The challenges facing the successful formulation of poorly soluble, lipophilic active pharmaceutical ingredients (APIs) can be complex and multifactorial. Perhaps the most critical barriers to overcome in a successful formulation are enhanced drug permeation and increased bioavailability of the active. While there are approaches capable of improving drug dissolution, there are relatively few that can improve drug permeability, claims Dr. Donald Kelemen, Head of Corporate Business Development, ABITEC Corp. Rarer still are excipients that improve dissolution and permeability, are part of


normal human physiology, and are capable of negating the food effect and protecting the API from degradation in the GI tract. “Functional lipid excipients can provide for all of these benefits,” says John K. Tillotson, RPh, PhD, Pharmaceutical Technical Business Director, ABITEC Corp. “By dissolving the API in a lipid-based pre-concentrate, an oil-in-water emulsion can be generated in the GI tract with the active ingredient molecularly dissolved or dispersed in the lipid phase of a micellar system.” Depending upon composition, these micelles can offer several functional advantages, including serving as a protective environment for the API, instilling permeation enhancement for polar actives through reversible tight junction modulation, and as a substrate for mitigating the impact of P-glycoprotein efflux.

ABITEC develops lipid-based excipients to enhance bioavailability of poorly water soluble and poorly permeable molecules for the pharmaceutical industry. The excipients are manufactured in accordance with strict cGMP and applicable IPEC (International Pharmaceutical Excipient Council) guidelines in ISO-certified facilities. Recently, ABITEC has expanded its manufacturing capabilities to provide greater flexibility to serve our customers throughout development from preclinical to commercialization.


“ABITEC supports the needs of the formulators by developing and providing applications research, investing in manufacturing agility, and innovating to develop new product lines that meet the changing demands of our customers,” says Dr. Tillotson. “Through research partnerships with major universities, we develop new applications papers and guidance on solubility, phase behavior, and permeability of functional lipid formulations that are available to formulators and provide a starting point for formulation development.”

Check out Drug Development & Delivery’s SPECIAL FEATURE – Bioavailability & Solubility: New Approaches to Enhance Drug Performance featuring ABITEC.

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