School of Basic Sciences, Indian Institute of Technology Mandi, Mandi 175005, Himachal Pradesh, India; Advanced Material Research Centre, Indian Institute of Technology Mandi, Mandi 175005, Himachal Pradesh, India.
School of Basic Sciences, Indian Institute of Technology Mandi, Mandi 175005, Himachal Pradesh, India; Advanced Material Research Centre, Indian Institute of Technology Mandi, Mandi 175005, Himachal Pradesh, India; Bio-X Research Centre, Indian Institute of Technology Mandi, Mandi 175005, Himachal Pradesh, India.
Mater Sci Eng C Mater Biol Appl. 2020 Jan;106:110184. doi: 10.1016/j.msec.2019.110184. Epub 2019 Sep 10.
There is an increasing attention on solid lipid nanoparticles (SLNs) due to their high biocompatibility and ability to enhance bioavailability for poorly water-soluble drugs. Preparation of SLNs that are capable of high drug loading and sustained drug release through hot melt sonication method is reported here. SLNs of palmitic acid and stearic acid loaded with poorly water-soluble drugs, viz. fenofibrate (FF) and nabumetone (NBT) having spherical morphology and average particle size below 200 nm were prepared. Poloxamer 407 and pluronic® F-127 were used as surfactants. Particle size and spherical morphology was confirmed by dynamic light scattering, field emission scanning electron microscopy, transmission electron microscopy, and atomic force microscopy. The chemical, crystal, and thermal properties of SLNs were studied by Fourier transform infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry, respectively. The palmitic acid-poloxamer 407 SLNs could entrap upto 13.8% FF with 80% entrapment efficiency while the stearic acid-pluronic® F-127 SLNs entrapped 13.6% NBT with 89% entrapment efficiency. The drug loaded in SLNs showed controlled release up to 3 days as confirmed by in-vitro drug release profile. Moreover, the drug loaded SLNs did not show any toxicity on macrophage cell line proving the use of these formulations as control drug delivery vehicles for the studied drugs.
由于固体脂质纳米粒（SLNs）具有高生物相容性和提高难溶性药物生物利用度的能力，因此越来越受到关注。本文报道了一种通过热熔超声法制备能够高载药和持续释放药物的 SLNs 的方法。制备了负载难溶性药物非诺贝特（FF）和萘丁美酮（NBT）的棕榈酸和硬脂酸 SLNs，其具有球形形态和平均粒径低于 200nm。使用泊洛沙姆 407 和泊洛沙姆 F-127 作为表面活性剂。通过动态光散射、场发射扫描电子显微镜、透射电子显微镜和原子力显微镜确认了粒径和球形形态。通过傅里叶变换红外光谱、X 射线衍射和差示扫描量热法分别研究了 SLNs 的化学、晶体和热性质。棕榈酸-泊洛沙姆 407 SLNs 可以包封高达 13.8%的 FF，包封效率为 80%，而硬脂酸-泊洛沙姆 F-127 SLNs 可以包封 13.6%的 NBT，包封效率为 89%。载药 SLNs 表现出长达 3 天的控制释放，这通过体外药物释放曲线得到证实。此外，载药 SLNs 对巨噬细胞系没有显示出任何毒性，证明这些制剂可作为研究药物的控释药物递送载体。
