Lipophilic systems have proven effectiveness in improving bioavailability by helping drugs to overcome problems like poor gastric solubilisation, degradation and elimination due to first-pass metabolism in the liver, other types of pre-systemic metabolism, and drug transport and efflux effects.
At Quay Pharma, we are highly experienced in identifying the most suitable lipid excipients for the challenges of dispersion, dissolution or digestion that your drug may be encountering, and then developing suitable formulations using oils or surfactant-based systems. We take prototype formulations through comprehensive in vitro testing and characterisation, enabling us to manufacture an optimised product for clinical studies that will give your drug product the best chance of success. We have a wide choice of proven technologies available.
To enhance drug solubility:
- The surfactant properties of self emulsifying and self micro-emulsifying drug delivery systems (SEDDS and SMEDDS) can be used to improve the dispersion and solubilisation of drugs in the gastrointestinal tract.
- The digestion of lipid excipients (oils and surfactants) in combination with the drug product can improve solubilisation and absorption in the gastrointestinal tract.
To enhance drug absorption, lipid excipients can be used:
- To act upon the enterocyte-based transport mechanisms, for example by inhibiting the P-glycoprotein efflux transporter that controls drug uptake and efflux.
- To facilitate uptake by the lymphatic transport system, thereby eliminating first-pass metabolism in the liver and improving bioavailability.
- To inhibit pre-systemic enzyme activity, notably from the P450 enzymes, that can increase the cellular concentration of the drug.