WHITEPAPER – Accelerate Preclinical Developments & Improve Oral Bioavailability With Lipid-Based Formulation & Encapsulation Technology Combination

Owing its convenience, oral administration is patients’ preferred route of delivery for therapeutic molecules. However, most New Chemical Entities (NCE) exhibit physico-chemical properties limiting their absorption in the gastro-intestinal (GI) tract. Indeed, according to Pharmacircle data from March 2022, almost 70% of identified molecules face solubility issues in aqueous GI fluids. Therefore, they require formulation strategies to boost their solubility in biorelevant conditions and meet their therapeutic effect.

Numerous options exist to enhance oral bioavailability of these poorly water-soluble (PWS) drugs [1]. Among them, lipid-based formulations (LBF) represent an interesting approach for their ease of development and manufacturing. Although LBF are mostly known for their ability to increase oral bioavailability of grease ball like Active Pharmaceutical Ingredient (API) (high log P1, low melting point), recent publications indicate promising results to also increase oral bioavailability of brick dust like small molecules (high log P, high melting point) as well as macromolecules such as peptides and proteins.

As LBF are composed of liquid or semi-solid excipients into which API are either dissolved or dispersed, capsules are the most convenient dosage forms for their administration.

This paper covers the benefits of the LBF and capsules combination in dosage form developments, an efficient technology platform to bring efficient and differentiated products to the market.