Schmidberger Markus, Nikolic Ines, Pantelic Ivana, Lunter Dominique
Department of Pharmaceutical Technology, Eberhard Karls University, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, 450 Vojvode Stepe Street, 11221 Belgrade, Serbia.
Pharmaceutics. 2019 Jul 24;11(8):361. doi: 10.3390/pharmaceutics11080361.
Topical formulations are an important pillar in the therapy of skin diseases. Nevertheless, after application the formulation will be exposed to environmental effects. Contact with other surfaces will reduce the available amount of formulation and drug substance. The resulting consequences for therapy range from reduced effects to therapeutic failure. The removed active ingredient also contaminates patients' environment. The aim of this work was to develop preparations that remain at the application site. These will enhance safety and efficiency and thus improve of skin disease therapies. Therefore, we developed polymer-stabilised emulsions that show thermogelling properties. Emulsions with different methyl cellulose concentrations and macrogols of different molecular weights were investigated. The dispersed phase consisted of nonivamide as the active pharmaceutical ingredient, dissolved in medium-chain triglycerides. Rheological properties, droplet size, substantivity and ex vivo penetration experiments were performed to characterise the developed formulations. Droplet size and rheological parameters were affected by the composition of the preparations. The tested formulations showed benefits in their substantivity compared to a conventional semi-solid cream. We found a residual amount of up to 100% at the application site. The drug levels in viable epidermis were in a therapeutic range. The developed emulsions are a promising vehicle to improve therapy for chronic skin diseases.
局部用制剂是皮肤病治疗的重要支柱。然而，制剂应用后会受到环境影响。与其他表面接触会减少制剂和药物的可用量。由此产生的治疗后果从疗效降低到治疗失败不等。被去除的活性成分还会污染患者的环境。这项工作的目的是开发能留在应用部位的制剂。这些制剂将提高安全性和有效性，从而改善皮肤病治疗。因此，我们开发了具有热凝胶特性的聚合物稳定乳液。研究了不同甲基纤维素浓度和不同分子量聚乙二醇的乳液。分散相由作为活性药物成分的辣椒素，溶解在中链甘油三酯中组成。进行了流变学性质、液滴大小、粘着性和离体渗透实验以表征所开发的制剂。液滴大小和流变学参数受制剂组成的影响。与传统半固体乳膏相比，测试的制剂在粘着性方面表现出优势。我们发现在应用部位残留量高达100%。活表皮中的药物水平在治疗范围内。所开发的乳液是改善慢性皮肤病治疗的有前景的载体。
