Luo Yang, Yang Lu, Feng Peipei, Qiu Haofeng, Wu Xujin, Lu Shuwei, Zhou Mi, Xu Long, Zhu Yabin
The Affiliated Hospital of Medical School, Ningbo University, Ningbo, China.
School of Medicine, Ningbo University, Ningbo, China.
Front Bioeng Biotechnol. 2020 Nov 5;8:581621. doi: 10.3389/fbioe.2020.581621. eCollection 2020.
Nanotechnology using biodegradable polymer carriers with good biocompatibility and bioabsorbability has been studied and applied extensively in drug delivery systems and biomedical engineering. In this work, the triblocked oligomer poly(L-lactide)--poly(ethylene glycol)--poly(L-lactide) (PLEL) with the molecular weight of 2.08 KDa was first synthesized. Its chemistry was characterized by hydrogen nuclear magnetic resonance (H-NMR) spectrum and Fourier transform infrared (FTIR) spectroscopy. Subsequently, the nanoparticles (NPs) of PLEL and pranoprofen (PF)-loaded PLEL were prepared with the average particle size of (151.7 ± 5.87) nm using the method of emulsion solvent evaporation. The formula and drug releasing profile were characterized by a transmission electron microscope (TEM), dynamic light scattering (DLS), and ultraviolet spectrophotometer (US). cytotoxicity assays and ophthalmic tests were performed to measure the safety and efficacy of the formulations. The results showed that PF NPs relieved the cytotoxicity of pure PF and eliminated ophthalmic irritation. The drug encapsulated in the nanoparticles displayed long-lasting release and good anti-inflammation efficiency in animal eyes. Therefore, we concluded that the present formula (PF NPs) could provide sustained drug release with good treatment effect on eye inflammation, and is promising for its use in ophthalmology in the future.
利用具有良好生物相容性和生物吸收性的可生物降解聚合物载体的纳米技术,已在药物递送系统和生物医学工程中得到广泛研究和应用。在本研究中,首先合成了分子量为2.08 kDa的三嵌段低聚物聚(L-丙交酯)-聚(乙二醇)-聚(L-丙交酯)(PLEL)。通过氢核磁共振(H-NMR)光谱和傅里叶变换红外(FTIR)光谱对其化学结构进行了表征。随后,采用乳液溶剂蒸发法制备了PLEL纳米颗粒(NPs)以及负载普拉洛芬(PF)的PLEL纳米颗粒,平均粒径为(151.7±5.87)nm。通过透射电子显微镜(TEM)、动态光散射(DLS)和紫外分光光度计(US)对配方和药物释放曲线进行了表征。进行了细胞毒性试验和眼科测试,以评估制剂的安全性和有效性。结果表明,PF纳米颗粒减轻了纯PF的细胞毒性并消除了眼部刺激。包裹在纳米颗粒中的药物在动物眼中显示出长效释放和良好的抗炎效果。因此,我们得出结论,目前的配方(PF纳米颗粒)可以提供持续的药物释放,对眼部炎症具有良好的治疗效果,并且在未来眼科应用中具有广阔前景。