Kumar Raj, Singh Ashutosh, Garg Neha
School of Basic Sciences, Advanced Material Research Centre, and Bio-X Research Centre, Indian Institute of Technology Mandi, Mandi 175005, Himachal Pradesh, India.
ACS Omega. 2019 Aug 7;4(8):13360-13370. doi: 10.1021/acsomega.9b01532. eCollection 2019 Aug 20.
Because of excellent bioavailability and high biocompatibility, solid lipid nanoparticles (SLNs) have gained attention in recent years, especially in drug delivery systems. SLNs are composed of a drug that is loaded in a lipid matrix and stabilized by surfactants. In this work, we have investigated the feasibility of the acoustic cavitation-assisted hot melt mixing method for the formulation of SLNs using different stabilizers. A lipid Compritol 888 ATO (CPT) and a poorly water-soluble drug ketoprofen (KP) were used as a model lipid and drug, respectively. Gelucire 50/13 (GEL), poloxamer 407 (POL), and Pluronic F-127 (PLU) were used as the stabilizers. The effect of the stabilizers on the physico-chemical properties of SLNs was thoroughly studied in this work. The particle size and stability in water at different temperatures were measured using a dynamic light scattering method. The spherical shape (below 250 nm) and core-shell morphology were confirmed by field-emission scanning electron microscopy and transmission electron microscopy. The chemical, crystal, and thermal properties of SLNs were studied by FTIR, XRD analysis, and DSC, respectively. SLNs prepared using different stabilizers showed an encapsulation efficiency of nearly 90% and a drug loading efficiency of 12%. SLNs showed more than 90% of drug released in 72 h and increased with pH was confirmed using in vitro drug release studies. SLNs were nontoxic to raw 264.7 cells. All stabilizers were found suitable for acoustic cavitation-assisted SLN formulation with high encapsulation efficiency and drug loading and good biocompatibility.
由于具有出色的生物利用度和高生物相容性，固体脂质纳米粒（SLNs）近年来受到了关注，尤其是在药物递送系统中。固体脂质纳米粒由负载在脂质基质中并通过表面活性剂稳定的药物组成。在这项工作中，我们研究了使用不同稳定剂通过声空化辅助热熔混合法制备固体脂质纳米粒的可行性。分别使用脂质Compritol 888 ATO（CPT）和水溶性差的药物酮洛芬（KP）作为模型脂质和药物。使用Gelucire 50/13（GEL）、泊洛沙姆407（POL）和普朗尼克F - 127（PLU）作为稳定剂。在这项工作中深入研究了稳定剂对固体脂质纳米粒物理化学性质的影响。使用动态光散射法测量不同温度下在水中的粒径和稳定性。通过场发射扫描电子显微镜和透射电子显微镜确认了球形形状（低于250 nm）和核壳形态。分别通过傅里叶变换红外光谱（FTIR）、X射线衍射分析（XRD）和差示扫描量热法（DSC）研究了固体脂质纳米粒的化学、晶体和热性质。使用不同稳定剂制备的固体脂质纳米粒显示包封率接近90%，载药效率为12%。通过体外药物释放研究证实，固体脂质纳米粒在72小时内药物释放超过90%，且随pH值升高而增加。固体脂质纳米粒对原代264.7细胞无毒。发现所有稳定剂都适用于声空化辅助的固体脂质纳米粒制剂，具有高包封率和载药量以及良好的生物相容性。
