DUAL ANTICANCER DRUG LOADED METHOXY POLY (ETHYLENE GLYCOL)-POLY (ε-CAPROLACTONE) BLOCK COPOLYMERIC MICELLES AS NOVEL DRUG CARRIERS
Objective: Curcumine (CUR) and rapamycin (RAPA) are two potent hydrophobic anticancer drugs. The clinical and preclinical applications of anticancer formulations are limited due to use of toxic excipients and poor bioavailability. In the present study, an approach has been made to develop CUR and RAPA loaded MePEG/PCL di-block copolymeric micelles keeping in the view to make excipient free formulation with slow release of drugs.
Methods: The CUR and RAPA loaded MePEG/PCL di-block copolymeric micelles were prepared. Physico-chemical characters like size, surface charge and encapsulation efficiency were measured. The in vitro release studies was carried out in pH 7.4 to evaluate the sustained release properties of micelles.
Results: MePEG/PCL di-block copolymeric micelles were efficiently encapsulate both the drugs, i. e. CUR (~ 64 %) and RAPA (~ 94 %) in the core and have loading capacity of ~ 12 % (CUR) and ~ 29 % (RAPA). The zetasizer measurement shows that particles have size range 128 nm to 176 nm with a negative zeta potential. SEM and AFM studies reveled that micelles have smooth exterior surface. The XRD and DSC studies explain that the drugs are uniformly distributed in the polymer matrix. The dual drug loaded micelles have sustained in vitro drug release activity as estimated in phosphate buffer (pH 7.4).
Conclusion: These MePEG/PCL di-block copolymeric micelles are capable of carrying both the hydrophobic anticancer drugs and the encouraging results suggest further studies to evaluate the bioavailability parameters as well as suitability of the formulation.
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