冰片修饰的胡椒碱醇质体的制备、表征及透皮吸收研究

Preparation, characterization and transdermal absorption of borneol-modified piperine ethosomes

目的:制备冰片修饰胡椒碱醇质体(borneol-modified piperine ethosomes,Bor-Pip-ES),并对其经皮渗透性能进行比较。方法:选择脂药比、磷脂与胆固醇用量比、乙醇体积分数和冰片占载体百分比为主要影响因素,Box-Behnken设计-效应面法优化Bor-Pip-ES处方工艺。制备成Bor-Pip-ES凝胶,并进行理化性质、流变学特性等研究。采用Franz扩散池法考察BorPip-ES凝胶体外透皮性能。结果:Bor-Pip-ES最佳处方为脂药比13.5:1,磷脂与胆固醇用量比14.4:1,乙醇体积分数12.7%,冰片占载体百分比1.9%。Bor-Pip-ES平均包封率为(81.52±1.36)%,载药量为(5.24±0.15)%,粒径为(170.98±9.18)nm,Zeta电位为–(8.16±0.73)mV。Bor-Pip-ES形态为球形或椭圆形。流变学显示Bor-Pip-ES凝胶具有固体弹性性质。透皮试验结果表明,Bor-Pip-ES凝胶显著提高了胡椒碱的透皮速率、累积渗透量和皮肤滞留量。结论:Bor-Pip-ES凝胶黏度适宜,易于涂展,为后续研究奠定实验基础。

OBJECTIVE To prepare borneol-modified piperine ethosomes(Bor-Pip-ES)and elucidate its transdermal per⁃meation properties.METHODS Lipids-to-drug ratio,phospholipids-to-cholesterol ratio,percentage concentration of ethanol and percentage of borneol in carrier were selected as major influencing factors.Box-Behnken design-response surface method was optimized for preparing Bor-Pip-ES.Also Bor-Pip-ES gels were also prepared and their physicochemical and rheological proper⁃ties evaluated.Franz diffusion cell method was employed for examining the transdermal properties of Bor-Pip-ES gels.RESULTS Optimal formulation of Bor-Pip-ES:lipids-to-drug ratio 13.5∶1,phospholipids-to-cholesterol ratio 14.4∶1,per⁃centage concentration of ethanol 12.7%and percentage of borneol in carrier 1.9%.Encapsulation efficiency,drug loading,par⁃ticle size and Zeta potential of Bor-Pip-ES were(81.52±1.36)%,(5.24±0.15)%,(170.98±9.18)nm and-(8.16±0.73)mV respectively.The shape of Bor-Pip-ES was spherical or elliptical.Rheological properties of bor-Pip-ES gels indicated solid elas⁃tic properties.Results of transdermal test showed that permeation rate,cumulative penetration and skin retention of Bor-Pip-ES gels spiked markedly.CONCLUSION Viscosity of Bor-Pip-ES gels is suitable and it spreads easily.Thus it offers experimental rationales for further researches.