Self-Assembling Dioscorea bulbifera loaded mixed micelles: Formulation optimization, in-vitro cytotoxicity and in-vivo pharmacokinetics

Dioscorea bulbifera (DB)is one among the traditionally used medicinal plant which has been reported to have anticancer property and capable of inducing apoptosis of tumors, but the poor water solubility restricts its pharmacological application. The study aims at improving the aqueous solubility of Dioscorea bulbifera and enhancing the bioavailability by formulating Pluronic F-127 and Soluplus® incorporated polymeric mixed micelles (PL–SO–MMs).

Micelles were prepared by thin film dispersion method, using 32 factorial design-response surface methodology with Particle size (nm) and entrapment efficiency (EE%)as indicators. Transmission electron microscopy (TEM)images revealed that prepared Mixed Micelles were nano-spherical and having average particle size of 61.45 ± 0.4 nm and zeta potential in range of −18.11 ± 1.2 mV to −21.70 ± 0.9 mV and with acritical micelle concentration (CMC) of 0.821 ± 0.002 % w/v.

The cell toxicity assays of DB loaded Polymeric mixed micelles was performed on MCF7 and MDAMB-231 showed higher cell toxicity compared with free DB.The IC50 values of DB and DB loaded PL–SO–MMs on MCF7 and MDAMB-231 were 8.92μg/ml,12μg/ml and 3.07 μg/ml, 8.1 μg/ml respectively. In conclusion, the Mixed Micelles (PL–SO–MMs) developed in the present study were proven as promising drug delivery system for Dioscorea bulbifera.

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Article information: Sagar Trivedi, Shubhangi Thool, Kamlesh Wadher, Mangesh Bhalekar, Priyanka Bire, Self-Assembling Dioscorea bulbifera loaded mixed micelles: Formulation optimization, in-vitro cytotoxicity and in-vivo pharmacokinetics, Journal of Drug Delivery Science and Technology, Volume 65, 2021. https://doi.org/10.1016/j.jddst.2021.102722.

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