Preparation, Evaluation Of Amorolfine Hydrochloride Ethosomes And A Novel Binary Ethosomes

OBJECTIVE:(1) To prepare and evaluate amorolfine hydrochloride ethosomes and Nit ethosomes.(2) To prepare and evaluate Nit binary ethosomes.METHODS:(1) Infusing method was used to prepare amorolfine hydrochloride ethosomes and Nit binary ethosomes, the release rate was determined by Franz diffusion cells.(2) The accumulated percutaneous permeability in vitro of amorolfine hydrochloride ethosomes and Nit binary ethosomes were determined by a setting of Franz diffusion cells.(3) The distribution of Rhodamine B (probe drug) in the rat skin was observed under confocal laser scanning microscope.RESULTS:(1) Amorolfine hydrochloride ethosomes were prepared (particle size: 105±4.3 nm; Encapsulation efficiency:86.23±3.2%). The ethosomes were stable in 3 months at room temperature. In vitro cumulative released quantity in 4 h was 40%, which was lower than the liposomes (60%) and ethanol (90%). Amorolfine hydrochloride was totally released in 24 h. In vitro percutaneous permeation experiments showed that:the amount of ethosomes through the skin into the acceptance solution was 1.7 times (ethanol solution) and 3 times (liposomes). The fluorescence intensity (Max FI= 161AU) of ethosomes in mouse skin was much higher than ethanol (Max FI= 82AU) and liposomes (Max FI=38AU). Its penetration depth of ethosomes to mice skin was the deepest, wchich was up to 170μm.(2) The diameter of Nicotine ethosomes was 108±2.15nm and the encapsulation efficiency was 86.23±3.2%. In vitro cumulative released quantity in 4 h was 50%, which was lower than the liposomes (62%). The cumulative penetration of nicotine ethosomes in 24 h was nearly five times than liposome.(3) The prescription of Nit binary ethosomes was optimized. The ratio of ethanol to propylene glycol was 5:5 for the best. The obtained diameter of nicotine ethosomes was 100±13.0nm and the entrapment efficiency was 95.3±13.87%. Nit binary ethosomes showed good stability at room temperature for 6 months.4 h before its release in vitro cumulative release was 37%and 24 h cumulative release was 68%. In vitro percutaneous penetration showed that the amount of Nit binary ethosomes through the skin into the acceptance solution was 1.3 times (ethosomes) and 4 times (liposomes). The fluorescence intensity (Max FI= 170AU) of Nit binary ethosomes. Its penetration depth of ethosomes to mice skin was the deepest, which was up to 170μm.CONCLUSION:(1) Ethosomes could increase the permeation of amorolfine hydrochloride and Nit through rat skin, and improve the retention of drug in rat skin. However, the stability of ethosomes was poor.(2) In our case, Nit binary ethosomes stability, encapsulation efficiency and skin permeability than ethosomes had increased (P<0.01). NEW IDEAS:(1) The preparation and evaluation of binary ethosomes were introduced for the first time. (2) The preparation, characterization and evaluation of Amorolfine hydrochloride ethosomes, Nit ethosomes and Nit binary ethosomes were introduced for the first time.