Abstract：
Lipid-based nanocarriers have been extensively utilized for the solubilization and cutaneous delivery of water-insoluble active ingredients in skincare formulations. However, their practical application is often limited by structural instability, leading to premature release and degradation of actives. Here we present highly robust multilamellar nanovesicles, prepared by the polyionic self-assembly of unilamellar vesicles with hydrolyzed collagen peptides, to stabilize all-trans-retinol and enhance its cutaneous delivery. Our results reveal that the reinforced multilayer structure substantially enhances dispersion stability under extremely harsh conditions, like freeze-thaw cycles, and stabilizes the encapsulated retinol. Interestingly, these multilamellar vesicles exhibit significantly lower cytotoxicity to human dermal fibroblasts than their unilamellar counterparts, likely due to their smaller particle number per weight, minimizing potential disruptions to cellular membranes. In artificial skin models, retinol-loaded multilamellar vesicles effectively upregulate collagen-related gene expression while suppressing the synthesis of metalloproteinases. These findings suggest that the robust multilamellar vesicles can serve as effective nanocarriers for the efficient delivery and stabilization of bioactive compounds in cutaneous applications.
摘要：
基于脂质的纳米载体已广泛用于皮肤护理制剂中水不溶性活性成分的溶解和皮肤递送。然而,它们的实际应用往往受到结构不稳定性的限制，导致活性物质的过早释放和降解。在这里，我们提出了高度坚固的多层纳米囊泡，通过水解胶原蛋白肽的单层囊泡的多离子自组装制备，以稳定全反式视黄醇并增强其皮肤递送。我们的结果表明，增强的多层结构在极端恶劣的条件下大大提高了分散稳定性，像冻融循环，并稳定包封的视黄醇。有趣的是,这些多层囊泡对人真皮成纤维细胞的细胞毒性明显低于单层囊泡，可能是由于它们的单位重量颗粒数较小，最大限度地减少对细胞膜的潜在破坏。在人造皮肤模型中，负载视黄醇的多层囊泡有效上调胶原相关基因表达，同时抑制金属蛋白酶的合成。这些发现表明，强大的多层囊泡可以作为有效的纳米载体，用于在皮肤应用中有效递送和稳定生物活性化合物。
