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
霍雨佳 1谷娟 1呼胜楠 1陈栋2
作者信息
- 1. 黄河科技学院医学院,河南郑州 450005
- 2. 河南大学药学院,河南开封 475001
- 折叠
摘要
目的:制备冰片修饰胡椒碱醇质体(bomeol-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Bor-Pip-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.
Abstract
OBJECTIVE To prepare bomeol-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 bomeol 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 bomeol 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.
关键词
胡椒碱/醇质体/经皮渗透Key words
piperine/ethosomes/transdermal permeation引用本文复制引用
出版年
2024
NETL
NSTL
万方数据