Department of Pharmaceutical Technology, National Facility for Drug Development (NFDD), BIT Campus, Anna University, Tiruchirappalli, 620 024, Tamilnadu, India.
Department of Pharmaceutical Technology, BIT Campus, Anna University, Tiruchirappalli, 620 024, Tamilnadu, India.
Int J Biol Macromol. 2017 Nov;104(Pt B):1837-1845. doi: 10.1016/j.ijbiomac.2017.04.117. Epub 2017 May 1.
Natural anti-oxidants resveratrol (RES) and quercetin (QUR) posses the ability to reduce intra ocular pressure efficiently. Concurrent administration of RES and QUR was able to enhance the bioavailability of RES. Present research work describes upsurge of QUR in RES loaded chitosan (CS) nanoparticles (NPs) and polyethylene glycol (PEG) modified CS NPs for improved delivery and synergic effects on reducing intra ocular pressure for the treatment of glaucoma. CS NPs and PEG modified CS NPs were prepared by ionic gelation of tripolyphosphate and CS. The synthesised NPs were spherical in shape and RES entrapment and loading efficiency in the formulation decreased with increasing PEG concentration. Particle size of the formulation increased while incorporating PEG and drugs. The crystalline nature of RES and QUR changed in the NPs and that was confirmed by XRD study. Free radical neutralising efficiency improved while incorporating QUR in the formulation. Ex-vivo corneal permeation of RES was higher from RES and QUR loaded formulation than RES alone containing NPs and free RES dispersion. RES and QUR loaded PEG modified CS NPs showed sustained and enhanced reduction of intra ocular pressure (5.5±0.5mmHg) in normotensive rabbits.
天然抗氧化剂白藜芦醇（RES）和槲皮素（QUR）具有有效降低眼内压的能力。RES 和 QUR 的联合给药能够提高 RES 的生物利用度。本研究工作描述了 QUR 在 RES 负载壳聚糖（CS）纳米粒子（NPs）和聚乙二醇（PEG）修饰的 CS NPs 中的增加，以改善输送并协同降低眼压以治疗青光眼。CS NPs 和 PEG 修饰的 CS NPs 通过三聚磷酸和 CS 的离子凝胶化制备。合成的 NPs 呈球形，随着 PEG 浓度的增加，制剂中 RES 的包封和载药效率降低。在加入 PEG 和药物时，制剂的粒径增加。XRD 研究证实了 NPs 中 RES 和 QUR 的晶体性质发生了变化。在制剂中加入 QUR 可提高自由基清除效率。与含有 RES 的 NPs 和游离 RES 分散体相比，从 RES 和 QUR 负载的制剂中，RES 的角膜体外渗透更高。RES 和 QUR 负载的 PEG 修饰的 CS NPs 在正常眼压兔中显示出持续和增强的眼压降低（5.5±0.5mmHg）。
