Transdermal delivery of a melanotropic peptide hormone analogue.
Transdermal delivery of a melanotropic peptide hormone analogue.
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促黑素肽激素类似物的透皮递送。
DOI：
10.1016/0024-3205(88)90469-9
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发表时间：
1988
期刊：
影响因子：
6.1
通讯作者：
Don,S
中科院分区：
文献类型：
--
作者：
Dawson,BV;Hadley,ME;Kreutzfeld,K;Dorr,RT;Hruby,VJ;Al-Obeidi,F;Don,S
我们之前报道过，局部应用[Nle 4， D-Phe 7] α - msh （α -黑素细胞刺激激素的超强类似物）对小鼠诱导整个皮肤的滤泡黑素细胞变暗。我们现在报道，在体外模型系统中，促黑素类似物可以通过小鼠而不是大鼠皮肤传递。通过生物测定和放射免疫测定，证明了类似物从局部应用的载体（聚乙二醇）穿过皮肤进入皮下接收血管。生物测定数据表明，经皮吸收的促黑素不会导致肽的生物活性丧失。肽在啮齿动物皮肤上的不同渗透表明，人们无法从单一物种的研究中预测物质在角质层上的经皮吸收。目前的结果是第一次证明，通过直接定量测量，生物活性肽可以在体外通过脊椎动物被膜传递。这些研究指出了局部应用促黑素治疗皮肤晒黑的潜力，并可能用于治疗某些低色素疾病。
We previously reported that topical application of [Nle 4, D-Phe 7] alpha-MSH, a superpotent analogue of alpha-melanocyte stimulating hormone, to mice induces a darkening of follicular melanocytes throughout the skin. We now report that the melanotropin analogue can be delivered across mouse but not rat skin in an in vitro model system. Passage of the analogue from the topically applied vehicle (polyethylene glycol) across the skin into a subcutaneous receiving vessel was demonstrated by both bioassay as well as by radioimmunoassay. The bioassay data demonstrate that percutaneous absorption of the melanotropin did not result in loss of biological activity of the peptide. The differential penetration of the peptide across rodent skin reveals that one cannot predict percutaneous absorption of a substance across the stratum corneum from studies on a single species. The present results are the first to demonstrate, by direct quantitative measurements, that a bioactive peptide can be delivered across the vertebrate integument in vitro. These studies point out the potential of a topically applied melanotropin for tanning of the skin and possibly for treatment of certain hypopigmentary disorders.