Aim: Paclitaxel (PTX) has no clinically available oral formulations. Cetyl alcohol is metabolized by alcohol dehydrogenase and aldehyde dehydrogenase that are overexpressed in cancer cells. So, PTX-encapsulated core-shell nanoparticle of cetyl alcohol (PaxSLN) could target the cancer cells through oral route. Materials & methods: PaxSLN was synthesized using microemulsion template. Efficiency of PaxSLN was evaluated by ALDEFLUOR™, multicellular tumor spheroid formation inhibition assays and CT26 colorectal carcinoma animal model. Pharmacokinetics and biodistribution studies were done in Sprague Dawley rats. Results: PTX was encapsulated at the core of approximately 78 nm PaxSLN. PaxSLN targeted aldehyde dehydrogenase overexpressing cells. Its oral bioavailability was approximately 95% and chemotherapeutic efficacy was better than Taxol® and nab-PTX. Conclusion: A novel oral nanoformulation of PTX was developed.
Keywords: ALDEFLUOR™ assay; alcohol dehydrogenase (ADH); aldehyde dehydrogenase (ALDH); cancer stem cell; cetyl alcohol nanoparticle; core–shell nanoparticle; nanoformulation; oral anticancer drug delivery; paclitaxel; solid lipid nanoparticle.