As surface area increases, the rate of dissolution increases and bioavailability improvements may result. If a solid dosage form is desired, the nano-particles are stabilized by adsorption onto polymer carriers – a process conducted by fluid bed coating.  Alternatively, the nano-particles can be prepared as a suspension and administered as a liquid – either orally or by injection.

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.

Lipid-Based Nano-Particles

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.

The figure shows the morphology of the lipid nano-particles.

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.

Ascendia specializes in the application of nano-technology approaches to develop novel pharmaceutical products.  Our suite of state-of-the-art technologies for formulating poorly water soluble compounds provides sophisticated formulation options for our clients.  Contact us today for more information on how our formulations can enable your pharmaceutical product.