Chauhan Swati, Jain Neha, Sharma Shilani, Mehra Shagun, Nagaich Upendra
Amity Institute of Pharmacy, Amity University, Sector-125, Noida, Uttar Pradesh-201303, India.
Adv Pharm Bull. 2021 May;11(3):490-496. doi: 10.34172/apb.2021.056. Epub 2020 Jul 15.
The aim of the present investigation was to formulate protein nanoparticles (PNPs) loaded suppositories for colon targeting of metronidazole (MZ), to achieve sustain release effect. PNPs were formulated via desolvation technique by utilizing 2 factorial design which results into eight formulations. The synthesized PNPs were characterized for different physicochemical and in vitro parameters . particle size, surface morphology, entrapment efficiency and zeta potential, drug- excipients compatibility studies. The formulated PNPs were found to be spherical in shape and have an average size in the range of 300.7 nm to 504.8 nm. Based on the results obtained, F7 was found to be the optimized formulation that was loaded into the suppository base. Furthermore, suppositories were also characterized for several parameters like content uniformity, weight variation and liquefaction time. Resultant, suppositories were free from pits, fissures and cracks. The release data of MZ-PNPs loaded suppositories were compared with the suppositories loaded with active ingredient only i.e. MZ. Screening against was also conducted. The results of drug release testing proved that protein nanoparticle loaded suppositories is a better approach, compared to pure MZ loaded suppositories. Release kinetic study concluded that the formulation follows Higuchi's equation i.e. having a biphasic release pattern. The efficiency of the formulated dosage form was evaluated using Indian earthworms, .
本研究的目的是制备用于甲硝唑(MZ)结肠靶向的载蛋白纳米颗粒(PNP)栓剂,以实现缓释效果。通过利用二因素设计的去溶剂化技术制备PNP,得到八种制剂。对合成的PNP进行了不同的物理化学和体外参数表征,包括粒径、表面形态、包封率和zeta电位、药物-辅料相容性研究。所制备的PNP呈球形,平均粒径在300.7nm至504.8nm范围内。根据所得结果,发现F7是优化的制剂,将其载入栓剂基质中。此外,还对栓剂的几个参数进行了表征,如含量均匀度、重量差异和液化时间。结果,栓剂无凹坑、裂缝和裂纹。将载MZ-PNP栓剂的释放数据与仅载有活性成分即MZ的栓剂进行了比较。还进行了抗菌筛选。药物释放测试结果证明,与纯载MZ栓剂相比,载蛋白纳米颗粒栓剂是一种更好的方法。释放动力学研究得出该制剂符合Higuchi方程,即具有双相释放模式。使用印度蚯蚓对所制备剂型的有效性进行了评估。