Development and physicochemical characterization of solid lipid nanoparticles containing tinidazole

Nhan Ho Hoang, Ngoc Le Thi Thanh, Hao Le Hoang, Ny Tran Thi Kieu, Tuan Dao Anh
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Abstract

Background: Periodontitis is a chronic inflammation of the periodontal tissues. To increase the effectiveness of treatment, antibiotics selected should have a spectrum of action on bacteria causing periodontitis, while also meeting the requirements of cell penetration and prolonging of the retention time at the target site. Therefore, this study aimed at developing solid lipid nanoparticles (SLNs) containing tinidazole (TNZ-SLNs) oriented to be incorporated into the gel to increase the penetration ability and prolong drug retention time in periodontal tissues. Objectives: Therefore, this study aimed to develop and characterize solid lipid nanoparticles (SLNs) containing tinidazole (TNZ-SLNs) oriented to be incorporated into the gel to increase the penetration ability and prolong drug retention time in periodontal tissues. Methods: TNZ-SLNs were prepared by combining hot homogenization and solvent evaporation using different types of lipids and surfactants. Factors related to the formula and the preparation process were investigated, Design Expert 12.0, FormRules v2.0 and InForm v3.1 software were used to design experiments and optimize the formula. The prepared nanoparticles were characterized by particle size, polydispersity index (PDI), encapsulation efficiency (EE), etc. Results: The optimized formulation had a particle size of 197.60 ± 19.67 nm, a PDI of 0.247 ± 0.011, a zeta potential of -15.79 ± 0.75mV and an EE of 37.96 ± 0.91%. TNZ-SLNs showed prolonged in vitro drug release (for up to 24 hours), while TNZ material achieved about 100% drug release after 4 hours. Conclusion: TNZ-SLNs were successfully fabricated and physicochemically characterized. Key words: Tinidazole, solid lipid nanoparticles, periodontitis.
含替硝唑固体脂质纳米颗粒的制备及理化性质研究
背景:牙周炎是牙周组织的慢性炎症。为了提高治疗效果,所选择的抗生素应对引起牙周炎的细菌具有广谱的作用,同时还要满足细胞渗透和延长在靶部位停留时间的要求。因此,本研究旨在制备含替硝唑的固体脂质纳米颗粒(SLNs),以提高药物在牙周组织中的渗透能力,延长药物在牙周组织中的滞留时间。因此,本研究旨在开发并表征含替硝唑的固体脂质纳米颗粒(SLNs),该纳米颗粒定向掺入凝胶中,以提高药物在牙周组织中的渗透能力,延长药物在牙周组织中的滞留时间。方法:采用热均质和溶剂蒸发相结合的方法制备tnz - sln。研究了影响配方及制备工艺的因素,采用Design Expert 12.0、FormRules v2.0和InForm v3.1软件进行实验设计和配方优化。通过粒径、多分散性指数(PDI)、包封效率(EE)等指标对制备的纳米颗粒进行表征。结果:优化后的配方粒径为197.60±19.67 nm, PDI为0.247±0.011,zeta电位为-15.79±0.75mV, EE为37.96±0.91%。TNZ- sln的体外释药时间较长(可达24小时),而TNZ材料在4小时后释药达到100%左右。结论:成功制备了tnz - sln,并对其进行了物理化学表征。关键词:替硝唑,固体脂质纳米颗粒,牙周炎
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