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Published on:May 2020
Indian Journal of Pharmaceutical Education and Research, 2020; 54(2s):s79-s87
Original Article | doi:10.5530/ijper.54.2s.64

2,4-Dichlorophenoxy Acetic Acid as an Antidiabetic Drug: In silico, Preformulation and in vivo Approaches

Authors and affiliation (s):

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.


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.

Key words: 2,4-D, Micronized, Pioglitazone, Repositioning, Streptozotocin.



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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.


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