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Using Caco-2 Cells to Study Lipid Transport by the Intestine
Published on: August 20, 2015
Rhamnolipids enhance epithelial permeability in Caco-2 monolayers
Lifang Jiang1, Xuwei Long, Qin Meng
1Department of Chemical Engineering and Biochemical Engineering, Zhejiang University, Zhejiang 310027, PR China.
International Journal of Pharmaceutics
|February 14, 2013
Summary
Rhamnolipids significantly enhance oral drug absorption by increasing intestinal permeability and inhibiting P-glycoprotein (P-gp) efflux. These natural compounds show promise as safe and effective permeation enhancers for drug delivery.
Area of Science:
- Pharmacology
- Drug Delivery
- Biochemistry
Background:
- Oral drug delivery faces challenges with low bioavailability due to poor absorption.
- Permeation enhancers can improve drug absorption, but safety and efficacy vary.
- Rhamnolipids are biosurfactants with potential pharmaceutical applications.
Purpose of the Study:
- To evaluate rhamnolipids as permeation enhancers for oral drug delivery.
- To assess the impact of rhamnolipids on paracellular and transcellular transport pathways.
- To investigate rhamnolipids' effect on P-glycoprotein (P-gp) activity and their safety profile.
Main Methods:
- Utilized Caco-2 cell monolayers as an in vitro model of the human small intestinal epithelium.
- Measured apparent permeability (Papp) of model drugs (phenol red, propranolol) with and without rhamnolipids.
- Assessed P-glycoprotein (P-gp) inhibition using rhodamine 123 (R123) efflux assays.
- Evaluated rhamnolipid safety through cell viability and hemolysis assays.
Main Results:
- Rhamnolipids significantly increased paracellular transport of phenol red (7-8 fold) and transcellular transport of propranolol (2 fold) in a concentration-dependent manner.
- Rhamnolipids effectively inhibited P-glycoprotein (P-gp) efflux of rhodamine 123 (R123), comparable to Tween-80.
- Cell viability and hemolysis assays confirmed the safety of rhamnolipids at effective concentrations.
Conclusions:
- Rhamnolipids are potent enhancers of both paracellular and transcellular drug transport pathways.
- Rhamnolipids demonstrate significant P-gp inhibitory activity, further aiding drug absorption.
- Rhamnolipids represent a safe and highly effective option for enhancing oral drug bioavailability.
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