Article · Volume 54, Issue 2S · pp. s79–s87
2,4-Dichlorophenoxy Acetic Acid as an Antidiabetic Drug: In silico, Preformulation and in vivo Approaches
Tamer Mohamed Shehata1,2, Mohammed Abdou Khedr1,3, Maged Elsayed Mohamed1,4
- 1College of Clinical Pharmacy, King Faisal University, Al-Ahsa, KINGDOM OF SAUDI ARABIA.
- 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, University of Zagazig, Zagazig, EGYPT.
- 3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ein Helwan, Cairo, EGYPT.
- 4Department of Pharmacognosy, Faculty of Pharmacy, University of Zagazig, Zagazig, EGYPT.
Abstract
Background: 2,4-Dichlorophenoxy acetic acid (2,4-D) was recently rediscovered as new anti-inflammatory agent through an in silico molecular modeling and in vivo anti-inflammatory inspection. Further computational investigations showed very close similarity between 2,4-D and pioglitazone in the mode of binding to PPARγ ligand binding pocket, suggesting an antidiabetic activity.Aim: To evaluate the binding strength of 2,4-D to PPARγ binding pocket and to improve the low water solubility of 2,4-D in formulation.Methods: particle size reduction via Nano Spray Dryer B-90 was chosen as possible technique to enhance the drug solubility and in turn facilitating its formulation. Chemical and physical properties of both raw and micronized forms of 2,4-D were investigated utilizing FTIR and DSC respectively. Additionally, dissolution profiles in different dissolution media were evaluated. Finally, the antidiabetic activity of micronized 2,4-D was investigated using streptozotocin (STZ)-induced animal model.Results: Revealed enhanced dissolution profiles for the micronized form of the drug on all media under investigation compared to its raw form. The in vivo antidiabetic activity for micronized 2,4-D form indicated no significant difference in its blood sugar lowering activity compared to pioglitazone as reference drug.Conclusion: the previous results could suggest micronized 2,4-D as a cheap antidiabetic agent with similar activity to pioglitazone.
Keywords: 2; 4-D; Micronized; Pioglitazone; Repositioning; Streptozotocin
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