| 郑迷雪,颜星星,吴仁杰,范婷,姚文栋.pH敏感载白藜芦醇PLGA纳米粒的制备及其体外评价[J].浙江中西医结合杂志,2023,33(3): |
| pH敏感载白藜芦醇PLGA纳米粒的制备及其体外评价 |
| Preparation and in vitro evaluation of resveratrol loaded pH sensitive nanoparticles |
| 投稿时间：2022-07-07 修订日期：2022-12-13 |
| DOI： |
| 中文关键词: 白藜芦醇 PLGA纳米粒 pH敏感 体外评价 复乳溶剂蒸发法 |
| 英文关键词:resveratrol PLGA nanoparticles pH sensitive in vitro evaluation double-emulsion solvent evaporation method |
| 基金项目:浙江省药学会医院药学专项科研资助项目（石药专项）（2019ZYY22, 2020ZYY04） |
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| 中文摘要: |
| 目的 通过pH敏感聚乳酸-羟基乙酸共聚物纳米粒(pH-PLGA-NP)的负载，改善白藜芦醇(resveratrol，RES)体内清除快、作用时间短的缺陷，使其具备pH敏感及缓释性。方法 以碳酸氢钠(NaHCO3)为pH响应因子结合复乳溶剂蒸发法制备pH敏感的PLGA纳米粒(pH-PLGA-NP)。pH-PLGA-NP载药后，离心纯化，减压干燥制得pH-PLGA-NP@RES；随之，透射电镜考察其形态；激光粒度分析仪考察粒径、Zeta电位和稳定性；HPLC法考察包封率和载药量；透析袋法考察其pH敏感性与体外释药特性。结果 制备的pH-PLGA-NP@RES粒径为(212.83 ± 1.92) nm，PDI为(0.24 ± 0.03)，Zeta电位为(-31.77 ± 1.65) mV。透射电镜观察其外观圆整均一；包封率为(82.01 ± 2.50)%，载药量为(7.89 ± 0.24)%。稳定性在加入NaHCO3及载药后，略有所下降。较原药相比，纳米粒负载后的RES体外突释降低，缓释特性明显；pH-PLGA-NP@RES在不同pH介质中展现pH敏感性，在低pH中释放显著加快。结论 本实验成功制备了pH-PLGA-NP@RES，并通过体外评价确定其pH敏感及缓释特性，有利于提高实体瘤的治疗效果。 |
| 英文摘要: |
| Objective A pH sensitive PLGA nanoparticles (pH-PLGA-NP) was designed and prepared to load resveratrol (RES) in order to remove the defects of quick clearance, providing pH sensitivity and sustained release. Methods Adding NaHCO3 as the pH response factor, pH-PLGA-NP@RES was synthesized by double emulsion solvent evaporation method, and free RES was removed by centrifugation after loading; The particle size, PDI, and Zeta potential of pH-PLGA-NP@RES were measured by Malvern particle size analyzer; then morphology was investigated by transmission electron microscopy; the entrapment efficiency and drug loading of pH-PLGA-NP@RES were measured by HPLC; the drug release behavior was studied by dialysis method under different pH conditions. Results The particle size, polydispersity coefficient (PDI), and Zeta potential of pH-PLGA-NP@RES were (212.83 ± 1.92) nm, (0.24 ± 0.03), (-31.77 ± 1.65) mV, with round and uniform shape. The encapsulation efficiency of pH-PLGA-NP@RES was (82.01 ± 2.50)%, while the drug loading rate was (7.89 ± 0.24)%, respectively. The stability of pH-PLGA-NP@RES decreased slightly after adding NaHCO3 and drug loading. Compared with the original drug, the in vitro release rate of RES after nanoparticle loading was reduced. PH-PLGA-NP@RES exhibited pH sensitivity in different pH media, and the release was significantly accelerated at low pH. Conclusion In this experiment, pH-PLGA-NP@RES was successfully prepared, and its pH-sensitive and sustained-release properties were determined by in vitro evaluation, which is beneficial to improve the therapeutic effect of solid tumors. |
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