固体自発的乳化製剤を用いた難水溶性薬物の粘液透過促進のためのナノエマルション形成

抄録

Nanoemulsions have been employed as one of the methods for nano-dispersing poorly water-soluble drugs in mucus. However, most liquid suspension such as the emulsions is washed by the clearance effect on the mucus surface. This study examined the spontaneous emulsification formulation using porous polymer microparticles with mucosal adhesion as the technology for drug permeation enhancement. The nanoemulsion formation expected in this technology could be realized using medium-chain fatty acid triglyceride as the oil component. Moreover, the spontaneous emulsification and the diffusion of the nanoemulsion in mucus proceeded smoothly by using porous particles composed of anionic polymers that have little interaction with mucus components, because mucus is composed of anionic polymer, mucin. It was anticipated that the fine emulsions prepared by this method would enhance drug transport in mucus.