Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats.
Berberine
bile salts
bilosomes
bioavailability
diabetes mellitus
optimization
pharmacokinetics
Journal
Drug delivery
ISSN: 1521-0464
Titre abrégé: Drug Deliv
Pays: England
ID NLM: 9417471
Informations de publication
Date de publication:
Dec 2022
Dec 2022
Historique:
entrez:
17
8
2022
pubmed:
18
8
2022
medline:
19
8
2022
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 35975320
doi: 10.1080/10717544.2022.2110997
pmc: PMC9387316
doi:
Substances chimiques
Blood Glucose
0
Hypoglycemic Agents
0
Berberine
0I8Y3P32UF
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2694-2704Références
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