Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats
Diabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic me...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2022-12-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2022.2110997 |
| _version_ | 1811215160306565120 |
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| author | Mohammed H. Elkomy Hussein M. Eid Mohammed Elmowafy Khaled Shalaby Ameeduzzafar Zafar Mohamed A. Abdelgawad Mostafa E. Rateb Mohammed R.A. Ali Izzeddin Alsalahat Heba A. Abou-Taleb |
| author_facet | Mohammed H. Elkomy Hussein M. Eid Mohammed Elmowafy Khaled Shalaby Ameeduzzafar Zafar Mohamed A. Abdelgawad Mostafa E. Rateb Mohammed R.A. Ali Izzeddin Alsalahat Heba A. Abou-Taleb |
| author_sort | Mohammed H. Elkomy |
| collection | DOAJ |
| description | Diabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic medication. The BER-BLS was fabricated using a thin-film hydration strategy and optimized using a central composite design (face-centered). The average vesicle size, entrapment efficiency, and surface charge of the optimized BER-BLS preparation were 196.5 nm, 89.7%, (−) 36.4 mV, respectively. In addition, it exhibited higher stability and better-sustained release of berberine than the berberine solution (BER-SOL). BER-BLS and BER-SOL were administered to streptozocin-induced diabetic rats. The optimized BER-BLS formulation had a significant hypoglycemic impact, with a maximum blood glucose decrease of 41%, whereas BER-SOL only reduced blood glucose by 19%. Furthermore, the pharmacological effect of oral BER-BLS and BER-SOL corresponded to 99.3% and 31.7%, respectively, when compared to subcutaneous insulin (1 IU). A pharmacokinetic analysis found a 6.4-fold rise in the relative bioavailability of berberine in BER-BLS when compared to BER-SOL at a dosage of 100 mg/kg body weight. Histopathological investigation revealed that BER-BLS is suitable for oral administration. Our data demonstrate that BLS is a potential nanocarrier for berberine administration, enhancing its oral bioavailability and antidiabetic activity. |
| first_indexed | 2024-04-12T06:17:02Z |
| format | Article |
| id | doaj.art-5b91575a0920404994b717c00dbbd534 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-12T06:17:02Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-5b91575a0920404994b717c00dbbd5342022-12-22T03:44:26ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642022-12-012912694270410.1080/10717544.2022.2110997Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic ratsMohammed H. Elkomy0Hussein M. Eid1Mohammed Elmowafy2Khaled Shalaby3Ameeduzzafar Zafar4Mohamed A. Abdelgawad5Mostafa E. Rateb6Mohammed R.A. Ali7Izzeddin Alsalahat8Heba A. Abou-Taleb9Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaSchool of Computing, Engineering & Physical Sciences, University of the West of Scotland, Paisley, UKDepartment of Pharmacology and Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptUK Dementia Research Institute Cardiff, School of Medicine, Cardiff University, Cardiff, UKDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Merit University (MUE), Sohag, EgyptDiabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic medication. The BER-BLS was fabricated using a thin-film hydration strategy and optimized using a central composite design (face-centered). The average vesicle size, entrapment efficiency, and surface charge of the optimized BER-BLS preparation were 196.5 nm, 89.7%, (−) 36.4 mV, respectively. In addition, it exhibited higher stability and better-sustained release of berberine than the berberine solution (BER-SOL). BER-BLS and BER-SOL were administered to streptozocin-induced diabetic rats. The optimized BER-BLS formulation had a significant hypoglycemic impact, with a maximum blood glucose decrease of 41%, whereas BER-SOL only reduced blood glucose by 19%. Furthermore, the pharmacological effect of oral BER-BLS and BER-SOL corresponded to 99.3% and 31.7%, respectively, when compared to subcutaneous insulin (1 IU). A pharmacokinetic analysis found a 6.4-fold rise in the relative bioavailability of berberine in BER-BLS when compared to BER-SOL at a dosage of 100 mg/kg body weight. Histopathological investigation revealed that BER-BLS is suitable for oral administration. Our data demonstrate that BLS is a potential nanocarrier for berberine administration, enhancing its oral bioavailability and antidiabetic activity.https://www.tandfonline.com/doi/10.1080/10717544.2022.2110997Berberinediabetes mellitusbilosomesbioavailabilitypharmacokineticsbile salts |
| spellingShingle | Mohammed H. Elkomy Hussein M. Eid Mohammed Elmowafy Khaled Shalaby Ameeduzzafar Zafar Mohamed A. Abdelgawad Mostafa E. Rateb Mohammed R.A. Ali Izzeddin Alsalahat Heba A. Abou-Taleb Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats Drug Delivery Berberine diabetes mellitus bilosomes bioavailability pharmacokinetics bile salts |
| title | Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats |
| title_full | Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats |
| title_fullStr | Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats |
| title_full_unstemmed | Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats |
| title_short | Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats |
| title_sort | bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats |
| topic | Berberine diabetes mellitus bilosomes bioavailability pharmacokinetics bile salts |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2022.2110997 |
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