Glycyrrhetinic Acid-Poly(ethylene glycol)-glycyrrhetinic Acid Tri-Block Conjugates Based Self-Assembled Micelles for Hepatic Targeted Delivery of Poorly Water Soluble Drug

The triblock 18 β ‐glycyrrhetinic acid‐poly(ethylene glycol)‐18 β ‐glycyrrhetinic acid conjugates (GA‐PEG‐GA) based self‐assembled micelles were synthesized and characterized by FTIR, NMR, transmission electron microscopy, and particle size analysis. The GA‐PEG‐GA conjugates having the critical micelle concentration of 6 × 10 −5 M were used to form nanosized micelles, with mean diameters of 159.21 ± 2.2 nm, and then paclitaxel (PTX) was incorporated into GA‐PEG‐GA micelles by self‐assembly method. The physicochemical properties of the PTX loaded GA‐PEG‐GA micelles were evaluated including in vitro cellular uptake, cytotoxicity, drug release profile, and in vivo tissue distribution. The results demonstrate that the GA‐PEG‐GA micelles had low cytotoxicity and good ability of selectively delivering drug to hepatic cells in vitro and in vivo by the targeting moiety glycyrrhetinic acid. In conclusion, the GA‐PEG‐GA conjugates have potential medical applications for targeted delivery of poor soluble drug delivery.