Preparation and Quality Control of Quetiapine Fumarate Solid Lipid Nanoparticles in situ Nasal Gel / 中国药房

ABSTRACT

OBJECTIVE:To prepare and evaluate the quality of Quetiapine fumarate solid lipid nanoparticles(QF-SLN)in situ nasal gel. METHODS:With the oil phase of dissoned glycerin monostearate,emulsifier of sorbitan oleate,and co-emulsifier of n-butyl alcohol,the proportion of emulsifier and co-emulsifier (Km) was screened by ternary phase diagrams. QF-SLN was pre-pared through the micro-emulsion technology,the gelling temperature was set as index,the mass fraction of poloxamerln 407 (P407)and P188 of in situ gel formulation was optimized by the central composite design-response surface methodology. in situ for-mation of QF-SLN was examined by transmission electron microscope,the particle size and potential distribution were determined by Malvern laser granularity equipment,and the encapsulation efficiency and stability were determined by the ultrafiltration centri-fuge tube and HPLC. RESULTS:The formulation of solid lipid nanoparticlesl was biggest at Km=1∶9. The optimized formulation was with 21% P407,5.6% P188 and 73.4% water. The prepared QF-SLN in situ nasal gel was uniform sphere,with an average particle size of (136.3 ± 6.4) nm and encapsulation efficiency of (97.60 ± 0.48)%. There were no obvious changes in the particle size and entrapment efficiency at 4℃within one month. CONCLUSIONS:The QF-SLN in situ nasal gel is successfully prepared.