Laboratory of Pharmaceutical Technology, Department of Pharmacy, University of Patras, Rio 26510, Greece.
J Biomed Nanotechnol. 2012 Aug;8(4):613-23. doi: 10.1166/jbn.2012.1426.
The aim of this study is to evaluate the influence of different lipid vesicular systems on the skin permeation ability of hydrophilic molecules, and understand if and which vesicle physicochemical properties may be used as predictive tools. Calcein and carboxyfluorescein were used as hydrophilic drug models. All vesicles (conventional liposomes [CLs], transfersomes [TRs] and invasomes [INVs]), were characterized for particle size distribution, zeta-potential, vesicular shape and morphology, encapsulation efficiency, integrity, colloidal stability, elasticity and finally in vitro human skin permeation. Dynamic light scattering (DLS) and cryo-transmission electron microscopy (cryo-TEM) defined that almost all vesicles had spherical structure, low polydispersity (PI < 0.2) and nanosize. Elasticity values (measured by extrusion through membranes) were in the order INVs > TRs > CLs. Three vesicle types were selected (having different elasticity) and in vitro skin permeation experiments demonstrated that calcein permeation was minimal from an aqueous solution, slightly enhanced from CLs, and enhanced by 1.8 and 7.2 times from TRs and INVs, respectively. Permeation and elasticity values were correlated by rank order but not linearly, indicating that elasticity can be used as a crude predictive tool for enhancement of skin transport. Drug encapsulation efficiency was not found to be an important factor in the current study.
本研究旨在评估不同脂质囊泡系统对亲水分子经皮渗透能力的影响，并探讨囊泡的物理化学性质是否可以作为预测工具。 钙黄绿素和羧基荧光素被用作亲水性药物模型。 所有囊泡（普通脂质体[CL]、传递体[TR]和侵入体[INV]）均进行了粒径分布、Zeta 电位、囊泡形状和形态、包封效率、完整性、胶体稳定性、弹性以及体外人皮渗透的表征。动态光散射（DLS）和冷冻透射电子显微镜（cryo-TEM）定义了几乎所有的囊泡都具有球形结构、低多分散性（PI < 0.2）和纳米尺寸。通过膜挤压测量的弹性值（elasticity values）的顺序为 INV > TR > CL。选择了三种囊泡类型（具有不同的弹性），体外皮肤渗透实验表明，从水溶液中钙黄绿素的渗透最小，从 CL 略有增加，从 TR 和 INV 分别增加了 1.8 和 7.2 倍。渗透和弹性值通过等级顺序相关，但不是线性相关，表明弹性可以作为增强皮肤传输的一种粗糙的预测工具。在本研究中，药物包封效率不是一个重要因素。
