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Article

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

1
Zoology Department, Faculty of Science, Minia University, Minia 61519, Egypt
2
Colloids & Advanced Materials Group, Chemistry Department, Faculty of Science, Minia University, Minia 61519, Egypt
3
Department of Chemistry, School of Sciences and Humanities, Nazarbayev University, Nursultan 010000, Kazakhstan
*
Author to whom correspondence should be addressed.
Academic Editor: Vanessa Andrés-Guerrero
Pharmaceutics 2021, 13(7), 1048; https://doi.org/10.3390/pharmaceutics13071048
Received: 22 May 2021 / Revised: 6 July 2021 / Accepted: 7 July 2021 / Published: 9 July 2021
(This article belongs to the Special Issue Innovative Polymers for Controlled Drug Delivery)
We developed a dual microencapsulation platform for the type 2 diabetes drug metformin (MTF), which is aimed to increase its bioavailability. We report the use of Lycopodium clavatum sporopollenin (LCS), derived from their natural spores, and raw Phoenix dactylifera L. (date palm) pollens (DPP) for MTF microencapsulation. MTF was loaded into LCS and DPP via a vacuum and a novel method of hydration-induced swelling. The loading capacity (LC) and encapsulation efficiency (EE) percentages for MTF-loaded LCS and MTF-loaded DPP microcapsules were 14.9% ± 0.7, 29.8 ± 0.8, and 15.2% ± 0.7, 30.3 ± 1.0, respectively. The release of MTF from MTF-loaded LCS microcapsules was additionally controlled by re-encapsulating the loaded microcapsules into calcium alginate (ALG) microbeads via ionotropic gelation, where the release of MTF was found to be significantly slower and pH-dependent. The pharmacokinetic parameters, obtained from the in vivo study, revealed that the relative bioavailability of the MTF-loaded LCS-ALG beads was 1.215 times higher compared to pure MTF, following oral administration of a single dose equivalent to 25 mg/kg body weight MTF to streptozotocin (STZ)-induced diabetic male Sprague-Dawley rats. Significant hypoglycemic effect was obtained for STZ-induced diabetic rats orally treated with MTF-loaded LCS-ALG beads compared to control diabetic rats. Over a period of 29 days, the STZ-induced diabetic rats treated with MTF-loaded LCS-ALG beads showed a decrease in the aspartate aminotransferase (AST), alanine aminotransferase (ALT), triglycerides, cholesterol, and low-density lipoprotein-cholesterol (LDL-C) levels, as well as an increase in glutathione peroxidase (GPx) and a recovery in the oxidative stress biomarker, lipid peroxidation (LPx). In addition, histopathological studies of liver, pancreas, kidney, and testes suggested that MTF-loaded LCS-ALG beads improved the degenerative changes in organs of diabetic rats. The LCS-ALG platform for dual encapsulation of MTF achieved sustained MTF delivery and enhancement of bioavailability, as well as the improved biochemical and histopathological characteristics in in vivo studies, opening many other intriguing applications in sustained drug delivery. View Full-Text
Keywords: metformin; antidiabetic; plant spores; sporopollenin; alginate; beads; biochemical parameters; histopathology metformin; antidiabetic; plant spores; sporopollenin; alginate; beads; biochemical parameters; histopathology
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MDPI and ACS Style

Meligi, N.M.; Dyab, A.K.F.; Paunov, V.N. Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules. Pharmaceutics 2021, 13, 1048. https://doi.org/10.3390/pharmaceutics13071048

AMA Style

Meligi NM, Dyab AKF, Paunov VN. Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules. Pharmaceutics. 2021; 13(7):1048. https://doi.org/10.3390/pharmaceutics13071048

Chicago/Turabian Style

Meligi, Noha M., Amro K.F. Dyab, and Vesselin N. Paunov. 2021. "Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules" Pharmaceutics 13, no. 7: 1048. https://doi.org/10.3390/pharmaceutics13071048

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