Arginine-assisted solubilization system for drug substances: solubility experiment and simulation.
Summary of "Arginine-assisted solubilization system for drug substances: solubility experiment and simulation."
The poor aqueous solubility of drug substances hampers their broader applications. This paper describes a de novo strategy to increase the aqueous solubility of drug substances using an arginine-assisted solubilization system (AASS) with alkyl gallates as model drug substances. Solubility experiments of alkyl gallates showed that arginine greatly increases the aqueous solubility of different alkyl gallates, whose aqueous solubilities differ widely. In contrast, lysine showed marginal effects on alkyl gallates solubility. Molecular dynamic simulation indicated a greater interaction of arginine with alkyl gallates than that of lysine, which reflects favorable interaction between the guanidinium group of arginine and the aromatic ring of alkyl gallates. Such interaction apparently disrupts association of alkyl gallate molecules, leading to solubilization. These results indicate AASS as a promising approach to solubilize poorly soluble drug substances containing aromatic ring structures.
Affiliation
Institute of Applied Physics, University of Tsukuba, Tsukuba, Ibaraki 305-8573, Japan.
Journal Details
This article was published in the following journal.
Name: The journal of physical chemistry. B
ISSN: 1520-5207
Pages: 13455-62
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/20925397
- DOI: http://dx.doi.org/10.1021/jp101909a
Medical and Biotech [MESH] Definitions
Drug Therapy, Computer-assisted
Adjunctive computer programs in providing drug treatment to patients.
Drug Carriers
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
Chemical Fractionation
Separation of a mixture in successive stages, each stage removing from the mixture some proportion of one of the substances, for example by differential solubility in water-solvent mixtures. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Drug Design
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Equine-assisted Therapy
Therapy assisted by the use of a horse and/or its movement, including equine-assisted psychotherapy, horseback riding, and hippotherapy.
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