Asahi Kasei – Hyaluronic acid nanogel
Asahi Kasei has established industrial manufacturing technology for hyaluronic acid (HA) nanogel as a new pharmaceutical excipient, and is providing samples to prospective customers in order to commercialize the product.
HA nanogel is expected to improve the quality of life (QOL) for patients by enabling the low-toxicity solubilization of insoluble drugs, facilitating the formulation of biopharmaceuticals such as proteins and peptides by suppressing their aggregation and denaturation, and reducing the frequency of injection when repeated administration is required.
The commitment of the Asahi Kasei Group
To do all that we can in every era to help the people of the world make the most of life and attain fulfillment in living. Since our founding, we have always been deeply committed to contributing to the development of society, boldly anticipating the emergence of new needs.
This is what we mean by “Creating for Tomorrow.”
Asahi Kasei: Creating for tomorrow
See the complete video about hyaluronic acid nanogel from Asahi Kasei here:
Structure
Hyaluronic acid nanogel is derived by the partial modification of hyaluronic acid with cholesterol. In water, self-association occurs among the cholesterol portions due to hydrophobic interaction, causing the formation of nanometer-scale hydrogel. The physical properties of HA nanogel depend on the molecular weight of HA and the cholesterol modification rate. Three grades of samples, a dispersion grade, a precipitation grade and an emulsification grade, are currently available.
Functions
The hydrophobic interaction enables a wide variety of insoluble drugs, ranging from low and medium molecular weight (MW) compounds to proteins, to be enclosed in the nanogel by simple mixing. This makes hyaluronic acid nanogel suitable for use as a base material for DDS. The main functions are sustained release, solubilization, suppression of aggregation, and retention of drug activity. Grades can be optimized to match specific customer requirements.
The different grades of hyaluronic acid nanogel:
Emulsification grade
The emulsification grade is suitable for coating and emulsifying the drug surface because it adsorbs to the hydrophobic surface of the drug particles.
Expected functions
- Emulsification of drug particles
Properties
- MW of HA 5 – 20 kD
- DS of cholesterol 5 – 10 unit mol %
- Particle size (PDI) 20 – 50 nm (0.3)
Precipitation grade
The precipitation grade can especially make protein or peptide complexes in high volumes. Furthermore, since precipitation occurs under the in vivo environment, it is especially suitable for subcutaneous sustained release.
Expected functions
- In situ depot sustained release
- Retained biological activity
- Inhibition of aggregation
- High loading capacity (20–40 w/w%)
Properties
![Easy formulation of biologics]()
MW of HA 25 – 40 kD- DS of cholesterol 10 – 20 unit mol %
- Particle size (PDI) 50 – 100 nm (0.3)
Easy formulation of biologics
Various drug molecules can be encapsulated by just mixing in water.
![Retention of activity]()
Loading capacities of biologics
Loading capacities of biologicsRetention of activity
HA nanogel protects proteins from denaturation while retaining full bioactivity.
- Retained activity of hGH
Sustained release
Precipitation grade is suitable for subcutaneous sustained release of proteins.
- Plasma PK of hGH after SC
![hGH is released by addition of BSA]()
Speculated mechanism of sustained release from HA nanogel
hGH is released by addition of BSA
Anti-aggregation of protein
- HA nanogel could protect conalbumin from aggregation
![Anti-aggregation of protein]()
caused by thermal denaturation.
Dispersion grade
- Improvement of solubility
- Inhibition of aggregation
- High loading capacity (5–15 w/w%)
Properties
- MW of HA 5 – 20 kD
- DS of cholesterol 30 – 50 unit mol %
- Particle size (PDI) 20 -50 nm (0.3)
Improvement of Solubility
- HA nanogel can improve the solubility of poorly water-soluble drugs.
Anti-aggregation of protein
![Anti-aggregation of protein]()
HA nanogel could protect conalbumin from aggregation caused by thermal denaturation.
Brochures
Contact
Asahi Kasei Corporation
Functional Additives Division
1-1-2 Yurakucho, Chiyoda-ku, Tokyo 100-0006 JAPAN
E-Mail: [email protected]