The study aims to investigate the propylene glycol-based liposomes named ‘proposomes’ in enhancing skin permeation of drugs with different physicochemical properties. Ibuprofen, tofacitinib citrate, rhodamine B, and lidocaine were loaded into proposomes. These drug formulations were analyzed for particle size, zeta potential, polydispersity index, entrapment efficiency, and in vitro skin permeation. The confocal laser scanning microscopy was performed on skin treated with calcein and rhodamine B laden proposomes. The transdermal delivery relative to physicochemical properties of drugs such as logP, melting point, molecular weight, solubility, etc., were analyzed. We tested the safety of the proposomes using reconstructed human skin tissue equivalents, which were fabricated in-house. We also used human cadaver skin samples as a control. The proposomes had an average diameter of 128 to 148 nm. The drug’s entrapment efficiencies were in the range of 42.9–52.7%, translating into the significant enhancement of drug permeation through the skin. The enhancement ratio was 1.4 to 4.0, and linearly correlated to logP, molecular weight, and melting point. Confocal imaging also showed higher skin permeation of calcein and rhodamine B in proposome than in solution. The proposome was found safe for skin application. The enhancement of skin delivery of drugs through proposomes was dependent on the lipophilicity of the drug. The entrapment efficiency was positively correlated with logP of the drug, which led to high drug absorption.

中文翻译：

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使用提案体增强药物的皮肤递送取决于药物的亲脂性


该研究旨在研究名为“Proposomes”的基于丙二醇的脂质体在增强不同理化性质的药物的皮肤渗透方面的作用。将布洛芬、柠檬酸托法替尼、罗丹明 B 和利多卡因装入提案体中。对这些药物制剂的粒径、zeta 电位、多分散指数、包封效率和体外皮肤渗透性进行了分析。对用钙黄绿素和罗丹明 B 负载的提案体处理的皮肤进行共聚焦激光扫描显微镜检查。分析了透皮给药与药物理化性质的关系，如logP、熔点、分子量、溶解度等。我们使用内部制造的重建人体皮肤组织等效物测试了提案体的安全性。我们还使用人类尸体皮肤样本作为对照。提案体的平均直径为128至148 nm。药物的包封率在 42.9-52.7% 范围内，这意味着药物通过皮肤的渗透性显着增强。增强比为1.4至4.0，与logP、分子量和熔点线性相关。共聚焦成像还显示，提案体中的钙黄绿素和罗丹明 B 的皮肤渗透性高于溶液中的皮肤渗透性。发现该提案体对于皮肤应用是安全的。通过提案体增强药物的皮肤递送取决于药物的亲脂性。包封率与药物的logP呈正相关，从而导致药物吸收高。