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Article

Optimization of Thiolated Chitosan Nanoparticles for the Enhancement of in Vivo Hypoglycemic Efficacy of Sitagliptin in Streptozotocin-Induced Diabetic Rats

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Department of Pharmacy Practice, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia
2
Department of Pharmaceutics, C.L.Baid Metha College of Pharmacy, Chennai 600097, India
3
Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia
4
Department of Pharmaceutics, Faculty of Pharmacy, Sinai University, Alarish, North Sinai 45511, Egypt
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(4), 300; https://doi.org/10.3390/pharmaceutics12040300
Received: 5 March 2020 / Revised: 19 March 2020 / Accepted: 20 March 2020 / Published: 26 March 2020
(This article belongs to the Special Issue Chitosan Nanoparticles in Drug Delivery)
Sitagliptin (SGN) is an antidiabetic drug used for treatment of diabetes mellitus type II. The objectives of this study were to formulate SGN in form of thiolated chitosan (TC) nanoparticles to enhance the mucoadhesion properties of SGN to the gastrointestinal tract, prolong drug release, decrease side effects, and enhance patient compliance. Seventeen batches of SGN-TC nanoparticles were designed by Box-Behnken design and prepared using the ionic gelation method using tripolyphosphate (TPP) as crosslinking agent. The prepared formulations were evaluated for particle size, entrapment efficiency %, and in vitro drug release. Based on the results of optimization, three formulations (F1–F3) were prepared with different drug polymer ratios (1:1, 1:2, and 1:3). The mucoadhesion study and in vivo hypoglycemic activity of three formulations were evaluated in comparison to free SGN in streptozotocin (STZ)-induced diabetic rats. The seventeen SGN-TC nanoparticles showed small particle sizes, high entrapment efficiency, and prolonged drug release. The concentration of TC polymers had highest effect on these responses. The percentage of SGN–TC nanoparticles adhered to tissue was increased and the release was prolonged as the concentration of TC polymer increased (F3 > F2 > F1). The hypoglycemic effect of SGN-TC nanoparticles was significantly higher than resulted by free SGN. It was concluded that TC nanoparticles had the ability to enhance the mucoadhesion properties of SGN and prolong the drug release. SGN-TC nanoparticles significantly reduced plasma glucose levels compared to free SGN in STZ-induced diabetic rats. View Full-Text
Keywords: Sitagliptin; thiolated chitosan (TC); ionic gelation; hypoglycemic activity; Box-Behnken design; mucoadhesion study Sitagliptin; thiolated chitosan (TC); ionic gelation; hypoglycemic activity; Box-Behnken design; mucoadhesion study
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MDPI and ACS Style

Prabahar, K.; Udhumansha, U.; Qushawy, M. Optimization of Thiolated Chitosan Nanoparticles for the Enhancement of in Vivo Hypoglycemic Efficacy of Sitagliptin in Streptozotocin-Induced Diabetic Rats. Pharmaceutics 2020, 12, 300. https://doi.org/10.3390/pharmaceutics12040300

AMA Style

Prabahar K, Udhumansha U, Qushawy M. Optimization of Thiolated Chitosan Nanoparticles for the Enhancement of in Vivo Hypoglycemic Efficacy of Sitagliptin in Streptozotocin-Induced Diabetic Rats. Pharmaceutics. 2020; 12(4):300. https://doi.org/10.3390/pharmaceutics12040300

Chicago/Turabian Style

Prabahar, Kousalya, Ubaidulla Udhumansha, and Mona Qushawy. 2020. "Optimization of Thiolated Chitosan Nanoparticles for the Enhancement of in Vivo Hypoglycemic Efficacy of Sitagliptin in Streptozotocin-Induced Diabetic Rats" Pharmaceutics 12, no. 4: 300. https://doi.org/10.3390/pharmaceutics12040300

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