Curative medicine, Diagnostic products

## Life Sciences

# Development of the absorption enhancement technique for pharmaceutical compounds using solid in oil (S/O)

Keyword: Nano-dispersion by S/O, Absorption enhancement, Feasibility study (FS)

## Organizations Involved

Masahiro Goto, Professor, Faculty of Engineering, Kyushu University

☐ Takeru Fujii, Ph. D. President, ASPION Co., Ltd.

☐ Megumi Takata, Director, IMAQ & Kyushu TLO Co., Ltd.

Prof. Goto

President Fujii

Mr. Takata

## 【Abstract】

Prof. Goto found that pharmaceutical compounds show the enhanced permeation through the biomembrane when nano-dispersed into oily base after included in the reversed micelles, based on the basic research of enzymatic reaction under the hydrophobic condition. ASPION Co., Ltd. has the exclusive right for commercialization through Kyushu University's TLO (Kyushu TLO Co., Ltd.), and develops the business in the field of pharmaceuticals, cosmetics, and health foods.

## [Summary of the technology transfer]

## Technological Impact

Hydrophilic compounds generally show lower absorption rate through biomembrane compared to hydrophobic compounds. But, it was discovered that hydrophilic compounds show the enhanced oral absorption or transdermal absorption when nano-dispersed into oily base after included in the reversed micelles. Moreover, biomembrane is protected from the irritation damage due to the bio-coat structure of S/O (pseudo-membrane). And then, drug compounds show the enhanced stability because of the decrease in hydrolysis.

## Market Impact

The technique is applied to the screening of the new chemical entity, but also to the renewal of the dosage form or additional dosage form for the extended market life. Therefore, we are now planning to contract the FS tests with many pharmaceutical companies and cosmetic companies.

## Special Features of the Collaboration

## ● Social Impact

Using the technique, injection could be changed to oral dosage form or transdermal dosage form, and the elaborated QOL will be expected. While, hydrophilic compounds having better pharmacokinetic profile could be screened when the technique will be applied to the drug candidate.

The research collaboration with Kyushu University helps ASPION's commercialization process and creating the good relationship with pharmaceutical companies.

## Project Background

When Takeru Fujii, the president of ASPION, visited the laboratory of Prof. Goto, he was deeply impressed that the appearance of proteins clearly dissolved in vegetable oil and decided to apply this technology for pharmaceutical products.

## Funding History

-Consortium R&D project

2. 2001-2004

-Sakigake 21 by JST

3. 2004-2006

-Regional R&D project by JST

## I ntellectual property protection

Patent Filed : JP 1, International 2 "O/W emulsion dosage form (JP2004-043355)", etc.

## Schematic graph of Solid in Oil (S/O)

Oily surfactant

Water soluble compound

Solubilization of protein (HRP) into oil phase.

Left: HRP included in S/O was dissolved in oil phase.

Right: HRP was precipitated.

## Turning point in the Project

ASPION Co., Ltd. and Kyushu TLO Co., Ltd. smoothly signed an exclusive licensing agreement with an equity scheme in early stage. Now, ASPION Co., Ltd. is commercializing and offering the proposal of S/O technology to companies in pharmaceutical, cosmetic, health food, and other relevant field.