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.
Ultrason Sonochem. 2018 Jan;40(Pt A):686-696. doi: 10.1016/j.ultsonch.2017.08.018. Epub 2017 Aug 19.
Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (IBP) are among the most prescribed drugs across the globe. However, most NSAIDs are insoluble in water leading them to have poor bioavailability and erratic absorption. Moreover, NSAIDs such as IBP and ketoprofen (KP) have to be administered very frequently due to their short plasma half-life leading to side effects. Controlled release formulations of IBP, KP and nabumetone (NBT) based on solid lipid nanoparticles (SLNs) were successfully synthesised in the present study to solve the above-mentioned challenges that are associated with NSAIDs. SLNs were prepared in two steps; hot-melt homogenization followed by sonication to formulate SLNs with spherical morphology. While capmul® GMS-50K (capmul) was used as the lipid due to the high solubility of the studied drugs in it, gelucire® 50/13 (gelucire) was used as the surfactant. It was found that particle size was directly proportional to drug concentration and inversely proportional to surfactant concentration, volume of water added and temperature of water. Ultrasonication in a pulse mode with optimum duration of 15min was essential to obtain smaller nanoparticles through the formation of a nanoemulsion. Drug loaded SLNs with small particle size and narrow size distribution with good solid loading, encapsulation efficiency and drug loading percentage could be prepared using the optimised conditions. SLNs prepared at the optimised condition were characterized thoroughly by using different techniques such as dynamic light scattering (DLS), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The cytotoxicity results showed that the prepared SLNs are non-toxic to Raw cell line. The drugs IBP, KP and NBT showed 53, 74 and 69% of percentage entrapment efficiency with drug loading of 6, 2 and 7% respectively. Slow, steady and sustained drug release was observed from the SLNs for over 6days.
非甾体抗炎药（NSAIDs），如布洛芬（IBP），是全球应用最广泛的药物之一。然而，大多数 NSAIDs 在水中的溶解度较低，导致其生物利用度差且吸收不稳定。此外，由于其血浆半衰期较短，IBP 和酮洛芬（KP）等 NSAIDs 必须频繁给药，导致副作用。本研究成功合成了基于固体脂质纳米粒（SLNs）的 IBP、KP 和萘普生（NBT）的控释制剂，以解决与 NSAIDs 相关的上述挑战。SLNs 通过两步法制备；热熔匀化后进行超声处理，以制备具有球形形态的 SLNs。由于研究药物在其中的高溶解度，使用 capmul® GMS-50K（capmul）作为脂质，而使用 gelucire® 50/13（gelucire）作为表面活性剂。结果发现，粒径与药物浓度成正比，与表面活性剂浓度、水的体积和水的温度成反比。采用脉冲模式进行超声处理，优化时间为 15min，对于通过形成纳米乳液获得更小的纳米颗粒至关重要。在优化条件下，可以制备具有小粒径和窄粒径分布、良好的固体载药量、包封效率和载药量的载药 SLNs。使用不同的技术（如动态光散射（DLS）、场发射扫描电子显微镜（FESEM）、透射电子显微镜（TEM）、原子力显微镜（AFM）、X 射线衍射（XRD）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR））对制备的 SLNs 进行了全面表征。细胞毒性结果表明，所制备的 SLNs 对 Raw 细胞系无毒性。IBP、KP 和 NBT 三种药物的包封效率分别为 53%、74%和 69%，载药量分别为 6%、2%和 7%。从 SLNs 中观察到超过 6 天的缓慢、稳定和持续的药物释放。
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