birth Defects
MicroRNA A Review on the Monoacylglycerol Lipase: At the Interface Between Fat and Endocannabinoid Signalling
Current Medicinal Chemistry Microarrays in Brain Research: Data Quality and Limitations
Current Genomics Identification of N- and C-Terminal Residues Involved in MAP Kinase Phosphatase 3 (MKP3) Interdomain Binding and Auto-Inhibition
Protein & Peptide Letters Mast Cells and Basophils: Trojan Horses of Conventional Lin- Stem/Progenitor Cell Isolates
Current Pharmaceutical Design Obesity and Herbal Drug Research: Exploring the Safer Alternative and Lead Molecule
Current Traditional Medicine Peripheral Arterial Disease and Oxidative Stress
Vascular Disease Prevention (Discontinued) Review of the Biological Activity of Maslinic Acid
Current Drug Targets Application of New Advanced Electrochemical Methods Combine with Nano-Based Materials Sensor in Drugs Analysis
Current Analytical Chemistry Application of Cigarette Smoke Characterisation Based on Optical Aerosol Spectrometry. Dynamics and Comparisons with Tar Values
Current Analytical Chemistry Phase-Change Contrast Agents for Imaging and Therapy
Current Pharmaceutical Design