Bioassay Guided Fractionation of Anti-Hyperglycemic Compounds Extracted from Cheilocostus Specious, and Model Development for Sustained Release of Anti-Hyperglycemic Compounds Using Acarbose

Abstract

Cheilocostus speciosus (COS) leaves are traditionally used for managing diabetes, though prolonged consumption risks severe hypoglycemia. This study explored anti-hyperglycemic compounds from ethanol extracts of COS leaves and developed a sustained drug delivery system using montmorillonite (MMT). Ethanol extracts showed strong α-amylase and α-glucosidase inhibition (IC₅₀: 14.62 ppm and 21.20 ppm), comparable to acarbose, a standard diabetic drug. Active fractions were isolated via gravity column, size exclusion, and thin-layer chromatography, confirming COS leaves’ anti-hyperglycemic potential. To enhance therapeutic applicability, acarbose was intercalated into MMT as a nanocarrier for sustained release. X-ray diffraction confirmed increased interlayer spacing (1.185 nm to 1.403 nm) when increased acarbose concentration from 50-100 ppm, while intensified OH stretching peak in FTIR indicated acarbose integration into the clay matrix. Intercalation efficiency improved with higher acarbose concentrations (43.77% to 52.27%). In-vitro studies revealed controlled acarbose release over 8 hours (45.66%) and sustained slow release, following pseudo-second-order kinetics (r² = 0.9767). These findings suggest COS as a promising source of anti-diabetic compounds and highlight MMT's potential as a nanocarrier for safer, sustained therapies. Future research will focus on large-scale isolation, structural elucidation, and integration of active compounds into MMT for enhanced diabetic treatments.

Keywords: Cheilocostus speciosus, Ethanol extract, α–amylase inhibitor, α–glucosidase inhibitor, montmorillonite, sustained drug release