首页|冰片修饰的胡椒碱醇质体的制备、表征及透皮吸收研究

冰片修饰的胡椒碱醇质体的制备、表征及透皮吸收研究

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

piperineethosomestransdermal permeation

霍雨佳、谷娟、呼胜楠、陈栋

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黄河科技学院医学院,河南郑州 450005

河南大学药学院,河南开封 475001

胡椒碱 醇质体 经皮渗透

2024

中国医院药学杂志
中国药学会

中国医院药学杂志

CSTPCD北大核心
影响因子:1.198
ISSN:1001-5213
年,卷(期):2024.44(6)
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