Download: A Guide to Bioavailability Enhancement

Bioavailability Enhancers

Enhancement techniques ensure that a pharmacological product will be bioavailable at optimal quantities at the desired location site. These “drug facilitators,” when combined with an API, enhance drug activity by increasing drug absorption.

Physical enhancers, such as particle engineering, manipulate an oral drug’s physical form to enhance bioavailability. Solid Dispersion (SD) and nanosuspension are two popular methods for physically manipulating a particle. In SD, drugs interact with hydrophilic carriers, decreasing agglomeration, and release in a supersaturation state for rapid absorption and improved bioavailability. Nanosuspension facilitates particle size by increasing the surface area to volume ratio. A higher surface area to volume ratio enables nanosuspension-based drugs to rapidly dissolve in the body.

Chemical enhancers, such as lipids and inclusion-complexes, can act as release-rate modifiers, stabilizers, solubilizers, and bioavailability enhancers. For example, Lipid-based drug carriers can, enhance solubilization in the GI tract and reduce variability of systemic exposure. Inclusion-complex delivery systems, such as cyclodextrin derivatives, interact with molecules to form a non-covalent inclusion complex, resulting in increased bioavailability.

The Patient Impact on Bioavailability

Ideally, a drug should be tested on patients diagnosed with the disease for which the drug is being developed. Drug sponsors will often turn to multi dose studies to determine if bioavailability is at a steady state in patient volunteers and to determine the drug absorption pattern. But there are many patient factors that can influence drug absorption, including other drugs the patient may be taking, the foods they eat, and their genetics. Without a strong scientific understanding of these factors, as well as patient physiology, finding the best formulation can delay your clinical progress.

Partnering With a CDMO to Enhance Bioavailability

Pharma is increasingly turning to skilled contract development and manufacturing organizations (CDMOs) for their level of technological innovation in determining the best formulation for a drug candidate. In fact, a growing number of CDMOs have broadened their offerings to tackle bioavailability enhancement challenges to accelerate the development pathway.

Hence, selection of the right CDMO that has the overall Pharmaceutics Know-How™ to offer a range of technologies, is important at the early development stages as well as ability to scale these processes for ultimate commercialization.