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Abstract
The usefulness of Docetaxel (DT) as an anti-cancer agent is limited to parenteral route owing to its very poor oral bioavailability. Thus, to improve its oral efficacy, DT was loaded in novel cationic lipid nanocapsules (DT CLNC). The DT CLNC possessed size of 130–150 nm, zeta potential of +72mV, adequate DT loading and over 95% encapsulation efficiency. TEM revealed capsular structure of DT CLNC. Lipolysis study indicated improved solubilization of DT by nanocapsules in comparison to DT solution. DT CLNC exhibited significantly higher release of DT in comparison to DT solution during in vitro permeation studies employing non-reverted rat-intestinal sac. Superior uptake of DT in zebra fishes exposed to DT CLNC resulted in greater apoptosis-based cell death as compared to those exposed to DT solution. This correlated well with the significantly superior (p < 0.05) anti-angiogenic activity of DT CLNC system over DT solution, in zebra fish model. DT CLNC also inhibited tumor growth in melanoma cell line induced tumors in C57BL/6 mice significantly, as compared to DT solution (p < 0.05). The DT CLNC system demonstrated adequate stability, with tremendous potential to improve oral efficacy of DT and can serve as an alternative to existing DT formulations available commercially for parenteral use.
Acknowledgements
Authors thank Mac-Chem Products (India) Pvt. Ltd., for providing gift samples of Docetaxel. and Gattefosse India Pvt. Ltd. and BASF Pvt. Ltd. for providing gift samples of various excipients used in this research project. Authors thank Lipoid GmBH, Germany for gift samples of lecithin.
Declaration of interest
The authors report no declarations of interest. Ankitkumar S. Jain is thankful to UGC (University Grants Commission, New Delhi, India) and AMRF (Amrut Mody Research Foundation, Mumbai, India) for financial assistance. Sanket M. Shah is thankful to ICMR (Indian Council of Medical Research, New Delhi, India) for fellowship and financial support to research. Dinesh T. Makhija and Peeyush N. Goel are thankful for fellowship provided by AMRF and CSIR (Council of Scientific and Industrial Research, New Delhi, India) respectively. No writing assistance was utilized in the production of this manuscript.