Phytochemical Characterization And Nanosponge-Based Delivery Of Bioactives From Moringa Oleifera, Glycyrrhiza Glabra, And Ficus Religiosa

Abstract

Background: Moringa oleifera, Glycyrrhiza glabra (licorice) and Ficus religiosa (sacred fig) have been traditionally used as medicinal plants and reported to possess anti-inflammatory, antidiabetic, and gastroprotective activities. However, the bioactive phytochemicals within them are frequently water-insoluble and unstable. To this end, a polyherbal formulation comprising of isolated phytomolecules quercetin (from M. oleifera), 18β-glycyrrhetinic acid (from G. glabra), and β-sitosterol (from F. religiosa) has been developed using β-cyclodextrin-based nanosponge drug delivery system in the present study.

Methods: The phytochemical was extracted, isolated and identified using spectral analysis. Nanosponges, namely β-cyclodextrin nanosponges were prepared, loaded with each phytochemical at optimized ratios and formulated as gastroretentive (floating) tablets.

 At a glance: The preliminary phytochemical screening revealed a high concentration of flavonoids, saponins and terpenoids in the plant extracts. Three compounds were isolated and their structures were determined as quercetin, 18β-glycyrrhetinic acid and β-sitosterol. Nanosponges encapsulating these phytomolecules were found to exhibit high encapsulation efficiencies (~81–85%) at an optimized 1:8 drug:polymer ratio, and to generate nanosized particles (200–232 nm) with low polydispersity and desirable zeta potentials (−20 mV) for stability. In vitro release studies revealed extended release profile of the phytomolecules from the nanosponges (77–83% release) over a period of 24 h. The floating system floated on the surface with no tendency to be drawn across the dissolution medium >12 h and was continuously expandable, releasing the drug in a sustained manner in simulated gastric fluid. In rats with ethanol-induced gastric ulcer model, the polyherbal nanosponge tablets elevated the gastric pH, inhibited the gastric acidity and ulcer index (by ~50% compared to ulcer control) and enhanced the mucosal defense (mucin levels) to an extent similar to that produced by omeprazole. The histopathology of gastric tissue showed that treated groups had highly maintained mucosal architecture in comparison to ulcerated controls.

Summary: Polyherbal β-cyclodextrin nanosponge system exhibited prolonged release and gastretentive delivery of three phytochemicals, leading to prominent gastroprotection. This new herbal combination utilizes the synergistic effects of herb–herb interaction and nanoparticle technology simultaneously, for optimal therapeutic efficacy. The finding highlights the prospect of nanosponge polyherbal formulations for enhanced therapeutics in the treatment of peptic ulcer and associated gastric ailments.