Department of Nanoengineering, University of California at San Diego, La Jolla, California 92093, USA.
ACS Nano. 2010 Apr 27;4(4):1935-42. doi: 10.1021/nn9018587.
We report a new approach to controlling the fusion activity of liposomes by adsorbing carboxyl-modified gold nanoparticles to the outer surface of phospholipid liposomes. The bound gold nanoparticles can effectively prevent liposomes from fusing with one another at neutral pH value, while at acidic environments (e.g., pH < 5), the gold particle stabilizers will detach from the liposomes, with liposome fusion activity resuming. The binding of carboxyl-modified gold nanoparticles to cationic phospholipid liposomes at neutral pH and detaching at acidic pH values are evaluated and confirmed by dynamic light scattering, electron microscopy, fluorescence and UV-vis absorption experiments. The relative fusion efficiency of gold-nanoparticle-stabilized cationic liposomes with anionic liposomes is approximately 25% at pH = 7 in contrast to approximately 80% at pH = 4. Since liposomes have been extensively used as drug nanocarriers and the infectious lesions on human skin are typically acidic with a pH < 5, these acid-responsive liposomes with tunable fusion ability hold great promise for dermal drug delivery to treat a variety of skin diseases such as acne vulgaris and staph infections.
我们报告了一种新的方法来控制脂质体的融合活性,方法是将羧基修饰的金纳米粒子吸附到磷脂脂质体的外表面。结合的金纳米粒子可以有效地防止脂质体在中性 pH 值下彼此融合,而在酸性环境下(例如,pH 值<5),金颗粒稳定剂将从脂质体上脱离,脂质体融合活性恢复。通过动态光散射、电子显微镜、荧光和紫外可见吸收实验评估和证实了羧基修饰的金纳米粒子在中性 pH 值下与阳离子磷脂脂质体的结合以及在酸性 pH 值下的脱离。在 pH = 7 时,金纳米粒子稳定的阳离子脂质体与阴离子脂质体的相对融合效率约为 25%,而在 pH = 4 时约为 80%。由于脂质体已被广泛用作药物纳米载体,并且人类皮肤的感染病变通常呈酸性,pH 值<5,因此这种具有可调节融合能力的酸响应脂质体有望用于经皮递药治疗各种皮肤病,如寻常痤疮和葡萄球菌感染。