Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats
Background/Aim: Gliclazide is one of the most commonly prescribed oral anti-hyperglycaemic therapies in type 2 diabetes mellitus (T2D). Recently reported additional beneficial pharmacological properties of gliclazide, including immunomodulatory and anticoagulant activities, suggested its potential a...
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| Format: | Article |
| Language: | English |
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Medical Society of the Republic of Srpska, Banja Luka, University of Banja Luka. Faculty of Medicine
2020-01-01
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| Series: | Scripta Medica |
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| Online Access: | https://scindeks-clanci.ceon.rs/data/pdf/2490-3329/2020/2490-33292001015J.pdf |
| _version_ | 1818656795804041216 |
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| author | Jović Jelena Milijašević Boris Vukmirović Saša Vasović Velibor Mikov Momir Mooranian Armin Al-Salami Hani Golocorbin-Kon Svetlana |
| author_facet | Jović Jelena Milijašević Boris Vukmirović Saša Vasović Velibor Mikov Momir Mooranian Armin Al-Salami Hani Golocorbin-Kon Svetlana |
| author_sort | Jović Jelena |
| collection | DOAJ |
| description | Background/Aim: Gliclazide is one of the most commonly prescribed oral anti-hyperglycaemic therapies in type 2 diabetes mellitus (T2D). Recently reported additional beneficial pharmacological properties of gliclazide, including immunomodulatory and anticoagulant activities, suggested its potential application in treatment of type 1 diabetes mellitus (T1D). However, following oral administration, gliclazide was shown to have poor and variable absorption directing research into development of novel pharmaceutical delivery systems of gliclazide suitable for T1D. Since bile acids have previously demonstrated stabilising and controlled-release effects on microcapsules, their use for preparation of microcapsules of gliclazide may lead to improvements in gliclazide release, absorption and antidiabetic effects. This investigation was aimed to evaluate drug absorption profiles and hypoglycaemic effects of alginate-based microcapsules of gliclazide, prepared together with or without cholic acid, in healthy rats. Methods: Thirty healthy Wistar rats with confirmed normal glucose blood concentration were allocated into five groups and administered with a single dose of either vehicle microcapsules, gliclazide in suspension, gliclazide microcapsules, gliclazide in suspension together with cholic acid or microencapsulated gliclazide in combination with cholic acid. Following respective gliclazide dose, blood was sampled over next 10 hours and blood glucose levels and gliclazide serum concentrations were measured. Results: This analysis demonstrated altered effects of different gliclazide formulations in healthy rats with the highest gliclazide absorption mirrored by the most profound hypoglycaemic effect being achieved after its oral administration as a suspension (p <0.01) compared to any other investigated pharmaceutical formulation. Concusion: When conducting pharmacokinetic characterisation of novel pharmaceutical formulations of antidiabetic drugs, it is of utmost importance to select the appropriate research model and consider the possible role of gut-metabolic activation on their hypoglycaemic effects. |
| first_indexed | 2024-12-17T03:31:16Z |
| format | Article |
| id | doaj.art-4b13049ff9ad45f7912c81092b242fa1 |
| institution | Directory Open Access Journal |
| issn | 2490-3329 2303-7954 |
| language | English |
| last_indexed | 2024-12-17T03:31:16Z |
| publishDate | 2020-01-01 |
| publisher | Medical Society of the Republic of Srpska, Banja Luka, University of Banja Luka. Faculty of Medicine |
| record_format | Article |
| series | Scripta Medica |
