Rathore Priyanka, Mahor Alok, Jain Surendra, Haque Anzarul, Kesharwani Prashant
Sagar Institute of Research and Technology Pharmacy Bhopal India.
Institute of Pharmacy, Bundelkhand University Jhansi India
RSC Adv. 2020 Dec 8;10(71):43629-43639. doi: 10.1039/d0ra07640f. eCollection 2020 Nov 27.
Insulin-dependent diabetic patients have to count on the administration of painful and discomforting insulin injections. However, inadequate insulin absorption and the risk of insulin level escalation in the blood are some disadvantages associated with insulin therapy. Thus, the current study intends to formulate insulin-loaded chitosan nanoparticles for refining the systemic absorption of insulin the ocular route. Insulin-loaded chitosan nanoparticles were prepared by the ionotropic gelation method and characterized for various parameters. Optimized insulin loaded nanoparticles (C4T4I4) were positively charged with a particle size of 215 ± 2.5 nm and showed 65.89 ± 4.3% entrapment efficiency. The drug release exhibited sustained release of insulin, where 77.2 ± 2.1% of release was observed after 12 h and leads to an assumption of the non-Fickian diffusion release mechanism. The permeation study discloses good mucoadhesive and better permeation properties of insulin loaded nanoparticles compared to free Insulin. No significant difference was observed in the size of particles after six months of storage, signifying their adequate stability. Nanoparticles were found to be non-irritant to ocular tissues and exhibited prominent blood glucose level reduction . The outcomes of this study suggested that the chitosan nanoparticulate system could act as a prominent carrier system for insulin with enhanced stability and efficacy.
胰岛素依赖型糖尿病患者不得不依靠注射带来疼痛和不适的胰岛素。然而，胰岛素吸收不足以及血液中胰岛素水平升高的风险是胰岛素治疗的一些缺点。因此，本研究旨在制备载胰岛素的壳聚糖纳米颗粒，以改善胰岛素通过眼部途径的全身吸收。通过离子凝胶法制备了载胰岛素的壳聚糖纳米颗粒，并对其各项参数进行了表征。优化后的载胰岛素纳米颗粒（C4T4I4）带正电荷，粒径为215±2.5nm，包封率为65.89±4.3%。药物释放显示胰岛素呈持续释放，12小时后释放率为77.2±2.1%，表明其符合非菲克扩散释放机制。渗透研究表明，与游离胰岛素相比，载胰岛素纳米颗粒具有良好的黏膜黏附性和更好的渗透性能。储存六个月后，颗粒大小没有显著差异，表明其稳定性良好。纳米颗粒对眼部组织无刺激性，并能显著降低血糖水平。本研究结果表明，壳聚糖纳米颗粒系统可作为一种出色的胰岛素载体系统，具有更高的稳定性和疗效。
