Sharma Rajeev, Gupta Umesh, Garg Neeraj K, Tyagi Rajeev K, Jain N K
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Central University, Sagar, MP 470003, India.
Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer Rajasthan 305817, India.
Colloids Surf B Biointerfaces. 2015 Mar 1;127:172-81. doi: 10.1016/j.colsurfb.2015.01.035. Epub 2015 Jan 29.
The present study was designed to enhance intestinal absorption of insulin by nanobioconjugate formulated with PEGylation and Concanavalin A based targeted synergistic approach. The attempts were aimed at maximizing bioavailability and therapeutic efficacy of insulin by incorporating it in Concanavalin A anchored PEGylated nanoconstructs. The Con A anchored PEGylated PLGA diblock copolymer was synthesized by modified surface functionalization method, and was then characterized by FTIR and 1H NMR spectrum analysis. The nanoparticles from synthesized polymers were prepared and characterized for mean size and distribution by laser diffraction spectroscopy. The physicochemically characterized (by SEM and TEM) formulations were evaluated for optimum particle size, polydispersity index, zeta potential and entrapment efficiency 196.3±4.5 nm, 0.15±0.04, -25.6±1.68 and 44.6±3.5% respectively. The insulin encapsulation efficiency and in vitro release were assessed by bicinchoninic protein assay (BCA). The in vitro results corroborated in vivo studies carried out in experimentally created diabetic albino rats. The nano-encapsulated insulin was discovered to meet the requirements by achieving better stability, improved absorption and enhanced oral bioavailability elucidated by in vivo and in vitro bioassays.
本研究旨在通过基于聚乙二醇化和伴刀豆球蛋白A的靶向协同方法制备的纳米生物缀合物来增强胰岛素的肠道吸收。这些尝试旨在通过将胰岛素掺入伴刀豆球蛋白A锚定的聚乙二醇化纳米结构中来最大化胰岛素的生物利用度和治疗效果。通过改进的表面功能化方法合成了伴刀豆球蛋白A锚定的聚乙二醇化聚乳酸-羟基乙酸共聚物二嵌段共聚物，然后通过傅里叶变换红外光谱（FTIR）和核磁共振氢谱（1H NMR）分析对其进行表征。由合成聚合物制备纳米颗粒，并通过激光衍射光谱法对其平均粒径和分布进行表征。对经物理化学表征（通过扫描电子显微镜和透射电子显微镜）的制剂评估其最佳粒径、多分散指数、zeta电位和包封率，分别为196.3±4.5 nm、0.15±0.04、-25.6±1.68和44.6±3.5%。通过双辛可宁酸蛋白测定法（BCA）评估胰岛素的包封效率和体外释放。体外结果证实了在实验性诱导的糖尿病白化大鼠中进行的体内研究。通过体内和体外生物测定法表明，纳米包裹的胰岛素具有更好的稳定性、改善的吸收和增强的口服生物利用度，符合要求。
