Production of lipophilic nanogels by spontaneous emulsification

Nanosized gel particles, so-called nanogels, have attracted substantial interest in different application fields, thanks to their controllable and three-dimensional physical structure, good mechanical properties and potential biocompatibility. Literature reports many technologies for their preparation and design, however a recurrent limitation remains in their broad size distributions as well as in the poor size control.

Therefore, the monodisperse and size-controlled nanogels preparation by simple process –like emulsification– is a real challenge still in abeyance to date. In this study we propose an original low energy emulsification approach for the production of monodisperse nanogels, for which the size can be finely controlled in the range 30 to 200 nm. The principle lies in the fabrication of a direct nano-emulsion containing both oil (medium chain triglycerides) and a bi-functional acrylate monomer. The nanogels are thus formed in situ upon UV irradiation of the droplet suspension. Advantage of such modification of the oil nano-carriers are the potential modulation of the release of encapsulated drugs, as a function of the density and/or properties of the polymer chain network entrapped in the oil nano-droplets.

This hypothesis was confirmed using a model of hydrophobic drug –ketoprofen– entrapped into the nanogels particles, along with the study of the release profile, carried out in function of the nature of the monomers, density of polymer chains, and different formulation parameters.

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Materials: Medium chain triglycerides (MCT, Labrafac® WL 1349) was purchased to Gattefossé S.A., Saint-Priest, France. Tri(propylene glycol) diacrylate (TPGDA), ethyl acrylate (EA), n-butyl acrylate (nBA), 1-hydroxycyclohexyl phenyl ketone (HCPK, as photoinitiator, 99% purity) were obtained from Sigma-Aldrich. Water used was milliQ water, and a nonionic hydrophilic surfactant (Kolliphor ELP®) was purchased from BASF, Ludwigshafen, Germany. It is a polyethoxylated-35 castor oil with a Hydrophilic-Lipophilic Balance (HLB) of 12 ~ 14. Ketoprofen was obtained from S.I.M.S (Florence, Italy).

Article information: Shukai Ding, Bilal Mustafa, Nicolas Anton, Christophe A. Serra, Delphine Chan-Seng, Thierry F. Vandamme, Production of lipophilic nanogels by spontaneous emulsification, International Journal of Pharmaceutics, Volume 585, 2020. https://doi.org/10.1016/j.ijpharm.2020.119481.