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Published on: September 20, 2017
Arginine-assisted solubilization system for drug substances: solubility experiment and simulation
Atsushi Hirano1, Tomoshi Kameda, Tsutomu Arakawa
1Institute of Applied Physics, University of Tsukuba, Tsukuba, Ibaraki 305-8573, Japan.
The Journal of Physical Chemistry. B
|October 8, 2010
Summary
Arginine significantly enhances aqueous solubility of poorly soluble drugs, unlike lysine. This arginine-assisted solubilization system (AASS) shows promise for drug formulation, particularly for compounds with aromatic rings.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Physical Chemistry
Background:
- Poor aqueous solubility is a major challenge in drug development, limiting the efficacy and application of many drug substances.
- Developing effective strategies to improve drug solubility is crucial for advancing pharmaceutical formulations.
Purpose of the Study:
- To introduce and evaluate a novel arginine-assisted solubilization system (AASS) for enhancing the aqueous solubility of poorly soluble drug substances.
- To investigate the efficacy of arginine compared to lysine in improving the solubility of model drug substances (alkyl gallates).
Main Methods:
- Solubility experiments were conducted using alkyl gallates as model drug substances in the presence of arginine and lysine.
- Molecular dynamic simulations were employed to elucidate the interaction mechanisms between the amino acids and the model drug substances.
Main Results:
- Arginine demonstrated a significant increase in the aqueous solubility of various alkyl gallates, irrespective of their differing solubilities.
- Lysine exhibited only marginal effects on the solubility of alkyl gallates.
- Molecular dynamic simulations revealed stronger interactions between arginine and alkyl gallates, attributed to the guanidinium group of arginine and the aromatic ring of the drugs, disrupting drug aggregation.
Conclusions:
- The arginine-assisted solubilization system (AASS) is a highly effective strategy for improving the aqueous solubility of poorly soluble drug substances.
- This approach is particularly promising for drugs containing aromatic ring structures, offering a potential solution for formulation challenges.
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