Flux of ionic dyes across microneedle-treated skin: effect of molecular characteristics.
Flux of ionic dyes across microneedle-treated skin: effect of molecular characteristics.
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DOI：
10.1016/j.ijpharm.2012.08.026
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发表时间：
2012-11-15
影响因子：
5.8
通讯作者：
Wilson CG
中科院分区：
文献类型：
--
作者：
Gomaa YA;Garland MJ;McInnes FJ;Donnelly RF;El-Khordagui LK;Wilson CG
通过微针（MN）处理皮肤的药物通量受MN阵列、微导管和药物分子的特性以及微导管和活组织的总体扩散阻力的影响。这些因素的相对含义尚未得到充分探讨。本文研究了6种不同分子量和化学取代基结构相关的离子杂蒽染料在mn预处理的全层猪皮上的体外渗透特性。采用pH 7.4的磷酸盐缓冲盐水作为皮肤渗透实验的介质，测定染料在各向同性正辛醇/水体系和猪皮/水体系中的平衡溶解度及其分配系数。此外，解离常数用电位法测定。结果表明，对于罗丹明染料，在生理pH下占主导地位的两性离子形式的皮肤渗透，由于MW的增加，化学反应性异硫氰酸酯取代基的存在与角质层蛋白质和皮肤厚度相互作用而显着降低。这些因素通常被证明优于水溶解度，水溶解度是药物在水环境中扩散的重要决定因素。研究结果进一步揭示了药物在mn处理皮肤中的渗透机制，对mn基透皮给药系统的设计和体外皮肤渗透研究具有重要意义。
Drug flux across microneedle (MN)-treated skin is influenced by the characteristics of the MN array, microconduits and drug molecules in addition to the overall diffusional resistance of microconduits and viable tissue. Relative implication of these factors has not been fully explored. In the present study, the in vitro permeation of a series of six structurally related ionic xanthene dyes with different molecular weights (MW) and chemical substituents, across polymer MN-pretreated full thickness porcine skin was investigated in relation of their molecular characteristics. Phosphate buffer saline pH 7.4, the medium used in skin permeation experiments, was used to determine the equilibrium solubility of the dyes and their partition coefficient both in the isotropic n-octanol/ aqueous system and porcine skin/ aqueous system. Additionally, dissociation constants were determined potentiometrically. Results indicated that for rhodamine dyes, skin permeation of the zwitterionic form which predominates at physiological pH, was significantly reduced by an increase in MW, the presence of the chemically reactive isothiocyanate substituent reported to interact with stratum corneum proteins and the skin thickness. These factors were generally shown to override aqueous solubility, an important determinant of drug diffusion in an aqueous milieu. Findings provided more insight into the mechanism of drug permeation across MN-treated skin, of importance to both the design of MN-based transdermal drug delivery systems and in vitro skin permeation research.
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影响因子：
3.7
作者：
Kalluri, Haripriya;Banga, Ajay K.
通讯作者：
Banga, Ajay K.
影响因子：
5.8
作者：
Caon, Thiago;Oliveira Costa, Ana Carolina;Oliveira Simoes, Claudia Maria
通讯作者：
Oliveira Simoes, Claudia Maria
DOI：
10.1016/j.saa.2005.02.012
发表时间：
2005-11-01
影响因子：
4.4
作者：
Ghasemi, J;Niazi, A;Kubista, M
通讯作者：
Kubista, M
DOI：
10.1007/s00128-008-9401-1
发表时间：
2008-08-01
影响因子：
2.7
作者：
Kwon, Jeong-Wook;Armbrust, Kevin L.
通讯作者：
Armbrust, Kevin L.
DOI：
10.1016/j.jconrel.2010.10.033
发表时间：
2011-02-10
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Chu LY;Prausnitz MR
通讯作者：
Prausnitz MR