De Gaetano Federica, Celesti Consuelo, Paladini Giuseppe, Venuti Valentina, Cristiano Maria Chiara, Paolino Donatella, Iannazzo Daniela, Strano Vincenza, Gueli Anna M, Tommasini Silvana, Ventura Cinzia Anna, Stancanelli Rosanna
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno d'Alcontres 31, 98166 Messina, Italy.
Department of Engineering, University of Messina, Contrada Di Dio, 98166 Messina, Italy.
Pharmaceutics. 2023 May 28;15(6):1605. doi: 10.3390/pharmaceutics15061605.
In recent years, bioactive compounds have been the focus of much interest in scientific research, due to their low toxicity and extraordinary properties. However, they possess poor solubility, low chemical stability, and unsustainable bioavailability. New drug delivery systems, and among them solid lipid nanoparticles (SLNs), could minimize these drawbacks. In this work, morin (MRN)-loaded SLNs (MRN-SLNs) were prepared using a solvent emulsification/diffusion method, using two different lipids, Compritol 888 ATO (COM) or Phospholipon 80H (PHO). SLNs were investigated for their physical-chemical, morphological, and technological (encapsulation parameters and in vitro release) properties. We obtained spherical and non-aggregated nanoparticles with hydrodynamic radii ranging from 60 to 70 nm and negative zeta potentials (about -30 mV and -22 mV for MRN-SLNs-COM and MRN-SLNs-PHO, respectively). The interaction of MRN with the lipids was demonstrated via μ-Raman spectroscopy, X-ray diffraction, and DSC analysis. High encapsulation efficiency was obtained for all formulations (about 99%, /), particularly for the SLNs prepared starting from a 10% (/) theoretical MRN amount. In vitro release studies showed that about 60% of MRN was released within 24 h and there was a subsequent sustained release within 10 days. Finally, ex vivo permeation studies with excised bovine nasal mucosa demonstrated the ability of SLNs to act as a penetration enhancer for MRN due to the intimate contact and interaction of the carrier with the mucosa.
近年来,生物活性化合物因其低毒性和非凡特性成为科学研究的热点。然而,它们具有溶解度差、化学稳定性低和生物利用度不可持续等缺点。新型药物递送系统,其中包括固体脂质纳米粒(SLNs),可以将这些缺点降至最低。在这项工作中,使用溶剂乳化/扩散法,以两种不同的脂质Compritol 888 ATO(COM)或磷脂80H(PHO)制备了载有桑色素(MRN)的SLNs(MRN-SLNs)。对SLNs的物理化学、形态和工艺(包封参数和体外释放)特性进行了研究。我们获得了球形且无聚集的纳米颗粒,其流体动力学半径在60至70nm之间,zeta电位为负(MRN-SLNs-COM和MRN-SLNs-PHO的zeta电位分别约为-30mV和-22mV)。通过μ-拉曼光谱、X射线衍射和差示扫描量热法(DSC)分析证明了MRN与脂质之间的相互作用。所有制剂均获得了高包封率(约99%),特别是对于从10%(/)理论MRN量开始制备的SLNs。体外释放研究表明,约60%的MRN在24小时内释放,随后在10天内持续释放。最后,用切除的牛鼻黏膜进行的离体渗透研究表明,由于载体与黏膜的密切接触和相互作用,SLNs能够作为MRN的渗透促进剂。