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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

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The Rational Selection for Solubilized Formulation Technologies Utilizing Physicochemical Properties.

Kouya Kimoto¹, Katsuhiko Yamamoto^2,3, Toshiro Fukami⁴

¹Analytical Development, Pharmaceutical Sciences, Takeda Pharmaceutical Company Limited, 2-26-1 Muraoka-Higashi, Fujisawa, Kanagawa 251-8555, Japan.

Chemical & Pharmaceutical Bulletin

|September 18, 2025

Summary

Selecting drug formulation technologies like amorphous solid dispersion (ASD), lipid-based formulation (LBF), and nanocrystals (NC) can be guided by molecular properties. This study identifies key indicators for optimizing early-stage drug development and accelerating timelines.

Keywords:

amorphous solid dispersion cyclodextrin lipid-based formulation nanocrystal physicochemical property solubility

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Area of Science:

Pharmaceutical Sciences
Drug Delivery
Formulation Development

Background:

Improving solubility of poorly water-soluble drugs is crucial for oral small-molecule drug development.
Lack of objective indicators hinders the selection of appropriate solubilized formulation technologies.
Early-stage selection of formulation technologies impacts development timelines.

Purpose of the Study:

To establish selection indicators for amorphous solid dispersion (ASD), cyclodextrin (CD), lipid-based formulation (LBF), and nanocrystal (NC) technologies.
To utilize molecular properties for guiding formulation technology selection.
To accelerate early-stage drug development by providing rational selection criteria.

Main Methods:

Analysis of molecular properties (molecular weight, melting point (T_m), Log P, polar surface area (PSA)) of marketed oral drugs.
Utilizing single-property and multiple-property plots for data visualization.
Developing a combined property plot (T_m and normalized Log P/PSA) to identify optimal formulation ranges.

Main Results:

Single-property plots indicated frequency distributions for molecular properties.
A multiple-property plot identified an optimal selection range for ASD, LBF, and NC technologies.
Cyclodextrin (CD) technology was found to be outside the identified optimal range based on the analyzed molecular properties.

Conclusions:

Molecular property analysis provides objective indicators for selecting solubilized formulation technologies.
The developed indicators can guide the rational selection of ASD, LBF, and NC for early-stage drug development.
This approach facilitates accelerated development timelines by leveraging early-stage molecular data.