PROTOCOL OPTIMIZATION FOR THE FORMULATION OF LINEZOLID-LOADED LIPOSOMES BY RESPONSE SURFACE METHODOLOGY AND IN VITRO DRUG RELEASE FOR ANTI-TUBERCULOSIS

Objective: To prepare linezolid liposomes through membrane dispersion method, and optimize the formulation and preparation process by response surface methodology Methods: drug-loaded liposomes and free drug were separated by centrifugation. Linezolid liposomes were prepared by membrane dispersion method with encapsulation rate as the main index, which was determined by ultraviolet spectrophotometry. The formulation and preparation process were optimized by single factor test and response surface method. The morphology of linezolid liposomes was observed by optical and fluorescence microscopy. The total release of linezolid liposomes at different rime points was measured by dialysis. Results: linezolid-liposome preparation was optimal for cholesterol:lectihin and linezolid:lecithin mass ratios of 1:2 and 1:20, respectively, and incubation at 50 degrees C. The encapsulation rate and relative standard deviation (RSD) were 75.53% and 0.34%, respectively. In vitro release experiments showed that linezolid encapsulation in liposomes delays drug release compared to linezolid solution. Conclusion: response surface analysis method is reliable to optimize the preparation and formulation of linezolid liposomes.