伊立替康微乳的制备及体外释药评价OA

The formulation components of irinotecan blank microemulsion were screened using the pseudo-ternary phase diagram method.The optimal formulation was determined based on evaluation indices including mean particle size,polydispersity index(PDI),and drug loading capacity,and the irinotecan-loaded microemulsion was successfully prepared.The pharmaceutical characteristics and in vitro drug release behavior of the microemulsion were investigated.The results showed that when 1944-CS was used as the oil phase,RH60 as the emulsifier,PEG300 as the co-emulsifier,and the mass ratio(Km)of the emulsifier to the co-emulsifier was 3∶1,the obtained microemulsion exhibited the largest area and the most stable properties.When the drug loading of irinotecan was 0.5％of the total system mass,the prepared microemulsion appeared spherical with uniform dispersion,a mean particle size of(78.12±2.42)nm,a PDI of 0.342±0.031,a Zeta potential of(-1.93±0.51)mV,and demonstrated good centrifugal stability and temporal stability.The 24-hour cumulative drug release rate was significantly lower than that of the free drug.Thus,the prepared irinotecan microemulsion possesses good stability and sustained-release properties,suggesting its potential as a feasible pharmaceutical formulation for the clinical anti-tumor therapy of irinotecan.