Preparation and Evaluation of PEGylated and Folate‐PEGylated Liposomes Containing Paclitaxel for Lymphatic Delivery

Abstract

This study attempted to prepare polyethylene‐glycol modified (PEGylated) and folate‐PEGylated liposomes containing paclitaxel (Ptx) in order to reduce the toxicity and improve the bioavailability and biocompatibility by targeting drugs to the lymphatics using cancer cell specific ligand folate to prevent metastasis via the lymphatic system. Liposomes were prepared by lipid film hydration method using PEG and folate‐PEG as surface modifiers. The mean particle size and encapsulation efficiency of liposomes were 114 ± 6.81 nm and 81 ± 2.3% for PEGylated liposome and 122 ± 4.87 nm and 88 ± 2.0% for folate‐PEGylated liposome, respectively. According to stability test, it could be confirmed that PEGylated and folate‐PEGylated liposomes were stable for at least 5 days. After intravenous administration of the PEGylated and folate‐PEGylated liposomes to rats, the CL t (total clearance) and t 1/2 (half‐life) were significantly different ( P < 0.05) compared with those of PADEXOL Inj. In targeting efficiency, calculated as the concentration ratio of Ptx in lymph nodes and plasma, there was significant increase in targeting efficiency at lymph nodes ( P < 0.05). From these results, we could conclude that the prepared Ptx‐containing PEGylated and folate‐PEGylated liposomes are good candidates for the targeted delivery of the drug to lymphatic system.