Synthesis, Characterization, and In Vivo Distribution of 99m Tc Radiolabelled Docetaxel Loaded Folic Acid-Thiolated Chitosan Enveloped Liposomes

The physico-chemical properties of drug loaded nanoparticles (NPs) are important determinants for in vivo distribution, serum stability, and drug delivery efficiency. Liposomal NPs are most widely used due to their bicompability nature and drug carrier efficiency. In this study, 99m Tc-labelled docetaxel (DTX) loaded folic acid-thiolated chitosan enveloped liposomal nanoparticles were synthesized and assessed for its localization, stability, and drug release in animal model. Folic acid grafted with thiolated chitosan was cross-linked with docetaxel and coated in liposomes (FTD-Lip). The radiolabelling efficiency of 99m Tc-FTD-Lip was 98.8% with 97.2% serum stability. The in vivo distribution of 99m Tc-FTD-Lip given by oral route showed that complex was localized in the buccal cavity, gastric fundus, and distal esophagus, with 20.2% DTX released after 5 h, while by intravenous route administration, the radio-complex was localized in the lungs and liver and 29.2% DTX release was observed after 5 h. 99m TcFTD-Lip can be used for site specific localization and comparative study indicates that intravenous drug release is higher than oral route while oral route shows steady drug release. Graphical Abstract The docetaxel grafted with chitosan and TGA were encapsulated in liposome that was further labelled with 99m Tc. The in vivo distribution in rabbits acquired by gamma camera showed localized of complex in gastric fundus in case of oral rout administration while by intravenous administration complex was localized in lungs and liver. Slow release of docetaxel inside the body was also observed.