Abstract
Passive transport properties of drug molecules are of utmost importance for their pharmacological and biopharmaceutical effectiveness. Diffusion in different media and through lipid bilayers is in many cases the ratedetermining step for the distribution in the body. In the present review an attempt is made to demonstrate the importance of solvation of drug molecules for the diffusion and partition / distribution in phases of different lipophilicity. Different approaches known in the literature to describe solvation of compounds with flexible conformation are discussed as well as the experimental methods to directly measure the energy of solvation. NSAIDs are chosen as an example of a class of drugs of different molecular structures that have already been studied thoroughly in many aspects, and a set of aliphatic alcohols can be used as a model for compartments of different lipophilic / hydrophilic properties. Thermodynamic characteristics of solvation of the drug molecules yielded by independent classical experimental methods (Gibbs energy, enthalpic and entropic terms of Gibbs energy) are studied in order to better understand diffusion and distribution properties. Correlations between in-vitro-data (partition coefficient, enthalpy of solvation) with biopharmaceutically relevant characteristics (plasma half-life) are also discussed.
Keywords: nsaid, sublimation, solvation, isothermal calorimetry, plasma half-life, solubility, passive transport, partitioning
Current Drug Delivery
Title: Solvation of Drugs as a Key for Understanding Partitioning and Passive Transport Exemplified by NSAIDs
Volume: 1 Issue: 3
Author(s): German L. Perlovich and Annette Bauer-Brandl
Affiliation:
Keywords: nsaid, sublimation, solvation, isothermal calorimetry, plasma half-life, solubility, passive transport, partitioning
Abstract: Passive transport properties of drug molecules are of utmost importance for their pharmacological and biopharmaceutical effectiveness. Diffusion in different media and through lipid bilayers is in many cases the ratedetermining step for the distribution in the body. In the present review an attempt is made to demonstrate the importance of solvation of drug molecules for the diffusion and partition / distribution in phases of different lipophilicity. Different approaches known in the literature to describe solvation of compounds with flexible conformation are discussed as well as the experimental methods to directly measure the energy of solvation. NSAIDs are chosen as an example of a class of drugs of different molecular structures that have already been studied thoroughly in many aspects, and a set of aliphatic alcohols can be used as a model for compartments of different lipophilic / hydrophilic properties. Thermodynamic characteristics of solvation of the drug molecules yielded by independent classical experimental methods (Gibbs energy, enthalpic and entropic terms of Gibbs energy) are studied in order to better understand diffusion and distribution properties. Correlations between in-vitro-data (partition coefficient, enthalpy of solvation) with biopharmaceutically relevant characteristics (plasma half-life) are also discussed.
Export Options
About this article
Cite this article as:
Perlovich L. German and Bauer-Brandl Annette, Solvation of Drugs as a Key for Understanding Partitioning and Passive Transport Exemplified by NSAIDs, Current Drug Delivery 2004; 1 (3) . https://dx.doi.org/10.2174/1567201043334786
DOI https://dx.doi.org/10.2174/1567201043334786 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...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
-
Preface [Hot Topic: Novel Therapeutics for the Treatment of Pain (Guest Editor: Kathleen R. Gogas)]
Current Drug Targets - CNS & Neurological Disorders Mechanistic and Clinical Aspects of Lenalidomide Treatment for Chronic Lymphocytic Leukemia
Current Cancer Drug Targets Proliferative Retinopathies: Animal Models and Therapeutic Opportunities
Current Neurovascular Research Distinct Functions of Interleukin-10 Derived from Different Cellular Sources
Current Immunology Reviews (Discontinued) A Phenotypic Screen for Small-Molecule Inhibitors of Constitutively Active Mutant Thrombopoietin Receptor Implicated in Myeloproliferative Neoplasms
Combinatorial Chemistry & High Throughput Screening Immunoadsorption Therapy for Patients with Dilated Cardiomyopathy and Heart Failure
Current Cardiology Reviews Rooteomics: The Challenge of Discovering Plant Defense-Related Proteins in Roots
Current Protein & Peptide Science Outcomes of Anticoagulant Therapy with Low-Molecular-Weight Heparin (LMWH) and Warfarin for Thromboangiitis Obliterans (TAO)
Current Vascular Pharmacology Thalidomide–A Notorious Sedative to a Wonder Anticancer Drug
Current Medicinal Chemistry Herb-Drug Interactions and Mechanistic and Clinical Considerations
Current Drug Metabolism Role of Ox-LDL and LOX-1 in Atherogenesis
Current Medicinal Chemistry The Inflammatory Milieu of the Degenerate Disc: Is Mesenchymal Stem Cell-based Therapy for Intervertebral Disc Repair a Feasible Approach?
Current Stem Cell Research & Therapy Preventive Effects of Mallotus japonicus Cortex Extracts on Dextran Sulfate Sodium-Induced Ulcerative Colitis in C57 BL/6J Mice
The Natural Products Journal Anti-inflammatory Property of AMP-activated Protein Kinase
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Ribozymes, DNAzymes and Small Interfering RNAs as Therapeutics
Current Drug Targets Epigenetics in Alzheimers Disease: a Focus on DNA Modifications
Current Pharmaceutical Design Editorial (Thematic Issue: GPCR-Targeted Drug Development)
Current Drug Targets Infringement of the Barriers of Cancer Via Dietary Phytoconstituents Capsaicin Through Novel Drug Delivery System
Current Drug Delivery Novel Therapeutic Approaches Targeting Matrix Metalloproteinases in Cardiovascular Disease
Current Topics in Medicinal Chemistry Alzheimer’s Disease, Astrocytes and Kynurenines
Current Alzheimer Research