White Paper

Microemulsion Capsule Technology To Optimize Drug Delivery

Source: Capsugel, a Lonza Company

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White Paper: Microemulsion Capsule Technology To Optimize Drug Delivery

While it seems that a new drug launch draws all the attention to the specific drug substance, it is clear that the authorities only approve a drug product which contains more than just the specific drug substance alone. In reality, the drug product is a combination of the drug, a formulation of functional excipients and their processing. The formulation and processing is critical for the pharmacokinetic profile of the drug substance in vivo, which is part of its efficacy and safety. The optimal efficacy and safety is dependent on the drug concentration at the receptor site, the input rate and the duration of receptor interaction. In a recent draft guideline the FDA addresses the need to evaluate the pharmacokinetic-pharmacodynamic correlation to develop the optimal drug delivery system in terms of maximised efficacy and safety profile for the drug substance.

According to the Biopharmaceutics Drug Classification (BCS), drugs are classified according to their aqueous solubility and membrane permeability. Drugs with poor solubility but high permeability are classified as ‘Class 2' compounds. Their oral bioavailability can be expected to be dependent on the solubilisation kinetic in the gastric juice of the GI tract.

A formulation for a ‘Class 2' drug will focus on solubility enhancement or solubilisation to improve the bioavailability and pharmacokinetic profile. Many different technologies have been proposed, especially particle size reduction to the nanometer range and solid dispersions. About a decade ago, self-emulsifying drug delivery systems (DDS) entered into the pharmaceutical development scene as a potential technology to enhance oral bioavailability.

The basic concept of self-emulsifying DDS is to deliver the drug in solution to the site of absorption or to protect the drug from being substantially metabolised in the gastro-intestinal tract or the gut membrane.

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White Paper: Microemulsion Capsule Technology To Optimize Drug Delivery