Brahmam Bheemisetty, Yarlagadda Dani Lakshman, Gurram Prasad Chowdari, Kumar Lalit, Shenoy Rekha R, Lewis Shaila A
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal- 576104, India.
Department of Quality of Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal- 576104, India.
Adv Pharm Bull. 2025 Jun 10;15(2):359-370. doi: 10.34172/apb.025.42583. eCollection 2025 Jul.
The present study aimed to fabricate microneedles (MNs) for transdermal delivery of insulin. Chitosan-conjugated carboxy phenyl boronic acid polymer was synthesized and characterized to load insulin in the form of nanoparticles.
Optimized insulin nanoparticles (ILN-NPs) were loaded into MN arrays by micromolding, and the resulting MN patches were characterized by scanning electron microscopy (SEM) and mechanical failure tests. The MNs were evaluated for skin insertion via a confocal laser scanning microscope. The in vivo efficacy (blood glucose levels [BGLs] and serum insulin concentration) of the MNs was studied in diabetic rats in comparison with traditional subcutaneous insulin injection.
In diabetic rats treated with MNs incorporated with insulin-loaded nanoparticles (ILN-MNs), the BGLs reached≤200 mg/dL at 2 h following the application of the ILN-MNs and maintained BGLs≤200 mg/dL from 2-8 h. The BGLs decreased to 29 mg/dL at 2 h following the subcutaneous administration of insulin. After 6 h, the BGLs rose to their initial level. These results were supported by the corresponding serum insulin concentrations.
The findings of this study demonstrate the reliability of the developed ILN-MNs for sustaining normal BGLs in diabetic rats. Therefore, it can be further explored as an approach for diabetes treatment to improve patient outcomes and quality of life.
本研究旨在制备用于胰岛素经皮递送的微针(MNs)。合成并表征了壳聚糖共轭羧基苯硼酸聚合物,以纳米颗粒形式负载胰岛素。
通过微成型将优化后的胰岛素纳米颗粒(ILN-NPs)加载到MN阵列中,所得MN贴片通过扫描电子显微镜(SEM)和机械失效测试进行表征。通过共聚焦激光扫描显微镜评估MNs对皮肤的插入情况。与传统皮下胰岛素注射相比,在糖尿病大鼠中研究了MNs的体内疗效(血糖水平[BGLs]和血清胰岛素浓度)。
在用负载胰岛素纳米颗粒的MNs(ILN-MNs)治疗的糖尿病大鼠中,在应用ILN-MNs后2小时,BGLs达到≤200mg/dL,并在2 - 8小时内维持BGLs≤200mg/dL。皮下注射胰岛素后2小时,BGLs降至29mg/dL。6小时后,BGLs回升至初始水平。相应的血清胰岛素浓度支持了这些结果。
本研究结果证明了所开发的ILN-MNs在维持糖尿病大鼠正常BGLs方面的可靠性。因此,它可作为一种糖尿病治疗方法进一步探索,以改善患者的治疗效果和生活质量。