Asahi Kasei – Hyaluronic acid nanogel

ceolus bannerAsahi 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.

flask asahi kaseiHA 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.

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This is what we mean by “Creating for Tomorrow.”


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See the complete video about hyaluronic acid nanogel from Asahi Kasei here:


Structure

ah nanogelHyaluronic 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

Key functions of HA nanogelThe 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 biologicsMW 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 activityLoading capacities of biologics

Retention of activity

HA nanogel protects proteins from denaturation while retaining full bioactivity.

  • Retained activity of hGH

Plasma PK of hGH after SCSustained release

Precipitation grade is suitable for subcutaneous sustained release of proteins.

  • Plasma PK of hGH after SC
  • hGH is released by addition of BSASpeculated 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 proteincaused by thermal denaturation.

 

 


Dispersion grade

Since the dispersion grade has many hydrophobic regions, it is possible to especially make complexes of poor water-soluble drugs in high volumes. In addition, since the dispersed state is maintained even under the in vivo environment, it is especially suitable as a solubilizer that can be administered intravenously.
Expected functions
  • 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)

table of HA nanogel solubilityImprovement of Solubility

  • HA nanogel can improve the solubility of poorly water-soluble drugs.

Anti-aggregation of protein

  • Anti-aggregation of proteinHA nanogel could protect conalbumin from aggregation caused by thermal denaturation.

 


Brochures

ey Functions of HA nanogel
Key functions of HA nanogel
Sustained Release and Improvement of Solubility
Sustained Release and Improvement of Solubility
Easy formulation of biologics
Easy formulation of biologics
HA nanogel - Short version_1
Hyaluronic acid nanogel – full overview
Hyaluronic Acid Nanogel as a Protein Delivery System
Hyaluronic Acid Nanogel as a Protein Delivery System

Contact

Asahi Kasei Corporation
Functional Additives Division
1-1-2 Yurakucho, Chiyoda-ku, Tokyo 100-0006 JAPAN
E-Mail: [email protected]


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