Why consider a lipid-based drug delivery system (LBDDS)?
- LBDDS should be considered when conventional formulations provide insufficient bioavailability.
- LBDDS are versatile; they include the use of lipids and lipid technologies in pharmaceutical formulations intended for various routes of administration, e.g., oral, transdermal, parenteral, rectal, ocular, etc.
- According to the American Association of Pharmaceutical Scientists (AAPS), lipid-based systems are used for a number of reasons:
- to impact systemic or local drug disposition by impacting solubility, permeability, absorption, distribution, and metabolism;
- to produce physically and chemically stable formulations that offer a safe and effective means to deliver drugs to the intended site of absorption or action; and
- to overcome patient compliance obstacles by improving taste, overall palatability, dosing frequency, and/or tolerability.
Approximately 90 percent of molecules in the discovery pipeline, and approximately 40 percent of drugs with market approval, are poorly water soluble. Advanced delivery technologies, like lipid-based systems, are an alternative solution to safely and effectively deliver the proper therapeutic dose to patients.
Unlike conventional tablets or powder-filled capsules, LBDDS can present the drug compound in a solubilized state, eliminating dissolution rate limited absorption and improving bioavailability. For highly potent drugs, dosage form content uniformity may also be improved. Lastly, LBDDS may circumvent hepatic first-pass metabolism by promoting lymphatic transport.
“However, the range of lipidic excipients and the abundance of factors that go into determining which combinations of lipids, cosolvents, and surfactants to select makes LBDDS a complex, formulation-dependent technology. Know what criteria to consider when selecting a CMO to handle LBDDS manufacturing.”