Sodium Alginate Beads Containing Epalrestat for Effective Management of Diabetic Mellitus

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of Pharmaceutical Innovation Pub Date : 2025-01-22 DOI:10.1007/s12247-024-09905-y

Rashmi Madhariya, Alpana Ram, Akhlesh K. Jain

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Abstract

Purpose

Epalrestat is the most common Aldose reductase inhibitor (ARI) approved for blood glucose management in several countries and has also shown efficacy in preventing the onset of diabetic neuropathy (DN), and diabetic retinopathy. The present study aims to formulate and evaluate the effectiveness of Alginate beads of epalrestat in Streptozotocin-induced (STZ) diabetic rats in order to effectively manage the diabetes.

Method

Various formulations of Sodium cross-linked alginate beads containing epalrestat (F1 to F9) were prepared based on full factorial design by ionotropic gelation method. The formulations were characterized for particle size, % Drug entrapment efficiency (DEE), Fourier Transform Infra-Red Spectroscopy (FT-IR), Differential scanning calorimetry (DSC), X-ray Diffraction Study (X-RD), Scanning Electron Microscopy (SEM), and In-Vitro Release Studies. Optimized formulation (F6) [containing sodium alginate (2.5%w/v), epalrestat (2.5%w/v), and calcium chloride (2.5%w/v)] was subjected to in-Vivo efficacy testing in diabetic rats.

Result

Epalrestat-loaded beads were prepared (F1 to F9; Size = 3.21 μm; DEE = 97%) successfully using sodium alginate as polymer and calcium chloride solution as the crosslinking agent by modified ionotropic gelation method Optimized formulation showed a % DEE of 97% and highest drug release of 95% at the end of 10 hrs. Drug Release Kinetic of optimized formulation followed first-order kinetic. Further, the hypoglycemic effect was observed over a longer period 50% reduction after 2 hrs and continued till 4 hrs. In addition, normoglycemia was maintained till 12 hrs (20% reduction) in STZ-induced diabetic rats.

Conclusion

The formulation F6 was found to be superior compared to all the other formulations because the percentage drug entrapment efficiency was highest and there was no chemical interaction took place between the drug and polymer (Confirmed by DSC and XRD studies). In-vivo study showed prolonged hypoglycaemia till 12 hrs with a maximum reduction at 2 hrs Compared to plain drug suspension (20% reduction till 5 hrs).

Graphical Abstract

Abstract Image

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含有依帕司他的海藻酸钠微珠有效治疗糖尿病

目的：伊帕司他是几个国家批准用于血糖管理的最常见醛糖还原酶抑制剂（ARI），并且在预防糖尿病神经病变（DN）和糖尿病视网膜病变方面也显示出疗效。本研究旨在研究依帕司他海藻酸盐珠对链脲佐菌素诱导（STZ）糖尿病大鼠的治疗效果。方法采用离子化凝胶法制备了依帕司他交联海藻酸钠微球（F1 ~ F9）。采用粒径、药物包封率（DEE）、傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DSC）、x射线衍射（X-RD）、扫描电镜（SEM）和体外释放研究等方法对处方进行表征。优化配方（F6）[含海藻酸钠（2.5%w/v）、依帕司他（2.5%w/v）、氯化钙（2.5%w/v）]对糖尿病大鼠进行体内药效试验。结果制备palrestat负载微球(F1 ~ F9；尺寸= 3.21 μm；以海藻酸钠为聚合物，氯化钙溶液为交联剂，经改性的亲离子胶凝法制备的最佳配方在10 h后，DEE为97%，释药率最高达95%。优化制剂的释药动力学符合一级动力学。此外，在较长时间内观察到降糖效果，2小时后降低50%，并持续到4小时。此外，stz诱导的糖尿病大鼠血糖维持正常至12小时（降低20%）。结论配方F6的药物包封率最高，且药物与聚合物之间不发生化学相互作用（DSC和XRD研究证实了这一点），优于其他配方。体内研究显示，与普通药物混悬液相比，低血糖可延长至12小时，2小时最大限度地降低（5小时降低20%）。图形抽象

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.