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pH-Responsive PLGA Nanoparticle for Controlled Payload Delivery of Diclofenac Sodium

机译:pH响应的PLGA纳米颗粒用于控制双氯芬酸钠的有效负载传递

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摘要

Poly(lactic-co-glycolic acid) (PLGA) based nanoparticles have gained increasing attention in delivery applications due to their capability for controlled drug release characteristics, biocompatibility, and tunable mechanical, as well as degradation, properties. However, thorough study is always required while evaluating potential toxicity of the particles from dose dumping, inconsistent release and drug-polymer interactions. In this research, we developed PLGA nanoparticles modified by chitosan (CS), a cationic and pH responsive polysaccharide that bears repetitive amine groups in its backbone. We used a model drug, diclofenac sodium (DS), a nonsteroidal anti-inflammatory drug (NSAID), to study the drug loading and release characteristics. PLGA nanoparticles were synthesized by double-emulsion solvent evaporation technique. The nanoparticles were evaluated based on their particle size, surface charge, entrapment efficacy, and effect of pH in drug release profile. About 390–420 nm of average diameters and uniform morphology of the particles were confirmed by scanning electron microscope (SEM) imaging and dynamic light scattering (DLS) measurement. Chitosan coating over PLGA surface was confirmed by FTIR and DLS. Drug entrapment efficacy was up to 52%. Chitosan coated PLGA showed a pH responsive drug release in in vitro. The release was about 45% more at pH 5.5 than at pH 7.4. The results of our study indicated the development of chitosan coating over PLGA nanoparticle for pH dependent controlled release DS drug for therapeutic applications.
机译:基于聚乳酸-乙醇酸(PLGA)的纳米颗粒由于其具有受控的药物释放特性,生物相容性和可调的机械以及降解特性,因此在递送应用中受到越来越多的关注。但是,在评估剂量倾倒,不一致的释放和药物-聚合物相互作用产生的颗粒的潜在毒性时,始终需要进行深入研究。在这项研究中,我们开发了由壳聚糖(CS)修饰的PLGA纳米颗粒,壳聚糖是一种阳离子和pH响应多糖,在其骨架上带有重复的胺基。我们使用模型药物双氯芬酸钠(DS)(一种非甾体类抗炎药(NSAID))来研究药物的负载和释放特性。通过双乳液溶剂蒸发技术合成了PLGA纳米颗粒。基于纳米颗粒的粒径,表面电荷,截留效果以及pH在药物释放曲线中的作用来评估纳米颗粒。通过扫描电子显微镜(SEM)成像和动态光散射(DLS)测量确认了颗粒的平均直径和均匀形态约为390-420 nm。通过FTIR和DLS证实在PLGA表面上的壳聚糖涂层。药物截留效率高达52%。壳聚糖包被的PLGA在体外显示出pH响应药物释放。在pH 5.5下的释放比在pH 7.4下的释放高约45%。我们的研究结果表明,PLGA纳米粒子上壳聚糖涂层的开发为pH依赖的控释DS药物的治疗应用。

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