Effect of chitosan coating on plga nanoparticles for oral delivery of thymoquinone: In vitro, ex vivo, and cancer cell line assessments

Abstract

In the present study, thymoquinone (TQ)‐encapsulated chitosan‐ (CS)‐coated poly(d,l-lactide‐co‐glycolide) (PLGA) nanoparticles (NPs) were formulated using the emulsion evaporation method. NPs were optimized by using 33‐QbD approach for improved efficacy against breast cancer. The optimized thymoquinone loaded chitosan coated Poly (d,l‐lactide‐co‐glycolide) nanoparticles (TQ‐CS‐PLGA‐NPs) were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA‐MB‐231 and MCF‐7 cell lines. The surface coating of PLGA‐NPs was completed by CS coating and there were no significant changes in particle size and entrapment efficiency (EE) observed. The developed TQ‐CS‐PLGA‐NPs showed particle size, polydispersibility index (PDI), and %EE in the range between 126.03–196.71 nm, 0.118–0.205, and 62.75%–92.17%. The high and prolonged TQ release rate was achieved from TQ‐PLGA‐NPs and TQ‐CS‐PLGA‐NPs. The optimized TQ‐CS‐PLGA‐NPs showed significantly higher mucoadhesion and intestinal permeation compared to uncoated TQ‐PLGA‐NPs and TQ suspension. Furthermore, TQ‐CS‐PLGA‐NPs showed statistically enhanced antioxidant potential and cytotoxicity against MDA‐MB‐231 and MCF‐7 cells compared to uncoated TQ‐PLGA‐NPs and pure TQ. On the basis of the above findings, it may be stated that chitosan‐coated TQ‐PLGA‐NPs represent a great potential for breast cancer management.