Fang Jia-You, Hung Chi-Feng, Liao Mei-Hui, Chien Chih-Chen
Graduate Institute of Natural Products, Chang Gung University, Taoyuan, Taiwan.
Eur J Pharm Biopharm. 2007 Aug;67(1):67-75. doi: 10.1016/j.ejpb.2007.01.008. Epub 2007 Jan 27.
Acoustically active lipospheres (AALs) were prepared using perfluorocarbons and coconut oil as the cores of inner phase. These AALs were stabilized using coconut oil and phospholipid coatings. A lipophilic antioxidant, resveratrol, was the model drug loaded into the AALs. AALs with various percentages of perfluorocarbons and oil were prepared to examine their physicochemical and drug release properties. Co-emulsifiers such as Brij 98 and Pluronic F68 (PF68) were also incorporated into AALs for evaluation. AALs with high resveratrol encapsulation rates ( approximately 90%) were prepared, with a mean droplet size of 250-350nm. The AALs produced with perfluorohexane as the core material had larger particle sizes than those with perfluoropentane. Resveratrol in these systems exhibited retarded drug release in both the presence and absence of plasma in vitro; the formulations with high oil and perfluorocarbon percentages showed the lowest drug release rates. The addition of PF68 slightly but significantly reduced resveratrol delivery from the AALs. Ultrasound treatment of 1MHz produced an increase in the drug release from the systems, illustrating the drug-targeting effect of the combination of AALs and ultrasound.
使用全氟碳化合物和椰子油作为内相核心制备了具有声学活性的脂质体（AALs）。这些AALs通过椰子油和磷脂涂层进行稳定化处理。一种亲脂性抗氧化剂白藜芦醇作为模型药物被载入AALs中。制备了具有不同全氟碳化合物和油比例的AALs，以研究它们的物理化学性质和药物释放特性。共乳化剂如Brij 98和普朗尼克F68（PF68）也被加入到AALs中进行评估。制备出了白藜芦醇包封率较高（约90%）、平均液滴尺寸为250 - 350nm的AALs。以全氟己烷为核心材料制备的AALs比以全氟戊烷制备的具有更大的粒径。这些体系中的白藜芦醇在体外有无血浆存在的情况下均表现出药物释放延迟；油和全氟碳化合物比例高的制剂显示出最低的药物释放速率。添加PF68略微但显著地降低了白藜芦醇从AALs中的释放。1MHz的超声处理使体系中的药物释放增加，说明了AALs与超声联合的药物靶向作用。
