Next Article in Journal
Description of a Naphthoquinonic Crystal Produced by the Fungus Scytalidium cuboideum
Previous Article in Journal
Effect of Heat Stress on Yield, Monoterpene Content and Antibacterial Activity of Essential Oils of Mentha x piperita var. Mitcham and Mentha arvensis var. piperascens
Open AccessArticle

Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model

Nanotechnology Research Center, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Golestan Ave, Ahvaz 67123, Iran
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(8), 1904; https://doi.org/10.3390/molecules23081904
Received: 17 May 2018 / Revised: 6 June 2018 / Accepted: 7 June 2018 / Published: 31 July 2018
The low oral bioavailability of ciprofloxacin is associated with two distinct challenges: its low aqueous solubility and efflux by p-glycoproteins (P-gp) in the intestinal membrane. Several studies were conducted in order to improve its solubility and permeability through the gastrointestinal membrane. In this study, in a full factorial design study, eight polymeric micelles were prepared and their characteristics, including particle size, loading and release rate were evaluated. Polymeric micelles demonstrated particle sizes below 190 nm and 27–88% loading efficiency. Drug release was affected by drug solubility, polymeric micelle erosion and swelling in simulated gastrointestinal fluids. An optimized polymeric micelle was prepared based on appropriate characteristics such as high drug loading and low particle size; and was used for a permeation study on Caco-2 cells. Optimized polymeric micelles with and without ginsenoside and ginsenoside alone enhanced drug permeability through Caco-2 cells significantly in the absorptive direction. The effect of ginsenoside was dose dependent and the maximum effect was seen in 0.23 mg/mL concentration. Results showed that P-gp may not be responsible for ciprofloxacin secretion into the gut. The main mechanism of ciprofloxacin transport through Caco-2 cells in both directions is active diffusion and P-gp has inhibitory effects on ciprofloxacin permeability in the absorptive direction that was blocked by ginsenoside and micelles without ginsenoside. View Full-Text
Keywords: ciprofloxacin; ginsenoside; P-glycoprotein; gastrointestinal drug transporter; polymeric micelles ciprofloxacin; ginsenoside; P-glycoprotein; gastrointestinal drug transporter; polymeric micelles
Show Figures

Graphical abstract

MDPI and ACS Style

Sharif Makhmal Zadeh, B.; Esfahani, G.; Salimi, A. Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model. Molecules 2018, 23, 1904.

AMA Style

Sharif Makhmal Zadeh B, Esfahani G, Salimi A. Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model. Molecules. 2018; 23(8):1904.

Chicago/Turabian Style

Sharif Makhmal Zadeh, Behzad; Esfahani, Golbarg; Salimi, Anayatollah. 2018. "Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model" Molecules 23, no. 8: 1904.

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop