Nano-Particle Technology

NanoSol is a technology for the production of nano-sized drug particles.     Formulation of a drug substance in nano-particle form significantly increases the surface area available for dissolution.  A ten-to-twenty-fold increase in surface area can result from reducing particle size from a micronized drug substance to a nanonized drug substance.

surface area

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.

plasma concentration

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

medicine pillsDissolution 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.


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.

formulation table

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

Morphology of Nano-particles

Morphology of Nano-particles (via SEM)

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)

In-vitro Dissolution of Nano-particles (at 37°C)

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.

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