Skin penetration and deposition of carboxyfluorescein and temoporfin from different lipid vesicular systems: In vitro study with finite and infinite dosage application
Skin penetration and deposition of carboxyfluorescein and temoporfin from different lipid vesicular systems: In vitro study with finite and infinite dosage application
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DOI：
10.1016/j.ijpharm.2011.02.006
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发表时间：
2011-04-15
影响因子：
5.8
通讯作者：
Fahr, Alfred
中科院分区：
文献类型：
--
作者：
Chen, Ming;Liu, Xiangli;Fahr, Alfred
本研究的目的是评估不同的脂质囊泡系统的影响，以及应用模式对羧基荧光素（亲水性模型药物）和替莫泊芬（亲脂性模型药物）的皮肤渗透和沉积行为的影响。所有的脂质囊泡系统，包括传统的脂质体，invasomes和醇质体，通过薄膜水合法制备和表征的粒径分布，zeta电位，囊泡形状和表面形态，在体外人体皮肤渗透和皮肤沉积。动态光散射（DLS）和透射电子显微镜（TEM）确定所有脂质囊泡具有几乎球形的结构，具有低多分散性（PDI < 0.2）和纳米尺寸范围（z-平均不超过150 nm）。此外，所有脂质囊泡系统表现出负zeta电位。体外皮肤渗透和沉积实验表明，在有限剂量应用（10 μ l/cm（2））和无限剂量应用（160 μ l/cm（2））的CF的情况下，与非囊泡系统相比，脂质囊泡系统，特别是醇质体和侵袭体，可以显著改善亲水性药物如羧基荧光素进入皮肤深层或穿过皮肤的递送。而在有限和无限剂量应用的mTHPC的情况下，对于脂质囊泡系统和非囊泡系统，大多数药物蓄积都在皮肤表层中观察到。结果还表明，影响药物皮肤分布的因素与药物的理化性质、赋形剂的选择和给药方式有关。(C)2011 Elsevier B. V.保留所有权利。
The aim of the present research is to evaluate the influence of different lipid vesicular systems as well as the effect of application mode on skin penetration and deposition behaviors of carboxyfluorescein (hydrophilic model drug) and temoporfin (lipophilic model drug). All of the lipid vesicular systems, including conventional liposomes, invasomes and ethosomes, were prepared by film hydration method and characterized for particle size distribution, zeta-potential, vesicular shape and surface morphology, in vitro human skin penetration and skin deposition. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) defined that all of lipid vesicles had almost spherical structures with low poly-dispersity (PDI < 0.2) and nanometric size range (z-average no more than 150 nm). In addition, all lipid vesicular systems exhibited a negative zeta potential. In vitro skin penetration and deposition experiments demonstrated that, in the case of CF with finite dose application (10 mu l/cm(2)) and infinite dose application (160 mu l/cm(2)), lipid vesicular systems, especially ethosomes and invasomes, compared with non-vesicular systems, can significantly improve the delivery of hydrophilic drug such as carboxyfluorescein into skin deep layers or across the skin. While in the case of mTHPC with finite and infinite dose application, most of drug accumulation was observed in the skin superficial layer for both lipid vesicular systems and non-vesicular systems. The results also revealed that the factors influencing the drug skin distribution concern the physicochemical characteristics of the drug, the choice of the vehicle formulation and the application mode applied. (C) 2011 Elsevier B.V. All rights reserved.