Self-nanoemulsifying composition containing curcumin, quercetin, Ganoderma lucidum extract powder and probiotics for effective treatment of type 2 diabetes mellitus in streptozotocin induced rats

Liquid self-nanoemulsifying drug delivery system (L-SNEDDS) of curcumin and quercetin were prepared by dissolving them in isotropic mixture of Labrafil M1944CS®, Capmul MCM®, Tween-80® and Transcutol P®. The prepared L-SNEDDS were solidified using Ganoderma lucidum extract, probiotics and Aerosil-200® using spray drying. These were further converted into pellets using extrusion-spheronization.

Highlights

Curcumin and quercetin loaded SD-S-SNEDDS pellets were formulated.

Ganoderma lucidum mushroom extract and probiotics were used as solid carriers.

SNEDDS pellets showed enhanced dissolution rate and permeability of CUR and QUE.

SNEDDS pellets showed significant increase in oral bioavailability of CUR and QUE.

SNEDDS pellets showed excellent antidiabetic activity for CUR-QUE in diabetic rats.

The mean droplet size and zeta potential of L-SNEDDS were found to be 63.46 ± 2.12 nm and – 14.8 ± 3.11 mV while for solid SNEDDS pellets, these were 72.46 ± 2.16 nm and -38.7 ± 1.34 mV, respectively. The dissolution rate for curcumin and quercetin each was enhanced by 4.5 folds while permeability was enhanced by 5.28 folds (curcumin) and 3.35 folds (quercetin) when loaded into SNEDDS pellets. The Cmax for curcumin and quercetin containing SNEDDS pellets was found 532.34 ± 5.64 ng/mL and 4280 ± 65.67 ng/mL, respectively. This was 17.55 and 3.48 folds higher as compared to their naïve forms.

About 50.23- and 5.57-folds increase in bioavailability was observed for curcumin and quercetin respectively, upon loading into SNEDDS pellets. SNEDDS pellets were found stable at accelerated storage conditions. The developed formulation were able to normalize the levels of blood glucose, lipids, antioxidant biomarkers, and tissue architecture of pancreas and liver in streptozotocin induced diabetic rats as compared to their naïve forms.

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Article information: Rubiya Khursheed, Sachin Kumar Singh, Bimlesh Kumar, Sheetu Wadhwa, Monica Gulati, Anupriya, Ankit Awasthi, Sukriti Vishwas, Jaskiran Kaur, Leander Corrie, K.R. Arya, Rajan Kumar, Niraj Kumar Jha, Piyush Kumar Gupta, Flavia Zacconi, Kamal Dua, Nitin Chitranshi, Gulam Mustafa, Ankit Kumar, Self-nanoemulsifying composition containing curcumin, quercetin, Ganoderma lucidum extract powder and probiotics for effective treatment of type 2 diabetes mellitus in streptozotocin induced rats, International Journal of Pharmaceutics, 2021. https://doi.org/10.1016/j.ijpharm.2021.121306.