López Karla L, Ravasio Andrea, González-Aramundiz José Vicente, Zacconi Flavia C
Institute for Biological and Medical Engineering, Schools of Engineering, Medicine and Biological Sciences, Pontificia Universidad Católica de Chile, Santiago 7820436, Chile.
Escuela de Química, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Av. Vicuña Mackenna 4860, Macul, Santiago 7820436, Chile.
Pharmaceutics. 2023 Apr 25;15(5):1333. doi: 10.3390/pharmaceutics15051333.
Many pharmaceutically active molecules are highly lipophilic, which renders their administration and adsorption in patients extremely challenging. Among the countless strategies to overcome this problem, synthetic nanocarriers have demonstrated superb efficiency as drug delivery systems, since encapsulation can effectively prevent a molecules' degradation, thus ensuring increased biodistribution. However, metallic and polymeric nanoparticles have been frequently associated with possible cytotoxic side effects. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), which are prepared with physiologically inert lipids, therefore emerged as an ideal strategy to bypass toxicities issues and avoid the use of organic solvents in their formulations. Different approaches to preparation, using only moderate amounts of external energy to facilitate a homogeneous formation, have been proposed. Greener synthesis strategies have the potential to provide faster reactions, more efficient nucleation, better particle size distribution, lower polydispersities, and furnish products with higher solubility. Particularly microwave-assisted synthesis (MAS) and ultrasound-assisted synthesis (UAS) have been utilized in the manufacturing of nanocarrier systems. This narrative review addresses the chemical aspects of those synthesis strategies and their positive influence on the characteristics of SLNs and NLCs. Furthermore, we discuss the limitations and future challenges for the manufacturing processes of both types of nanoparticles.
许多具有药理活性的分子具有高度亲脂性,这使得它们在患者体内的给药和吸收极具挑战性。在克服这一问题的无数策略中,合成纳米载体作为药物递送系统已展现出卓越的效率,因为包封可以有效防止分子降解,从而确保生物分布增加。然而,金属和聚合物纳米颗粒经常与可能的细胞毒性副作用相关联。因此,由生理惰性脂质制备的固体脂质纳米颗粒(SLN)和纳米结构脂质载体(NLC)成为绕过毒性问题并避免在其配方中使用有机溶剂的理想策略。已经提出了不同的制备方法,仅使用适量的外部能量来促进均匀形成。更环保的合成策略有可能提供更快的反应、更有效的成核、更好的粒径分布、更低的多分散性,并提供具有更高溶解度的产品。特别是微波辅助合成(MAS)和超声辅助合成(UAS)已被用于纳米载体系统的制造。这篇叙述性综述阐述了这些合成策略的化学方面及其对SLN和NLC特性的积极影响。此外,我们讨论了这两种类型纳米颗粒制造过程的局限性和未来挑战。