Enavail’s proprietary Controlled Precipitation (CP) and Rapid Freezing (RF) processes provide the Enavail engineering team flexibility in designing a solution with the highest bioavailability, highest potency, and tailor made for your route of administration. Equally important – the Enavail technologies offer an economical and scalable solution for getting your compounds to market.

Currently, about 30% of drugs that appear on the World Health Organization (WHO) Essential Drug List were reported to be poorly water-soluble, based on the Biopharmaceutics Classification System (BCS) [1, 2]. Furthermore, over 40% of newly developed pharmaceutically active substances have solubility issues [3]. The poor dissolution and/or permeability of these drugs often result in low and highly variable bioavailability. The major obstacle of successfully commercializing these compounds is the difficulty of enhancing their dissolution rate and extent of dissolution.

Particle engineering can allow for increased surface area and wetability for enhancement of bioavailability. However, numerous challenges exist with other particle technologies, including economic viability and scalability.

In addition, many employ harsh conditions, making them unsuitable for labile compounds. Other disadvantages include low potency and limitations on route of administration.

Enavail’s Particle Engineering Technologies (Rapid Freezing and Controlled Precipitation) focus on designing nano-structured drug particles with increased surface area and thermodynamic potential, which allow for enhanced dissolution of poorly water-soluble drugs and improved bioavailability. Administration of these compositions can produce high supersaturation levels rapidly in biological fluid. Pulmonary delivery of these compositions can also provide improved lung local drug exposure and potentially reduce dose and systemic side effects. The flexibility and versatility of these processes allow for the use of a wide variety of FDA approved and generally regarded as safe (GRAS) biodegradable and biocompatible excipients which can also enhance the stability, patient compliance, safety, and therapeutic efficacy of these drugs [4].

Enavail’s Precise Control of Sub-Micron Processed API Particles

The Enavail Technologies were used to produce highly controlled, sub-micron particles of both Cyclosporin A and Danazol. Bulk Cylcosporin A was processed using the Controlled Precipitation method whereas the Rapid Freezing technology was used to process the bulk Danazol.