다공성의 콜로이드성 이산화규소를 이용한 닐로티닙 함유 고형의 자가미세유화 약물전달시스템의 개발

Development of Nilotinib HCl-loaded solid SNEDDS (Self-Nanoemulsifying Drug Delivery System) using Mesoporous Colloidal Silica

The objective of this study was to develop a novel nilotinib HCl-loaded solidified self-nanoemulsifying drug delivery system (SNEDDS) formulation with enhanced solubility and dissolution rate. Various oils and surfactants were screened, resulting in the selection of Peceol (oil) and Tween 80 (surfactant) and Transcutol P (co-surfactant). Pseudoternary phase diagram was constructed to detect the nanoemulsion zone. Among the SNEDDS formulations tested, the SNEDDS consisting of Peceol (oil), Tween 80 (surfactant), and Transcutol P (co-surfactant) at a weight ratio of 30/50/20 produced an emulsion droplet size of 182.1±1.0 nm. The spray drying technique, using mesoporous silicon dioxide as an inert carrier, was employed to solidify the selected nilotinib HCl-loaded SNEDDS. The resulting nilotinib HCl-loaded solid SNEDDS (S-SNEDDS) was characterized by scanning electron microscopy (SEM), powder X-ray diffractometry (PXRD), dynamic light scattering, saturation solubility and in vitro dissolution study. The S-SNEDDS produced an emulsion droplet size of 185.2±0.9 nm and there was no change in emulsion particle size upon the addition of drug. SEM and PXRD results suggested that nilotinib HCl existed in an amorphous form in nilotinib HCl-loaded S-SNEDDS. Solubility tests across various pH levels showed a significant improvement in nilotinib HCl solubility. Similarly, dissolution tests demonstrated enhanced dissolution rates in all tested solutions, consistent with the solubility results. These results indicate that the employed methodologies were effective in increasing both the solubility and dissolution rates of nilotinib HCl across different pH environments, suggesting a successful enhancement of its bioavailability.