엔잘루타마이드의 용해도 개선을 위한 고형의 자가나노유화 약물전달시스템

Abstract

The objective of this study was to develop a novel enzalutamide-loaded solidified self-nanoemulsifying drugdelivery system formulation with enhanced solubility and dissolution rate. Various oil and surfactant were screened, thenMedium Chain Triglyceride oil and Polysorbate 80 and Labrafil M2125CS were selected as oil and a surfactant. Pseudoternaryphase diagram was constructed to detect the nanoemulsion zone. Among the SNEDDS formulations tested,SNEDDS consisted of MCT oil (oil), Polysorbate 80 (surfactant) and Labrafil M2125CS (co-surfactant) at a weight ratioof 20:70:10. The SNEDDS produced the emulsion droplet size 18.66±0.88 nm. Spray drying technique was used toconvert the selected enzalutamide-loaded SNEDDS into solid SNEDDS with inert carrier such as silicon dioxide. Enzlautamide-loaded solid SNEDDS was characterized by scanning electron microscopy, transmission electron microscopy,powder X-ray diffractometry, dynamic light scattering, saturation solubility and in vitro dissolution study. The S-SNEDDSproduced an emulsion droplet size of 15.37±0.49 nm and there was no change in particle size between with or withoutdrug. SEM and PXRD results suggested that enzalutamide existed in amorphous form in enzalutamide-loaded solidSNEDDS. In addition, enzalutamide-loaded solid SNEDDS increased saturation solubility 42-fold and dissolution rates 23-fold compared to crystalline enzalutamide. Therefore, the solid SNEDDS could be a potential nano-sized drug deliverysystem for poorly water-soluble drug enzalutamide.