Preparation and pharmacokinetic evaluation of cinnamaldehyde nanoemulsion
Objective To prepare cinnamaldehyde nanoemulsion(Cin-NE)for improving the stability,water-solubility and oral bioavailability of cinnamaldehyde.Methods Cinnamaldehyde was used as both drug and oil phases,and cremophor EL-35 was used as emulsifier to construct cinnamaldehyde emulsion(Cin-E),which was diluted to obtain the nano delivery system with anti dilution property,Cin-NE.The particle size and PDI of Cin-NE was measured by laser particle sizer,and the cinnamaldehyde content of Cin-NE was examined using UPLC to investigate the stability of Cin-NE obtained from Cin-E stored for a long period of time,using appearance properties,particle size and content as indicators.In addition,the oral absorption and in vivo pharmacokinetic characteristics of Cin-NE were explored by intragastric administration in SD rats.Results The loading of cinnamaldehyde into the nanoemulsion significantly improved the solubility of the drug in water.The content of Cin in Cin-E was 90.9 mg/ml,and the particle size of its prepared Cin-NE was small and uniformly distributed,which also exhibits anti-dilution property in water,SGF and SIF.The stability of Cin-NE obtained from Cin-E stored at 4℃was good.In vivo pharmacokinetic results of SD rats administered by oral gavage showed that the bioavailability of Cin-NE was 3 times that of the raw drug,which shows that the nanoemulsion significantly improved the oral absorption of cinnamaldehyde.Conclusion By using cinnamaldehyde itself as both drug and oil phases,without additional oil phases or co-emulsifiers,Cin-NE,a cinnamaldehyde nano drug delivery system with streamlined prescription and simple process,was successfully constructed.Cin-NE significantly improved the stability,solubility,and oral bioavailability of cinnamaldehyde compared with the raw drug,providing useful exploration and insights for the clinical application of cinnamaldehyde.
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维普
