Formulation, Optimization, and In vivo Evaluation of Curcumin–Quercetin Phytosome Tablets for the Management of Type 2 Diabetes Mellitus
摘要
Diabetes is a metabolic syndrome indicated by chronic hyperglycemia owing to inadequate secretion of insulin and insulin resistance. Present antidiabetic treatments are associated with inadequate bioavailability, side effects, and high costs. These challenges led to a diversion of the focus towards herbal-based therapies. Curcumin and quercetin, naturally occurring polyphenolic compounds, have demonstrated significant antidiabetic potential but are associated with low systemic bioavailability and poor solubility.
ObjectiveThe objective of the current research is to prepare and assess a polyherbal phytosome-loaded tablet formulation of curcumin and quercetin to augment their therapeutic potential in the management of Type 2 diabetes mellitus.
MethodsCurcumin and quercetin are incorporated in phytosomes to improve stability, solubility, and bioavailability. The phytosomes are characterized by their zeta potential, particle size, entrapment efficiency, and in vitro release properties. Response surface central composite design was used to optimize the phytosome formulation compressed into a tablet using microcrystalline cellulose (97.92-112.07 mg) and starch (18.55–28.22 mg) as dependent variables and hardness and disintegration time as the responses. The optimized formulation was evaluated for antidiabetic potential by the alloxan-induced model.
ResultsFormulations displayed acceptable disintegration time (30–37 min) and hardness (2.7–3.8 kg/cm2) with p value < 0.0001 and < 0.0297, respectively. The optimized formulation contained starch (27 mg) and microcrystalline cellulose (110 mg); it displayed a hardness of 3.7 kg/cm² and a disintegration time of 32 min. In vitro drug release from optimized formulation was about 72.79% for curcumin and 74.18% for quercetin, respectively. In vivo study indicated a reduction in SGPT (185.2 ± 0.48) and SGOT (25.5 ± 0.43) levels, leading to the protection of the pancreas with a higher dose of curcumin and quercetin, i.e., 50 mg/kg each.
DiscussionThe therapeutic potential of both phytoconstituents and bioavailability was boosted by phytosome-loaded tablet formulation. The optimized formulation demonstrated sustained drug release and better biochemical results in diabetic models.
ConclusionThe phytosomes-loaded tablet offers a safer, promising alternative for the management of diabetes with augmented efficacy, reduced side effects, and potential for clinical development.