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脂质体钴胺素水凝胶局部应用于特应性皮炎治疗。

Topical application of liposomal cobalamin hydrogel for atopic dermatitis therapy.

作者信息

Jung Suk Hyun, Cho Young Sik, Jun Sung Soo, Koo Ja Seong, Cheon Hyae Gyeong, Shin Byung Cheol

机构信息

Korea Research Institute of Chemical Technology, Daejeon, Korea.

出版信息

Pharmazie. 2011 Jun;66(6):430-5.

Abstract

Topical vitamin B12 was shown to be effective for atopic dermatitis. However, vitamin B12 itself is light sensitive and has low skin permeability, thus reducing its therapeutic effectiveness. In the present study, we prepared a liposomal hydrogel of adenosylcobalamin (AdCbl), a vitamin B12 derivative, and investigated possible beneficial effects of AdCbl on atopic dermatitis using an NC/Nga murine atopic dermatitis model. AdCbl was loaded into liposomes prepared by a thin film hydration method using a pH gradient method that employed citric acid buffer solution. This resulted in AdCbl-loaded liposomes that were 106.4 +/- 2.2 nm in size. The loading efficiency was 40% (of the initial AdCbl amount). Lipo-AdCbl had enhanced skin permeability, being about 17-fold compared with AdCbl-gel. Topical administration of Lipo-AdCbl-gel to 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis-like skin lesions in NC/Nga mice ameliorated lesion intensity scores, dorsal skin thickness, and total serum IgE in a concentration-dependent manner. Other preparations, including AdCbl solution, AdCbl cream, liposomes alone, and a mixture of AdCbl solution and liposomes had little effect. Taken together, our findings indicate that Lipo-AdCbl-gel has protective effects against atopic dermatitis symptoms, and suggest that it may be of benefit in the treatment of human inflammatory skin diseases.

摘要

局部应用维生素B12已被证明对特应性皮炎有效。然而,维生素B12本身对光敏感且皮肤渗透性低,从而降低了其治疗效果。在本研究中,我们制备了维生素B12衍生物腺苷钴胺素(AdCbl)的脂质体水凝胶,并使用NC/Nga小鼠特应性皮炎模型研究了AdCbl对特应性皮炎可能的有益作用。通过使用柠檬酸缓冲溶液的pH梯度法,采用薄膜水化法将AdCbl载入脂质体。这产生了尺寸为106.4±2.2nm的载AdCbl脂质体。载入效率为40%(相对于初始AdCbl量)。脂质体-腺苷钴胺素(Lipo-AdCbl)的皮肤渗透性增强,与AdCbl凝胶相比约为17倍。将Lipo-AdCbl凝胶局部应用于2,4-二硝基氯苯(DNCB)诱导的NC/Nga小鼠特应性皮炎样皮肤病变,可使病变强度评分、背部皮肤厚度和血清总IgE以浓度依赖的方式改善。其他制剂,包括AdCbl溶液、AdCbl乳膏、单独的脂质体以及AdCbl溶液与脂质体的混合物几乎没有效果。综上所述,我们的研究结果表明Lipo-AdCbl凝胶对特应性皮炎症状具有保护作用,并表明它可能对治疗人类炎症性皮肤病有益。

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