Pharmaceutical Nanosuspensions with Improved Bioavailability

Nanosuspensions prepared by sonication show a significant improved pharmacological bioavailability. Especially drug molecules with poor water-solubility, which reduces its bioavailability and effect onset, benefit from the nanosizing technique of ultrasonication. Ultrasonication is used reduce drug particles and crystals to nanometer size and to prepare stable nanosuspensions with superior drug bioavailability and effectiveness.

Improved Drug Bioavailability with Sonication

Poorly soluble pharmaceutical molecules have a very low bioavailability and therefore a low efficacy especially when administered orally. When such drugs with low water-solubility are nano-sized and formulated into nanosuspensions, bioavailability can be increased dramatically. For instance, for azithromycin nanosuspensions more than 65% drug was dissolved in 5 hours in comparison to merely 20% dissolution of micronized azithromycin.
Ultrasonication is a highly efficient method to reduce particle size, to precipitate nano-crystals and to disperse active pharmaceutical ingredients into nanosuspensions. Such nanosuspensions consist solely in the pure pharmaceutical active compound.
Additionally, nanosized drug molecules and nanosuspensions are simple to incorporate into various dosage forms like tablets, capsules, and fast melts.

Ultrasonic Preparation of Meloxicam Nanocrystals

Meloxicam, a commonly prescribed non-steroidal anti-inflammatory drug (NSAID), has only poor water-solubility, which reduces its bioavailability and effect onset. Ultrasonication is used to micronize and nanosize meloxicam crystals and to prepare stable nanosuspensions with superior drug bioavailability and effectiveness.

Microscopic images of meloxicam suspension:
Left: untreated meloxicam suspension
Right: Meloxicam nanosuspension obtained by ultrasonication with the UP100H for 45 minutes at 100% amplitude and cycle 1.

Iurian et al. (2015) investigated the effects of sonication on meloxicam crystals and their corresponding bioavailability. The demonstrated that the most important influencing factor for the preparation of meloxicam nanocrystals is the ultrasound amplitude.
The amplitude and the time were found as the most important variables. Their increase determined significant size reduction and homogeneity due to cavitation phenomenon, while the applied cycle was less important. The crystal size greatly influenced dissolution; a strong correlation was noted between small crystals and fast dissolution after freeze-drying the nanosuspensions. The optimal formulation was obtained by continuous sonication at 100% amplitude for 45 minutes, conditions which led to 600 nm crystals with 0.521 polydispersion index and fast drug dissolution. The morphological analysis revealed small, round-shaped crystals with narrow size distribution.

Higher amplitudes result in the most effective meloxicam nanocrystals preparation.

High-Performance Ultrasonic Homogenizers for Nanosuspensions

Hielscher Ultrasonics is your trustworthy supplier for reliable high-performance ultrasonic equipment from lab and pilot to full-industrial systems. Hielscher Ultrasonics’ devices feature sophisticated hardware, smart software and outstanding user-friendliness – designed and manufactured in Germany. Hielscher’s robust ultrasonic machines for dispersion, deagglomeration, nanoparticle synthesis and functionalization can be operated 24/7/365 under full load. Depending on your process and your production facility, our ultrasonicators can be run in batch or continuous in-line mode. Various accessories such as sonotrodes (ultrasonic probes), booster horns, flow cells and reactors are readily available.
Contact us now to get more technical information, scientific studies, protocols and a quotation for our ultrasonic homogenizers for the production of nanosuspensions containing pharmaceutical nanocrystals or nanoparticles! Our well-trained, long-experienced staff will be glad to discuss your nano-application with you!

The table below gives you an indication of the approximate processing capacity of our ultrasonicators:

Sonofragmentation of acetylsalicylic acid (aspirin) crystals
[study and pictures: ©Zeiger and Suslick, 2011]