Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santos Dumont 964, 4to piso, Of. 09, Independencia, 8380494, Santiago, Chile.
Advanced Center for Chronic Diseases (ACCDiS), 8380494, Santiago, Chile.
Drug Deliv Transl Res. 2018 Dec;8(6):1807-1814. doi: 10.1007/s13346-018-0521-9.
High-energy methods for the manufacturing of nanomedicines are widely used; however, interest in low-energy methods is increasing due to their simplicity, better control over the process, and energy-saving characteristics during upscaling. Here, we developed a novel lipid-core micelle (LCM) as a nanocarrier to encapsulate a poorly water-soluble drug, nifedipine (NFD), by hot-melt emulsification, a low-energy method. LCMs are self-assembling colloidal particles composed of a hydrophobic core and a hydrophilic shell. Hybrid materials, such as Gelucire 44/14, are thus excellent candidates for their preparation. We characterized the obtained nanocarriers for their colloidal properties, drug loading and encapsulation efficiency, liquid state, stability, and drug release. The low-energy method hot-melt emulsification was successfully adapted for the manufacturing of small and narrowly dispersed LCMs. The obtained LCMs had a small average size of ~ 11 nm and a narrow polydispersity index (PDI) of 0.228. These nanocarriers were able to increase the amount of NFD dispersible in water more than 700-fold. Due to their sustained drug release profile and the PEGylation of Gelucire 44/14, these nanocarriers represent an excellent starting point for the development of drug delivery systems designed for long circulation times and passive targeting.
高能方法广泛用于纳米药物的制造;然而,由于其简单性、更好的过程控制以及在放大过程中的节能特性,人们对低能量方法的兴趣日益增加。在这里,我们开发了一种新型的脂质核胶束(LCM)作为纳米载体,通过热熔乳化(一种低能量方法)来封装疏水性差的药物硝苯地平(NFD)。LCM 是由疏水性核和亲水性壳组成的自组装胶体颗粒。因此,混合材料,如 Gelucire 44/14,是其制备的绝佳候选材料。我们对所得纳米载体的胶体性质、载药量和包封效率、液体状态、稳定性和药物释放进行了表征。成功地将低能量方法热熔乳化法适用于小而分散性良好的 LCM 的制造。所得的 LCM 具有约 11nm 的小平均粒径和 0.228 的窄多分散指数(PDI)。这些纳米载体能够将 NFD 在水中的分散量增加 700 多倍。由于其持续的药物释放特性和 Gelucire 44/14 的 PEG 化,这些纳米载体为开发设计用于长循环时间和被动靶向的药物递送系统提供了一个极好的起点。