Related Experiment Video
Updated: Feb 25, 2026

Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
In vivo fate of lipid-silybin conjugate nanoparticles: Implications on enhanced oral bioavailability
Yuhua Ma1, Haisheng He2, Fei Xia2
1Key Laboratory of Smart Drug Delivery of MOE and PLA, School of Pharmacy, Fudan University, Shanghai, China; Key Laboratory for Tibet Plateau Phytochemistry of Qinghai Province, School of Pharmacy, Qinghai Nationalities University, Xining, China.
Abstract:
Lipid-drug conjugates (LDCs) of a poorly soluble and poorly permeable drug silybin (SB) and lipids with different chain lengths (6C, 12C, 18C) are synthesized and formulated into solid lipid nanoparticles (SLNs). The in vivo fate of LDCs as well as SLNs is investigated by tracking either SB or LDCs or SLNs. LDCs are prone to be hydrolyzed by lipases either in simulated gastrointestinal media or in Caco-2 cell lines in a lipid chain length-dependent mode. The oral bioavailability of SB is enhanced by 5-7-fold in comparison with a fast-release formulation. No integral LDCs are detected in plasma confirms the readily degradable nature of LDCs. The absorption of LDCs by enteric epithelia and subsequent transportation into circulation might play a leading role in absorption enhancement, whereas the contribution of then M-cell pathway is not as remarkable. A shorter lipid chain favors earlier lipolysis and faster absorption along the intestine-to-circulation path.
Related Concept Videos
Modified-Release Drug Delivery Systems: Bioavailability
Bioavailability Enhancement: Drug Permeability Enhancement
Bioavailability Enhancement: Drug Solubility Enhancement
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
Bioavailability: Overview
Bioavailability: Overview