| spelling | doaj.art-4b13049ff9ad45f7912c81092b242fa12022-12-21T22:05:16ZengMedical Society of the Republic of Srpska, Banja Luka, University of Banja Luka. Faculty of MedicineScripta Medica2490-33292303-79542020-01-0151115202490-33292001015JPharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in ratsJović Jelena0Milijašević Boris1Vukmirović Saša2Vasović Velibor3Mikov Momir4https://orcid.org/0000-0002-2804-0624Mooranian Armin5Al-Salami Hani6Golocorbin-Kon Svetlana7https://orcid.org/0000-0002-2850-6375University of Novi Sad, Faculty of Medicine, Department of Pharmacology and Toxicology, SerbiaUniversity of Novi Sad, Faculty of Medicine, Department of Pharmacology and Toxicology, SerbiaUniversity of Novi Sad, Faculty of Medicine, Department of Pharmacology and Toxicology, SerbiaUniversity of Novi Sad, Faculty of Medicine, Department of Pharmacology and Toxicology, SerbiaUniversity of Novi Sad, Faculty of Medicine, Department of Pharmacology and Toxicology, SerbiaCurtin University, Curtin Health Innovation Research Institute, School of Pharmacy and Biomedical Sciences, Biotechnology and Drug Development Research Laboratory, Perth, AustraliaCurtin University, Curtin Health Innovation Research Institute, School of Pharmacy and Biomedical Sciences, Biotechnology and Drug Development Research Laboratory, Perth, AustraliaUniversity of Novi Sad, Faculty of Medicine, Department of Pharmacy, SerbiaBackground/Aim: Gliclazide is one of the most commonly prescribed oral anti-hyperglycaemic therapies in type 2 diabetes mellitus (T2D). Recently reported additional beneficial pharmacological properties of gliclazide, including immunomodulatory and anticoagulant activities, suggested its potential application in treatment of type 1 diabetes mellitus (T1D). However, following oral administration, gliclazide was shown to have poor and variable absorption directing research into development of novel pharmaceutical delivery systems of gliclazide suitable for T1D. Since bile acids have previously demonstrated stabilising and controlled-release effects on microcapsules, their use for preparation of microcapsules of gliclazide may lead to improvements in gliclazide release, absorption and antidiabetic effects. This investigation was aimed to evaluate drug absorption profiles and hypoglycaemic effects of alginate-based microcapsules of gliclazide, prepared together with or without cholic acid, in healthy rats. Methods: Thirty healthy Wistar rats with confirmed normal glucose blood concentration were allocated into five groups and administered with a single dose of either vehicle microcapsules, gliclazide in suspension, gliclazide microcapsules, gliclazide in suspension together with cholic acid or microencapsulated gliclazide in combination with cholic acid. Following respective gliclazide dose, blood was sampled over next 10 hours and blood glucose levels and gliclazide serum concentrations were measured. Results: This analysis demonstrated altered effects of different gliclazide formulations in healthy rats with the highest gliclazide absorption mirrored by the most profound hypoglycaemic effect being achieved after its oral administration as a suspension (p <0.01) compared to any other investigated pharmaceutical formulation. Concusion: When conducting pharmacokinetic characterisation of novel pharmaceutical formulations of antidiabetic drugs, it is of utmost importance to select the appropriate research model and consider the possible role of gut-metabolic activation on their hypoglycaemic effects.https://scindeks-clanci.ceon.rs/data/pdf/2490-3329/2020/2490-33292001015J.pdfgliclazidecapsulesbile acidshypoglycaemic agentsrats |
| spellingShingle | Jović Jelena Milijašević Boris Vukmirović Saša Vasović Velibor Mikov Momir Mooranian Armin Al-Salami Hani Golocorbin-Kon Svetlana Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats Scripta Medica gliclazide capsules bile acids hypoglycaemic agents rats |
| title | Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats |
| title_full | Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats |
| title_fullStr | Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats |
| title_full_unstemmed | Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats |
| title_short | Pharmacokinetic and drug absorption profiles of the anti-hyperglycaemic agent gliclazide in oral tissue-targeted microcapsules in rats |
| title_sort | pharmacokinetic and drug absorption profiles of the anti hyperglycaemic agent gliclazide in oral tissue targeted microcapsules in rats |
| topic | gliclazide capsules bile acids hypoglycaemic agents rats |
| url | https://scindeks-clanci.ceon.rs/data/pdf/2490-3329/2020/2490-33292001015J.pdf |
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