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Ameliorative effect of rubiadin-loaded nanocarriers in STZ-NA-induced diabetic nephropathy in rats: formulation optimization, molecular docking, and in vivo biological evaluation

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Abstract

Diabetic nephropathy (DN) is a significant source of end-stage renal illness all over the world in both developed and developing countries. The aim of the study was to optimize rubiadin-loaded niosomes (RLN) using Box-Behnken design for the management of streptozotocin-nicotinamide (STZ-NA)-induced DN in Wistar rats. The RLN were formulated by a “thin-layer hydration technique.” The optimization of RLN was done by Box-Behnken design; the independent variables were cholesterol (CHOL), Span 80, and methanol, while the dependent factors were the vesicle size, zeta potential, and entrapment efficiency. The optimized formulation was characterized for various biochemical parameters including anti-diabetic activity in Wistar rats. The optimized RLN presented vesicle size of 238 nm, zeta potential −68 mV, and entrapment efficiency 85%. A noteworthy decreased in blood glucose level was detected in STZ-NA-induced DN rats when orally treated with RLN (100 mg/kg/week and 200 mg/kg/week). Oral administration of RLN formulation considerably decreased the levels of urea, uric acid, and creatinine in DN rats. In addition, treatment of DN rats with RLN formulation considerably improves the level of TBARS, GSH, SOD, and CAT. The lipid profile of DN rats was also improved on treatment with RLN formulation. This study revealed that the prepared RLN formulation was successfully optimized by Box-Behnken design and found to be useful for the management of STZ-NA-induced DN in Wistar rats.

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Funding

The author (Tinku) received financial support from Hamdard National Foundation (HNF), Jamia Hamdard New Delhi, India.

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Authors and Affiliations

  1. School of Pharmaceutical Education and Research, Jamia Hamdard (Deemed University), M. B. Road, New Delhi, 110062, India

    Tinku, Mohd. Mujeeb, Mohd. Aqil, Abul Kalam Najmi, Mymoona Akhtar, Apeksha Shrivastava, Abdul Qadir & Thasleem Moolakkadath

  2. Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia

    Abdul Ahad

  3. Interdisciplinary Biotechnology Unit, Aligarh Muslim University, Aligarh, 202001, India

    Waseem Ahmad Siddiqui

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  1. Tinku
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Correspondence to Mohd. Mujeeb.

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The animal study protocol was approved, and experiments were conducted as per the “Jamia Hamdard Animal Ethics Committee” (approval number 1493, dated 22-01-2019) and “CPCSEA, Government of India.”

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Tinku, Mujeeb, M., Ahad, A. et al. Ameliorative effect of rubiadin-loaded nanocarriers in STZ-NA-induced diabetic nephropathy in rats: formulation optimization, molecular docking, and in vivo biological evaluation. Drug Deliv. and Transl. Res. 12, 615–628 (2022). https://doi.org/10.1007/s13346-021-00971-0

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