Physical and chemical gels of lipid nanoparticles for controlled delivery of lipophilic drugs and proteins

摘要

The controlled delivery of drugs and biologicals (proteins, antibodies, DNA and derivatives) is a growing need to take the full benefit of new therapeutic strategies. However these new molecules or biomolecules display solubility issues, or high degradation rates once injected. Therefore, both suitable delivery materials for their encapsulation and protection from the surrounding environment, and smart delivery devices (such as micro-needles or implanted pumps) are necessary to achieve controlled delivery of these precious therapeutic agents. We have developed bio-inspired gel materials, based on lipid nanoparticles which act as reservoirs for lipophilic drugs. The lipid nanoparticles, termed lipidots™, are biocompatible, colloidally stable, non-immunogenic, and obtained from a cheap and simple solvent-free process. The particles can be assembled to form physical or chemical gels, with tunable rheological properties. Physico-chemical studies have been carried out to determine the limits of the stability domains for colloidal and gel formulations (choice of surfactants for nanoparticle surface, and composition ratios of lipids, surfactants and co-surfactants). In particular, it is demonstrated that lipid nanoparticles keep their integrity in the gels. Gels of lipidots™ could therefore constitute biocompatible materials for the efficient encapsulation and tuned delivery of lipophilic drugs and biomolecules.