Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)-Guwahati, Kamrup, Assam, India.
NIPER-Guwahati, Changsari-781 101, Kamrup, Assam, India.
Chem Phys Lipids. 2021 Mar;235:105037. doi: 10.1016/j.chemphyslip.2020.105037. Epub 2021 Jan 2.
Active plant constituents obtained from edible sources have manifested their pharmacological potential as a therapy against several diseases. But the lack of their desired physicochemical properties such as solubility, permeability ultimately leads to poor bioavailability. Two potent active plant constituents namely, quercetin and piperine having a problem with either solubility or permeability or both, and hence require an advanced lipid-mediated separate formulation system to improve their aforementioned concerns. Concerning advancement in nanoformulations, lipid-based nano-carriers systems have created their mark as a novel drug delivery system. Therefore, an advanced formulation like nanostructured lipid carriers (NLCs) has been formulated individually for both the active plant constituents/drugs through the solvent evaporation technique using high shear homogenization method followed by sonication. Compritol® 888 ATO, a solid lipid, and squalene as liquid lipid was used in their optimized ratios to formulate individual NLCs. Blank and individual drugs loaded NLCs were further characterized for their in vitro physicochemical properties. NLCs showed a negative surface charge with an average particle size below 200 nm. Electron microscopy images showed an anomalous structure of both the formulated NLCs with higher % drug encapsulation efficiency (DEE) with the desired in vitro drug release profile. In the case of quercetin-NLCs, 93.18 ± 5.5 % DEE was observed followed by drug release up to 45.0 ± 1.3 % within 12 h, while piperine-NLCs showed 91.80 ± 2.51 % DEE and drug release up to 38 ± 5.2 % at the same time. XRD and DSC plots showed the conversion of both the drugs into an amorphous structure encapsulated in a lyophilized NLCs matrix. Finally, the safety profile for formulated NLCs was confirmed by haemolysis assay. Hence, the developed active plant constituents enriched NLCs can further be delivered separately and/or in combination, and also may further be evaluated both in vitro and in vivo means.
从食用来源获得的活性植物成分已表现出其作为治疗多种疾病的疗法的药理学潜力。但是，它们缺乏所需的物理化学性质，例如溶解度、渗透性，最终导致生物利用度差。两种有效的活性植物成分，槲皮素和胡椒碱，要么存在溶解度或渗透性问题，要么两者都存在问题，因此需要先进的脂质介导的单独配方系统来改善上述问题。关于纳米制剂的进展，基于脂质的纳米载体系统已作为新型药物递送系统崭露头角。因此，通过溶剂蒸发技术，使用高剪切匀化方法随后进行超声处理，为两种活性植物成分/药物分别制备了先进的制剂，如纳米结构脂质载体 (NLC)。使用 Compritol®888 ATO（一种固体脂质）和角鲨烯作为液体脂质，以优化比例用于各自的 NLC 配方。空白和载药 NLC 进一步进行体外物理化学性质的表征。NLC 显示出负表面电荷，平均粒径小于 200nm。电子显微镜图像显示，两种配方的 NLC 均呈现异常结构，具有较高的药物包封效率 (DEE) 和所需的体外药物释放特性。在槲皮素-NLC 的情况下，观察到 93.18±5.5%的 DEE，随后在 12 小时内释放高达 45.0±1.3%的药物，而胡椒碱-NLC 则显示 91.80±2.51%的 DEE 和 38±5.2%的药物释放。XRD 和 DSC 图谱显示，两种药物均转化为包封在冻干 NLC 基质中的无定形结构。最后，通过溶血试验确认了所制备的 NLC 的安全性概况。因此，开发的富含活性植物成分的 NLC 可以单独或联合使用，并且还可以进一步在体外和体内进行评估。
