Bacillus-derived Hyaluronic acid from Novozymes Biopharma, Hyasis®, increases in vitro drug release time from under 10 minutes to approximately 15 hours

An investigation undertaken by Novozymes Biopharma DK has shown that when the corticosteroid dexamethasone is formulated in a cross-linked Hyaluronic acid (HA) hydrogel, the drug’s in vitro release time increases from under 10 minutes to approximately 15 hours. In addition, the in vivo half-life of dexamethasone is shown to plateau with stable dexamethasone concentration up to four hours after injection.

Hyasis^®, the Bacillus-derived HA used in the investigation was formulated by Novozymes Biopharma DK, which is part of world leader in bioinnovation, Novozymes A/S. The findings support the development of sustained release formulations consisting of cross-linked HA hydrogels and dexamethasone, and will be presented at the 2013 Controlled Release Society (CRS) annual meeting, July 21-24, Hawaii USA.

“We are delighted with these results,” commented Hans Ole Klingenberg, Global Marketing Director of Novozymes Biopharma. “By offering pharmaceutical manufacturers more control over drug release, dosing frequency can be reduced and stable levels can be maintained in the body, increasing patient safety and compliance.”

Experimentally, the in vitro drug release was assessed using a USP 4 dissolution method with a closed loop configuration. The pharmacokinetics of dexamethasone were tested further after administration to Sprague Dawley rats, who had blood drawn at different time intervals. The amount of drug present was analysed by LC-MS. Results were compared with those of dexamethasone formulated in a PBS buffer, revealing a significant increase of in vitro release times. The in vivo half-life data showed an initial plateau in dexamethasone plasma concentration when it was formulated with cross-linked HA hydrogels, indicating a slow release of dexamethasone in comparison to dexamethasone formulated with PBS buffer.

Novozymes Biopharma’s Hyasis^® is an ultra-pure material with exceptionally low amounts of nucleic acids, proteins, bacterial endotoxins and microbial contamination. With a reproducible molecular weight and narrow size distribution, it is well-tolerated, safe and biocompatible, allowing the sustained and controlled release of drugs in a HA concentration dependent manner.

For further information on Novozymes’ range of innovative drug delivery products or to request a copy of the scientific poster, please visit booth 416 at the 2013 CRS meeting or www.biopharma.novozymes.com