Investigation of keratolytic impact of synthetic bolalipids on skin penetration of a model hydrophilic permeant

IF 4.4 2区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2024-08-02 DOI:10.1016/j.ejpb.2024.114433

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Abstract

Synthetic single-chain bolalipids (SSCBs) are novel excipients in drug delivery, with potential as stabilizers or solubilizers. However, their impact on skin barrier function has not been comprehensively studied. Therefore, two SSCBs (PC-C24-PC and PC-C32-PC) were studied in aqueous systems for their impact on penetration of a model permeant into porcine skin. Concentrations of 0.05 – 5 % w/w were tested; PC-C24-PC formulations were low-viscosity liquids while PC-C32-PC formed viscous dispersions to gels at room temperature. Formulations were compared for their ability to enhance sodium fluorescein penetration (SF, 0.1 % w/w) into skin via tape stripping. Using NIR-densitometry, the effect of SSCB formulations on corneocyte cohesion was evaluated. Data were compared with phospholipid mixture Lipoid S-75, sodium dodecyl sulfate (SDS), and polyethylene glycol 12-hydroxystearate (PEG-HS), and distilled water as negative control. Contrary to the hypothesis, both SSCBs failed to increase SF penetration into the stratum corneum, but rather showed a significant decrease in penetration depth compared to water. Both SSCBs exhibited a keratolytic effect at 5 % w/w, leading to substantial removal of proteins from the skin surface. Consequently, SSCBs may not enhance penetration of hydrophilic drugs into skin, but could be used as keratolytic agents.

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合成栓脂对模型亲水性渗透剂皮肤渗透的角质溶解影响研究

合成单链硼烷脂（SSCBs）是一种新型给药辅料，具有稳定剂或增溶剂的潜力。然而，它们对皮肤屏障功能的影响尚未得到全面研究。因此，我们在水性体系中研究了两种 SSCB（PC-C24-PC 和 PC-C32-PC）对模型渗透剂渗入猪皮肤的影响。测试的浓度为 0.05 - 5 % w/w；PC-C24-PC 配方为低粘度液体，而 PC-C32-PC 则在室温下形成粘稠的分散体至凝胶体。通过胶带剥离，比较了这些配方增强荧光素钠（SF，0.1 % w/w）渗透皮肤的能力。使用近红外密度计评估了 SSCB 配方对角质细胞凝聚力的影响。数据与磷脂混合物 Lipoid S-75、十二烷基硫酸钠（SDS）和聚乙二醇 12-羟基硬脂酸酯（PEG-HS）以及作为阴性对照的蒸馏水进行了比较。与假设相反，两种 SSCB 都未能增加 SF 对角质层的渗透，与水相比，渗透深度反而显著下降。两种 SSCB 在 5% w/w 浓度下都具有角质溶解作用，导致皮肤表面的蛋白质大量脱落。因此，SSCB 可能不会增强亲水性药物对皮肤的渗透，但可用作角质分解剂。

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来源期刊

European Journal of Pharmaceutics and Biopharmaceutics 医学-药学

CiteScore

8.80

自引率

4.10%

发文量

211

审稿时长

36 days

期刊介绍： The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.