Simultaneous delivery of paclitaxel and erlotinib from dual drug loaded PLGA nanoparticles: Formulation development, thorough optimization and in vitro release

Abstract The current approach involves the development of dual drug loaded nanoparticles of Paclitaxel (Pac) and Erlotinib (Erl) with subsequent thorough optimization in order to achieve sustained and simultaneous delivery of Pac and Erl. The formulation is developed to produce maximum efficacy with least side effects. The dual loaded paclitaxel and erlotinib nanoparticles (PE-NPs) were prepared by modified single emulsion method with appropriate optimization. The formulation was optimized for size, polydispersity index (PDI), zeta potential, surface morphology, encapsulation efficiency and loading capacity. The XRD and DSC results of a physical mixture and PE-NPs together confirmed that there was not any physical or chemical interaction among the drugs and polymer (PLGA). Further, the XRD and DSC analyses revealed that the crystalline forms of both drugs in PE-NPs were changed into amorphous form. The optimized PE-NPs were observed to have the particle size of 145.5 ± 3.2 nm, zeta potential of −9.3 ± 1.4 mV and PDI of 0.135 which indicated the particles to be of uniform size with optimum stability. The entrapment efficiency of paclitaxel was found to be 90.36% and that of erlotinib was found to be 62.23% from PE-NPs. PE-NPs further showed the sustained release of drugs from the particles with total release of 65.25% for paclitaxel and 74.83% for erlotinib in 120 h. Accelerated and intermediate stability studies also indicated that there was a minimal variation in size and entrapment efficiency of PE-NPs.