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油质体的纳米设计用于局部递送抗氧化剂白藜芦醇。

Nanodesign of olein vesicles for the topical delivery of the antioxidant resveratrol.

机构信息

Department Ingeniería Química y Tecnología del Medio Ambiente, University of Oviedo, Oviedo, Spain.

出版信息

J Pharm Pharmacol. 2013 Aug;65(8):1158-67. doi: 10.1111/jphp.12093. Epub 2013 Jun 20.

Abstract

OBJECTIVES

The ex-vivo percutaneous absorption of the natural antioxidant resveratrol in liposomes and niosomes was investigated. The influence of vesicle composition on their physicochemical properties and stability was evaluated. Liposomes containing resveratrol were formulated using soy phosphatidylcholine (Phospholipon90G). Innovative niosomes were formulated using mono- or diglycerides: glycerol monooleate (Peceol) and polyglyceryl-3 dioleate (Plurol OleiqueCC), respectively, two suitable skin-compatible oleins used in pharmaceutical formulations as penetration enhancers.

METHODS

Small, negatively charged vesicles with a mean size of approximately 200 nm were prepared. The accelerated stability of vesicles was evaluated using Turbiscan Lab Expert, and the bilayer deformability was also assessed. Ex-vivo transdermal experiments were carried out in Franz diffusion cells, on newborn pig skin, to study the influence of the different vesicle formulations on resveratrol skin delivery.

KEY FINDINGS

Results indicated a high cutaneous accumulation and a low transdermal delivery of resveratrol, especially when Peceol niosomes were used.

CONCLUSIONS

Overall, niosomes formulated with Plurol oleique or Peceol showed a better behaviour than liposomes in the cutaneous delivery of resveratrol.

摘要

目的

研究了天然抗氧化剂白藜芦醇在脂质体和非离子型囊泡中的经皮吸收。评估了囊泡组成对其理化性质和稳定性的影响。含有白藜芦醇的脂质体采用大豆卵磷脂(Phospholipon90G)进行配方设计。创新的非离子型囊泡采用单或双甘油酯:甘油单油酸酯(Peceol)和聚甘油-3 二油酸酯(Plurol OleiqueCC)分别进行配方设计,这两种适用于药物制剂的皮肤相容性油,作为渗透增强剂使用。

方法

制备了平均粒径约为 200nm 的小而带负电荷的囊泡。使用 Turbiscan Lab Expert 评估了囊泡的加速稳定性,并评估了双层变形性。在 Franz 扩散池中进行离体透皮实验,在新生猪皮上进行,以研究不同囊泡配方对白藜芦醇皮肤传递的影响。

主要发现

结果表明,白藜芦醇的皮肤蓄积量高,经皮传递量低,尤其是使用 Peceol 非离子型囊泡时。

结论

总体而言,与脂质体相比,用 Plurol oleique 或 Peceol 制成的非离子型囊泡在白藜芦醇的皮肤传递方面表现出更好的性能。

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