Lipid-Based Drug Delivery Systems

Lipid-based formulations are a powerful tool to increase oral bioavailability of poorly water-soluble or poorly permeable drugs. Consisting in a mixture of excipients they are easy to formulate and produce. They can be used from early-stage development to market, significantly reducing the development time.

What are the advantages of lipid-based formulations?

Poor solubility, poor permeability, and pre-systemic elimination are factors that can limit absorption of some drugs. Lipid excipients have the capability to overcome these hurdles and enhance oral bioavailability through different mechanisms.

How to develop lipid-based formulation?

An optimized LBF enables solubilization of the entire therapeutic dose and maintains the drug in solubilized state throughout the digestion process.

To speed up LBF development, we have produced tools to guide you at each stage of development:

1 – methods for saturation solubility screening

2 – database of solubility of drugs in common pharmaceutical excipients

3 – methods for miscibility and dispersability testing

4 – miscibility table

5 – in vitro lipolysis procedure

6 – guideline for preclinical studies

What are the different types of lipid-based formulations?

Depending on their composition, LBF exhibit different in vivo behaviors. They typically consist of biocompatible excipients falling into four main categories: oils, low-HLB surfactants, high HLB surfactants and co-solvents. To facilitate their identification, Pouton et al. introduced the Lipid Formulation Classification System based on the composition, size of the droplets generated after the dispersion of the formulation in aqueous media, and the impact of natural lipid digestion process on the in vivo performance of the formulation classes.

What functional excipients for oral bioavailability enhancement do Gattefossé deliver?

Our range of functional excipients includes oils, low HLB surfactants, high HLB surfactants and solvents. They can be combined to formulate all types of lipid-based formulations

What are self-emulsifying formulations?

Self-emulsifying lipid formulations form emulsions upon contact with aqueous fluids without the need for mechanical or thermal energy. The size of the dispersion depends on the composition of excipients in the formulation.

How to use lipid excipients and lipid-based formulations in early stage development?

A vehicle or formula intended for preclinical studies must allow adequate administration of the test compound with little or no effect on the test species. The vehicle or formulation must be suitable for the intended route of administration, maintain the stability of the active ingredient, and preferably, maximize the systemic bioavailability of the drug. Lipid excipients provide a solution to these challenges and have proven utility in preclinical studies. Further information is available from Gattefossé guideline