Department of Chemical Engineering, Brigham Young University, Provo, UT 84602, USA.
J Control Release. 2013 Apr 10;167(1):92-100. doi: 10.1016/j.jconrel.2013.01.009. Epub 2013 Jan 23.
eLiposomes are liposomes encapsulating emulsions and therapeutics for targeted delivery. By applying ultrasound to eLiposomes, emulsion droplets can transform from liquid to gas and rupture the lipid bilayer of the eLiposome to release a drug or plasmid. In this study, perfluoropentane (PFC5) emulsions were encapsulated inside folated eLiposomes carrying a model drug (calcein) or a model GFP plasmid to examine the effects of a folate ligand, PFC5 emulsion and various ultrasonic acoustic parameters in drug delivery and gene transfection into HeLa cells. Confocal microscopy was used to quantify drug delivery and the level of plasmid transfection into HeLa cells. The results showed that drug delivery or transfection was minimal without incorporation of internal PFC5 emulsions and folate ligand on the eLiposome surface. It was also shown that application of ultrasound greatly enhanced the drug delivery and plasmid transfection. Delivery of these therapeutics appears to be to the cytosol, indicating that the expansion of the emulsion droplets disrupted both the eLiposomes and the endosomes.
电脂质体是包封乳液和治疗剂的脂质体，用于靶向递药。通过向电脂质体施加超声，可以使乳液液滴从液体变为气体，并破坏电脂质体的脂质双层，从而释放药物或质粒。在这项研究中，全氟戊烷 (PFC5) 乳液被包裹在携带模型药物（钙黄绿素）或模型 GFP 质粒的叶酸化电脂质体中，以研究叶酸配体、PFC5 乳液和各种超声声参数在递药和基因转染到 HeLa 细胞中的作用。共聚焦显微镜用于定量测定药物递药和质粒转染到 HeLa 细胞的水平。结果表明，没有内部 PFC5 乳液和叶酸配体在电脂质体表面的情况下，药物递药或转染很少。还表明，超声的应用大大增强了药物递药和质粒转染。这些治疗剂的递药似乎是到细胞质，表明乳液液滴的膨胀破坏了电脂质体和内体。
