Institut Galien Paris-Sud, Université Paris-Saclay, Labex LERMIT, 92296, Châtenay-Malabry, France.
Lip(Sys)² Chimie Analytique Pharmaceutique, EA7357 Université Paris-Saclay, 92296, Châtenay-Malabry, France.
Colloids Surf B Biointerfaces. 2020 Nov;195:111242. doi: 10.1016/j.colsurfb.2020.111242. Epub 2020 Jul 3.
The aim of this paper is to investigate the time and thermal stability of innovative multicompartmental nanoparticles. These particles, having a hydrophilic side and a hydrophobic side, belong to the family of Janus particles and are promising tools to carry active ingredients with opposite solubilities in a unique nanocarrier. The stability of nanoparticles obtained with mainly two types of polyoxylglycerides (Labrafil® M2125 CS and Labrafil® M1944 CS) has been investigated. The suspensions describe a two-step maturation/destabilization process with an Ostwald ripening phase followed by the coalescence of the particles. The effect of lipid composition and temperature on these steps has been investigated in deep as stability with temperature is a critical parameter to consider in order to envisage the development of any formulation for pharmaceutical or cosmetic uses. These nanoparticles were particularly stable at room temperature as their hydrodynamic diameter did not change significantly for 20 months. Contrarily, a strong dependency to temperature appears when storage temperature increases from 25 °C to 43 °C. Indeed, Labrafil® M1944 CS seemed to undergo a progressive destabilization where a significant increase of particles size is visible from 25 °C and phase separation occurred after 4 months at 32 °C. At the opposite, Labrafil® M2125 CS remained stable until 36 °C and reached a threshold temperature between 32 °C and 36 °C after which Labrafil® M2125 CS underwent a consequent increase of particles size at the longer time, i.e. after 6 months. Moreover, Labrafil® M2125 CS formulation was stable at least 3 months at 43 °C.
本文旨在研究创新型多腔室纳米粒子的时间和热稳定性。这些粒子具有亲水侧和疏水侧，属于扬努斯粒子家族，是携带在单一纳米载体中具有相反溶解度的活性成分的有前途的工具。研究了主要由两种聚氧甘油酯（Labrafil® M2125 CS 和 Labrafil® M1944 CS）获得的纳米粒子的稳定性。悬浮液描述了一个两步成熟/失稳过程，具有奥斯特瓦尔德成熟阶段，随后是粒子的聚结。深入研究了脂质组成和温度对这些步骤的影响，因为稳定性是温度是考虑任何药物或化妆品制剂开发的关键参数。这些纳米粒子在室温下特别稳定，因为它们的水动力直径在 20 个月内没有明显变化。相反，当储存温度从 25°C 升高到 43°C 时，对温度的依赖性很强。事实上，Labrafil® M1944 CS 似乎经历了渐进的失稳，从 25°C 开始，粒子尺寸显著增加，在 32°C 时发生相分离。相反，Labrafil® M2125 CS 在 36°C 之前保持稳定，在 32°C 和 36°C 之间达到一个阈值温度后，Labrafil® M2125 CS 在较长时间后，即 6 个月后，粒子尺寸会相应增加。此外，Labrafil® M2125 CS 制剂在 43°C 下至少稳定 3 个月。
