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单独添加超氧化物歧化酶或与α-生育酚联合添加的制剂的物理和抗氧化活性稳定性、体外释放及体内疗效评估。

Assessment of physical and antioxidant activity stability, in vitro release and in vivo efficacy of formulations added with superoxide dismutase alone or in association with alpha-tocopherol.

作者信息

Di Mambro Valéria Maria, Fonseca Maria José Vieira

机构信息

Department of Pharmaceutical Science, University of São Paolo, Ribeirão Preto, Brazil.

出版信息

Eur J Pharm Biopharm. 2007 Jun;66(3):451-9. doi: 10.1016/j.ejpb.2006.11.012. Epub 2006 Nov 26.

Abstract

A topical formulation was added with different concentrations of superoxide dismutase (SOD) alone or in association with alpha-tocopherol (alpha-TOC). The physical stability was evaluated by rheological behavior of formulations stored at 4 degrees C, 30 degrees C/60% RH and 40 degrees C/70% RH for 6 months. SOD alone and formulations containing SOD 0.2%, 0.4% or 0.6% or SOD and alpha-TOC were stored in the same conditions and the enzymatic activity was evaluated by the superoxide anion scavenging using chemiluminescence measurement. In vitro release study was carried out using modified Franz diffusion cell and SOD formulations photoprotection against skin erythema was observed for 72 h. SOD and alpha-TOC formulation proved to be instable, since the interaction between the antioxidants led to both physical and enzymatic activity instability. SOD formulations showed to be physically stable and maintained the enzymatic activity for 6 months when stored at 4 and 30 degrees C/60% RH. Despite the fact of low SOD release from the formulation, it was effective in inhibiting the UVB-induced skin erythema for 48 h after a single application. Topical administration of antioxidants provides an efficient way to enrich the endogenous cutaneous protection system, and SOD formulations could be used for improving photoprotection of skin.

摘要

一种局部用制剂单独添加了不同浓度的超氧化物歧化酶(SOD),或与α-生育酚(α-TOC)联合添加。通过在4℃、30℃/60%相对湿度和40℃/70%相对湿度下储存6个月的制剂的流变学行为来评估物理稳定性。单独的SOD以及含有0.2%、0.4%或0.6% SOD或SOD与α-TOC的制剂在相同条件下储存,并通过化学发光测量超氧化物阴离子清除来评估酶活性。使用改良的Franz扩散池进行体外释放研究,并观察SOD制剂对皮肤红斑的光保护作用72小时。SOD与α-TOC制剂被证明是不稳定的,因为抗氧化剂之间的相互作用导致了物理和酶活性的不稳定。SOD制剂在4℃和30℃/60%相对湿度下储存时显示出物理稳定性,并在6个月内保持酶活性。尽管制剂中SOD的释放量较低,但单次应用后它在48小时内有效抑制了紫外线B诱导的皮肤红斑。局部施用抗氧化剂提供了一种丰富内源性皮肤保护系统的有效方法,并且SOD制剂可用于改善皮肤的光保护作用。

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