Background Berberine (BBR) possesses several biological activities in humans, but the poor water solubility and low oral bioavailability preclude its pharmacological use. To overcome these limitations, several formulations have been prepared including encapsulation, micro- and nano-emulsion. The aim of this study was to develop a nanoemulsion delivery system of BBR and to evaluate its membrane permeability using Caco-2 cell model. Methods Nanoemulsions containing different ratios BBR:Compritol ATO 888 (a lipid excipient) were formulated at 25 and 80 °C. The controls consisted of BBR and carboxymethylcellulose. Absorption of BBR nanoemulsions delivery systems was evaluatedin vitro by using human colon adenocarcinoma cells (Caco-2) Transwell model. The amount of permeated BBR was determined by LC-HR-MS at time zero and every 30 min for 180 min. Results Nanoemulsions significantly improved apical-to-basal transport of BBR compared to the control formulation. Kinetics of BBR uptake showed that the maximum amount absorbed was reached after 90-120 min and the percentage of BBR absorbed by Caco-2 cells increased with increasing BBR-to-Compritol ratio (1:20 > 1:10 > 1:5 > 1:1). Moreover, the formulation prepared at 80 °C showed a higher absorption rate (6-fold increment compared to control) than that developed at 25 °C (4.5-fold increment compared to control). Furthermore, demethyl-BBR was detected after 120 min of incubation as partial metabolism of berberine in the intestine. Conclusions Overall, in ourin vitro model, these new nanoemulsions seem to potentially improve the absorption of BBR. However, in vivo studies are required in order to demonstrate the bioavailability of BBR from this new formulation.

An in vitro approach to study the absorption of a new oral formulation of berberine / M. Marino, C.S. Gardana, A. Scialpi, G. Giorgini, P. Simonetti, C. Del Bo'. - In: PHARMANUTRITION. - ISSN 2213-4344. - 18(2021 Dec), pp. 100279.1-100279.7. [10.1016/j.phanu.2021.100279]

An in vitro approach to study the absorption of a new oral formulation of berberine

M. Marino
Primo
;
C.S. Gardana
Secondo
;
P. Simonetti
Penultimo
;
C. DEL BO'
Ultimo
2021-12

Abstract

Background Berberine (BBR) possesses several biological activities in humans, but the poor water solubility and low oral bioavailability preclude its pharmacological use. To overcome these limitations, several formulations have been prepared including encapsulation, micro- and nano-emulsion. The aim of this study was to develop a nanoemulsion delivery system of BBR and to evaluate its membrane permeability using Caco-2 cell model. Methods Nanoemulsions containing different ratios BBR:Compritol ATO 888 (a lipid excipient) were formulated at 25 and 80 °C. The controls consisted of BBR and carboxymethylcellulose. Absorption of BBR nanoemulsions delivery systems was evaluatedin vitro by using human colon adenocarcinoma cells (Caco-2) Transwell model. The amount of permeated BBR was determined by LC-HR-MS at time zero and every 30 min for 180 min. Results Nanoemulsions significantly improved apical-to-basal transport of BBR compared to the control formulation. Kinetics of BBR uptake showed that the maximum amount absorbed was reached after 90-120 min and the percentage of BBR absorbed by Caco-2 cells increased with increasing BBR-to-Compritol ratio (1:20 > 1:10 > 1:5 > 1:1). Moreover, the formulation prepared at 80 °C showed a higher absorption rate (6-fold increment compared to control) than that developed at 25 °C (4.5-fold increment compared to control). Furthermore, demethyl-BBR was detected after 120 min of incubation as partial metabolism of berberine in the intestine. Conclusions Overall, in ourin vitro model, these new nanoemulsions seem to potentially improve the absorption of BBR. However, in vivo studies are required in order to demonstrate the bioavailability of BBR from this new formulation.
berberine, nanoparticles, Caco-2 cells, in vitro absorption, mass spectrometry
Settore MED/49 - Scienze Tecniche Dietetiche Applicate
1-set-2021
https://www.sciencedirect.com/science/article/pii/S221343442100030X
Article (author)
File in questo prodotto:
File Dimensione Formato  
Marino et al 2021.pdf

embargo fino al 01/09/2022

Descrizione: Post-print
Tipologia: Post-print, accepted manuscript ecc. (versione accettata dall'editore)
Dimensione 2.29 MB
Formato Adobe PDF
2.29 MB Adobe PDF Visualizza/Apri
Pre-print_Manuscript by Marino et al.pdf

accesso aperto

Tipologia: Pre-print (manoscritto inviato all'editore)
Dimensione 376.53 kB
Formato Adobe PDF
376.53 kB Adobe PDF Visualizza/Apri
1-s2.0-S221343442100030X-main.pdf

accesso riservato

Tipologia: Publisher's version/PDF
Dimensione 1.85 MB
Formato Adobe PDF
1.85 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/864714
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 1
  • ???jsp.display-item.citation.isi??? 0
social impact