다공성의 콜로이드성 이산화규소를 이용한 닐로티닙 함유 고형의 자가미세유화 약물전달시스템의 개발

Abstract

The objective of this study was to develop a novel nilotinib HCl-loaded solidified self-nanoemulsifying drugdelivery system (SNEDDS) formulation with enhanced solubility and dissolution rate. Various oils and surfactants werescreened, resulting in the selection of Peceol (oil) and Tween 80 (surfactant) and Transcutol P (co-surfactant). Pseudoternaryphase diagram was constructed to detect the nanoemulsion zone. Among the SNEDDS formulations tested, theSNEDDS consisting of Peceol (oil), Tween 80 (surfactant), and Transcutol P (co-surfactant) at a weight ratio of 30/50/20produced an emulsion droplet size of 182.1±1.0 nm. The spray drying technique, using mesoporous silicon dioxide as aninert carrier, was employed to solidify the selected nilotinib HCl-loaded SNEDDS. The resulting nilotinib HCl-loaded solidSNEDDS (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 dropletsize of 185.2±0.9 nm and there was no change in emulsion particle size upon the addition of drug. SEM and PXRDresults suggested that nilotinib HCl existed in an amorphous form in nilotinib HCl-loaded S-SNEDDS. Solubility testsacross various pH levels showed a significant improvement in nilotinib HCl solubility. Similarly, dissolution testsdemonstrated enhanced dissolution rates in all tested solutions, consistent with the solubility results. These results indicatethat the employed methodologies were effective in increasing both the solubility and dissolution rates of nilotinib HClacross different pH environments, suggesting a successful enhancement of its bioavailability.