Assessment of ex-vivo intestinal permeability and lymphatic uptake of curcumin and piperine-loaded nanostructured lipid carriers

Abstract

Curcumin (CUR) is a naturally occurring compound in food known for its potential pharmacological activity but faces challenges due to its high metabolism. Piperine (PIP) is an effective inhibitor of metabolizing enzymes, enhancing the bioavailability of CUR. This work evaluated the lymphatic absorption and ex-vivo intestinal permeability of nanostructured lipid carriers (NLCs) containing PIP and CUR (CP NLCs). The optimized lipid formulation underwent in-vitrodrug release, ex-vivo permeation, and lymphatic uptake studies utilizing chicken intestinal (jejunum) segments. Studies were conducted under different conditions, specifically in the presence and absence of the lymphatic uptake blocker Pluronic-F68 (PF68). PF68 is a non-ionic surfactant commonly used in pharmaceutical research, and it's known for its ability to inhibit lymphatic uptake. In-vitro drug release profiles indicated the controlled release of CUR and PIP from NLCs over 24 h. The ex-vivo permeability study demonstrated that CP NLCs exhibited higher permeation compared to CUR and PIP Suspension (CP Suspension). Studies on the lymphatic uptake of CP NLCs, conducted with and without the presence of the lymphatic uptake blocker PF68, demonstrated a decrease in drug permeation. However, in the absence of the lymphatic blocker, drug transport via the lymphatic path increased significantly by 4.07-fold for CUR and 6.56-fold for PIP. This means that the NLCs significantly enhanced the lymphatic transport of both CUR and PIP. The results imply that the lipid-based NLC system shows potential as a drug delivery method, improving solubility, and aiding in the lymphatic transport of both CUR and PIP.

Keywords

• Curcumin
• Piperine
• Nanostructured Lipid Carriers
• Lymphatic Uptake
• payer’s patches