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

PLGA-Based Nanoparticles in Cancer Treatment

“…The NPs offer a platform to co-encapsulate various pairs of drugs with varying hydrophobicity and pharmacokinetic profiles ensuring simultaneous long term distribution to the target site. Such NP co-formulations can extend the drugs’ circulation time ( Tian et al, 2017 ), sustain drug release ( Khuroo et al, 2018 ) and also inhibit development of drug resistance ( Misra and Sahoo, 2011 ) as well as increase drug accumulation in tumors ( Afrooz et al, 2017 ). Among the many combinations co-loaded in one particle are PTX-Cisplatin ( Tian et al, 2017 ), PTX-Erlotinib ( Khuroo et al, 2018 ), DOX-CUR ( Misra and Sahoo, 2011 ), PTX-Verapamil ( Afrooz et al, 2017 ), and PTX-epigallocatechin gallate (EGCG).…”

A chemotherapeutic approach targeting the acidic tumor microenvironment: combination of a proton pump inhibitor and paclitaxel for statistically optimized nanotherapeutics

“…The kinetics of PTX and LAN release from the optimized nanoformulation were determined by tting the obtained data to various kinetic models, [35][36][37][38][39][40] including the zero order release model (eqn (4)), rst order release model (eqn (5)), Higuchi model (eqn (6)) and Korsmeyer-Peppas model (eqn (7)): 21,31…”

“…This may be due to the release of drugs adhered to the surface of the NPs. 21 Steady and controlled release of the drugs occurred by diffusion of the drugs from the polymeric core of the NPs due to the gradual disintegration of the polymeric matrix via the thin layers of liquid surrounding the particles. 60 Due to the presence of free carboxyl groups, acid-terminated PLGA (PLGA 50 : 50) provided more swelling due to water uptake compared to the more hydrophobic ester-terminated PLGA.…”

“…34 The erupted release may be due to the large surface-to-volume ratio of the NPs. 21 According to the literature, PLGA (50 : 50) has a long degradation period of 102 days. 62 The in vitro release kinetics of both drugs were studied by tting the cumulative release data in various models, including the zero order kinetic model (% cumulative drug release vs. time plot); the rst order kinetic model (log % cumulative release vs. time); the Higuchi model (% cumulative release vs. square root of time); and the Korsmeyer-Peppas model (log % cumulative release vs. log time).…”

“…20 In contrast with APIs administered separately, when drugs are combined in a single nanocarrier system, the exposure of each drug in the body can be controlled more precisely, which may translate into synergistic action. 21 Hence, the main goal of this work was to develop a statistically optimized polymeric nano drug delivery system that combines PTX with LAN. The nanocarrier system addressed the major physicochemical hindrances of the drugs, such as the poor water solubility of PTX and the instability of LAN in heat, light and acidic media.…”