Dymek Michał, Olechowska Karolina, Hąc-Wydro Katarzyna, Sikora Elżbieta
Faculty of Chemical Engineering and Technology, Cracow University of Technology, Warszawska 24, 31-155 Kraków, Poland.
Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Kraków, Poland.
Pharmaceutics. 2023 Oct 18;15(10):2485. doi: 10.3390/pharmaceutics15102485.
Liposomes are self-assembled spherical systems composed of amphiphilic phospholipids. They can be used as carriers of both hydrophobic and hydrophilic substances, such as the anti-aging and wound-healing copper-binding peptide, GHK-Cu (glycyl-L-histidyl-L-lysine). Anionic (AL) and cationic (CL) hydrogenated lecithin-based liposomes were obtained as GHK-Cu skin delivery systems using the thin-film hydration method combined with freeze-thaw cycles and the extrusion process. The influence of total lipid content, lipid composition and GHK-Cu concentration on the physicochemical properties of liposomes was studied. The lipid bilayer fluidity and the peptide encapsulation efficiency () were also determined. Moreover, in vitro assays of tyrosinase and elastase inhibition were performed. Stable GHK-Cu-loaded liposome systems of small sizes (approx. 100 nm) were obtained. The bilayer fluidity was higher in the case of cationic liposomes. As the best carriers, 25 mg/cm CL and AL hydrated with 0.5 mg/cm GHK-Cu were selected with of 31.7 ± 0.9% and 20.0 ± 2.8%, respectively. The obtained results confirmed that the liposomes can be used as carriers for biomimetic peptides such as copper-binding peptide and that the GHK-Cu did not significantly affect the tyrosinase activity but led to 48.90 ± 2.50% elastase inhibition, thus reducing the rate of elastin degeneration and supporting the structural integrity of the skin.
脂质体是由两亲性磷脂自组装形成的球形体系。它们可用作疏水性和亲水性物质的载体，如具有抗老化和伤口愈合作用的铜结合肽甘氨酰-L-组氨酰-L-赖氨酸（GHK-Cu）。采用薄膜水化法结合冻融循环和挤压工艺，制备了基于阴离子氢化卵磷脂（AL）和阳离子氢化卵磷脂（CL）的脂质体作为GHK-Cu的皮肤给药系统。研究了总脂质含量、脂质组成和GHK-Cu浓度对脂质体物理化学性质的影响。还测定了脂质双层流动性和肽包封率（）。此外，进行了酪氨酸酶和弹性蛋白酶抑制的体外测定。获得了尺寸较小（约100 nm）的稳定负载GHK-Cu的脂质体系统。阳离子脂质体的双层流动性较高。作为最佳载体，选择了用0.5 mg/cm GHK-Cu水化的25 mg/cm CL和AL，其包封率分别为31.7±0.9%和20.0±2.8%。所得结果证实脂质体可用作铜结合肽等仿生肽的载体，且GHK-Cu对酪氨酸酶活性无显著影响，但导致弹性蛋白酶抑制率达48.90±2.50%，从而降低了弹性蛋白的降解速率并维持了皮肤的结构完整性。
