This work describes the development of liposomes encapsulating curcumin (CURC) aiming to provide insights on the influence of CURC on the thermodynamic and skin permeation/penetration features of the vesicles. CURC-loaded liposomes were prepared by hydration of lipid film, in the 0.1-15% CURC:DPPC w/w ratio range. The obtained formulations were characterized for their size distribution, zeta potential and vesicle deformability, along with their thermodynamic properties and ex vivo skin penetration/permeation ability. Liposome size was 110-130 nm for all formulations, with fairly narrow size distribution (polydispersity index was ≤0.20) and a zeta potential mildly decreasing with CURC loading. DSC outcomes indicated that CURC interferes with the packing of DPPC acyl chains in liposome bilayer when CURC percentage was at least 10%, leading to a more fluid state than blank and low-payload vesicles. Consistently, the deformability index of liposomes with 15% CURC:DPPC was strongly increased compared to other formulations. This is congruent with ex vivo skin penetration/permeation results, which showed how more deformable liposomes showed an improved deposition in the epidermis, which acts as a reservoir for the active molecule. Altogether, results hint at a possible application of high payload liposomes for improved topical dermal accumulations of actives.

中文翻译：

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姜黄素脂质体的皮肤渗透和热力学特征。

这项工作描述了封装姜黄素的脂质体（CURC）的开发，旨在提供有关CURC对囊泡的热力学和皮肤渗透/渗透特征的影响的见解。通过脂质膜的水合制备负载CURC的脂质体，CURC：DPPC w / w比率范围为0.1-15％。获得的制剂的特征在于其尺寸分布，ζ电势和囊泡可变形性，以及它们的热力学性质和离体皮肤渗透/渗透能力。对于所有制剂，脂质体的大小为110-130 nm，具有相当窄的大小分布（多分散性指数≤0.20），并且zeta电位随CURC负载而轻度降低。DSC结果表明，当CURC百分比至少为10％时，CURC会干扰脂质体双层中DPPC酰基链的堆积，与空白和低有效载荷的囊泡相比，其流动性更高。一致地，与其他制剂相比，含15％CURC：DPPC的脂质体的可变形性指数大大提高。这与离体皮肤渗透/渗透的结果一致，后者显示出更多可变形的脂质体在表皮中显示出改善的沉积，这是活性分子的储存库。总之，结果提示高有效载荷脂质体可能用于改善活性物质的局部皮肤积累。该图显示了更多可变形的脂质体在表皮中的沉积改善了，这是活性分子的储存库。总之，结果提示高有效载荷脂质体可能用于改善活性物质的局部皮肤积累。该图显示了更多可变形的脂质体在表皮中的沉积改善了，这是活性分子的储存库。总之，结果提示高有效载荷脂质体可能用于改善活性物质的局部皮肤积累。