Ascendia uses a bead-milling process for production of nano-particles, and can investigate the impact of nanonization with small amounts of drug substance. Ascendia’s nano-particle technology can enable pharmaceutical products with enhanced bioavailability, reduced food-effect and more rapid onset-of-action.
Dissolution of poorly soluble drugs can be further improved by formulating the nano-particle as a homogenous mixture of the drug and a lipophilic excipient. By combining the drug with a lipid carrier, the energy required for the drug to dissolve in the body is greatly lowered.
CASE STUDY – ASD-005
ASD-005 is a weakly basic cardiovascular drug with a low solubility in aqueous media. Currently it is only available as an oral dosage form. An injectable nano-particle formulation was developed for use in an acute care setting. The drug substance in nanoparticle form is stabilized using lipid excipients to enhance the drug loading and to achieve a sustained release in vivo. The process involves the homogenous mixture of drug and lipids, and nano-sizing in a parenteral grade vehicle. Three prototype formulations were prepared with different drug loadings (drug weight/solution volume). The table shows the nano-particle size and drug loading for the three formulations.
A sustained release PK profile with a enhanced bioavailability was achieved in an animal study over a 24 hour period following IV injection of the nano-particle formulation.
In-vitro Dissolution of Nano-particles (at 37°C)