Food and Drug Department, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Biomed Res Int. 2018 Aug 2;2018:1281673. doi: 10.1155/2018/1281673. eCollection 2018.
The objective of this work was to study propranolol permeation and skin retention after topical application of different semisolid vehicles, with the final aim of developing new topical formulations intended for the treatment of infantile hemangioma, able to produce therapeutic drug levels in the skin, avoiding systemic absorption. Propranolol ointments, creams, and gels were prepared and tested on pig skin, an accepted model of human skin. From the results obtained in the present work it is clear that the permeation of propranolol across the skin is a poor predictor of its skin retention, at least in the time-frame considered. With an application time of 4 h, reasonably close to the permanence time of a semisolid formulation on the skin surface, the best performance (high retention and low skin penetration) was obtained with lipophilic formulations, in particular with a lipophilic cream containing olive oil. Hydrophilic formulations, such as gels, are characterized by a significant permeation across the skin, probably leading to systemic side effects, accompanied by a limited skin retention. Overall, the results obtained in the present work pose the basis for the development of new topical formulations, containing propranolol, with better performance and reduced systemic absorption.
本工作的目的是研究不同半固体制剂经皮应用后普萘洛尔的渗透和皮肤滞留情况，最终开发出用于治疗婴幼儿血管瘤的新型局部制剂，使药物在皮肤中达到治疗水平，避免全身吸收。制备了普萘洛尔软膏、乳膏和凝胶，并在猪皮上进行了测试，猪皮是人体皮肤的一种公认模型。从本工作获得的结果清楚地表明，普萘洛尔在皮肤中的渗透是其皮肤滞留的不良预测指标，至少在考虑的时间范围内是这样。在 4 小时的应用时间内，与半固体制剂在皮肤表面的停留时间相当接近，最具性能（高保留和低皮肤穿透性）的是脂溶性制剂，特别是含有橄榄油的脂溶性乳膏。亲水制剂，如凝胶，其特点是皮肤穿透性明显，可能导致全身副作用，并伴有有限的皮肤滞留。总的来说，本工作获得的结果为开发具有更好性能和减少全身吸收的新型局部制剂奠定了基础，这些制剂含有普萘洛尔。
