Enhanced oral delivery of hesperidin-loaded sulfobutylether-β-cyclodextrin/chitosan nanoparticles for augmenting its hypoglycemic activity : in vitro-in vivo assessment study

© 2023. The Author(s)..

Hesperidin (Hsd), a bioactive phytomedicine, experienced an antidiabetic activity versus both Type 1 and Type 2 Diabetes mellitus. However, its intrinsic poor solubility and bioavailability is a key challenging obstacle reflecting its oral delivery. From such perspective, the purpose of the current study was to prepare and evaluate Hsd-loaded sulfobutylether-β-cyclodextrin/chitosan nanoparticles (Hsd/CD/CS NPs) for improving the hypoglycemic activity of the orally administered Hsd. Hsd was first complexed with sulfobutylether-β-cyclodextrin (SBE-β-CD) and the complex (CX) was found to be formed with percent complexation efficiency and percent process efficiency of 50.53 ± 1.46 and 84.52 ± 3.16%, respectively. Also, solid state characterization of the complex ensured the inclusion of Hsd inside the cavity of SBE-β-CD. Then, Hsd/CD/CS NPs were prepared using the ionic gelation technique. The prepared NPs were fully characterized to select the most promising one (F1) with a homogenous particle size of 455.7 ± 9.04 nm, a positive zeta potential of + 32.28 ± 1.12 mV, and an entrapment efficiency of 77.46 ± 0.39%. The optimal formula (F1) was subjected to further investigation of in vitro release, ex vivo intestinal permeation, stability, cytotoxicity, and in vivo hypoglycemic activity. The results of the release and permeation studies of F1 manifested a modulated pattern between Hsd and CX. The preferential stability of F1 was observed at 4 ± 1 °C. Also, the biocompatibility of F1 with oral epithelial cell line (OEC) was retained up to a concentration of 100 µg/mL. After oral administration of F1, a noteworthy synergistic hypoglycemic effect was recorded with decreased blood glucose level until the end of the experiment. In conclusion, Hsd/CD/CS NPs could be regarded as a hopeful oral delivery system of Hsd with enhanced antidiabetic activity.

Medienart:

E-Artikel

Erscheinungsjahr:

2024

Erschienen:

2024

Enthalten in:

Zur Gesamtaufnahme - volume:14

Enthalten in:

Drug delivery and translational research - 14(2024), 4 vom: 01. März, Seite 895-917

Sprache:

Englisch

Beteiligte Personen:

Elmoghayer, Mona Ebrahim [VerfasserIn]
Saleh, Noha Mohamed [VerfasserIn]
Abu Hashim, Irhan Ibrahim [VerfasserIn]

Links:

Volltext

Themen:

2PP9364507
9012-76-4
Beta-Cyclodextrins
Chitosan
Drug Carriers
E750O06Y6O
Hesperidin
Hypoglycemic
Hypoglycemic Agents
Journal Article
Nanoparticles
Permeation
Release
SBE4-beta-cyclodextrin
Sulfobutylether-β-cyclodextrin

Anmerkungen:

Date Completed 12.03.2024

Date Revised 14.03.2024

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1007/s13346-023-01440-6

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM363365400