Process for preparing lipid nanoparticles

摘要

A process for preparing nanocapsules with a liquid lipid core and a solid lipid shell, charged with at least one active agent. The process contains at least the steps of formulating a microemulsion by phase inversion of an emulsion, totally or partially forming from at least one active agent a second composition different than the microemulsion, placing the microemulsion in contact with the second composition under conditions suitable for interaction of the active agent with the microemulsion, and chill-hardening the microemulsion that has interacted with the active agent, to obtain the nanocapsules.

主权项

1. A process for preparing nanocapsules by incorporating an active agent inside at least one of a liquid lipid core or a solid lipid shell of the nanocapsule, the process comprising:
contacting a microemulsion with a second oily composition under conditions suitable for promoting the incorporation of the active agent inside nanodroplets of an oily phase of the microemulsion; and chill-hardening the microemulsion charged with the active agent in order to obtain nanocapsules comprising the active agent, wherein the microemulsion is formulated by phase inversion of an emulsion through a phase inversion temperature operation, the microemulsion is free from the active agent, the microemulsion is stabilized with a surfactant system comprising a hydrophilic, nonionic, heat-sensitive surfactant, the second oily composition is totally or partially formed from the active agent to be charged, in which the second oily composition is different than the microemulsion, the active agent is either: (i) liposoluble or lipodispersible, or (ii) water-soluble or water-dispersible and in the form of inverse micellar species with a surfactant having an HLB value of less than 10, the nanocapsules have a lipid core that is liquid at room temperature, coated with a lipid shell that is solid at room temperature, and the water-soluble or water-dispersible active agent in the form of inverse micellar species, or the liposoluble or lipodispersible active agent, is incorporated inside the liquid lipid core, the solid lipid shell, or both, of the nanocapsules.