A cytotoxic medication with an excellent mechanism of action against cancer cells is paclitaxel. When given as an infusion, it revealed severe dose-limiting toxicity. A proper delivery method is widely desired to combat these negative effects. When used with pharmaceuticals, bioenhancers increase and promote their bioavailability while lowering the risk of adverse drug reactions and the incidence of drug resistance. Therefore, nanoparticles are chosen as a delivery mechanism in this investigation based on the literature review. The goal of this research was to include herbal bioenhancer and paclitaxel into a nanoparticle technology. In that study, the nanoparticles were created using the Eudragit RLPO1 polymer and the emulsion solvent evaporation process. The produced nanoparticles underwent testing for drug entrapment, in vitro drug release, zeta potential, and particle size. Additionally, the pharmacokinetic profile and mean transit time (MTT) assay on a lung cancer cell line were used to evaluate the nanoparticles for an in vitro cell cytotoxicity research. The bioenhancer-loaded nanoparticles exhibit better in-vitro performance with a particle size range of 124 to 200 nm. In a 24-hour period, every formulation that was released contained between 82.71 and 95.47% of the medication. The drug's release kinetics followed Fick's law of diffusion and were best described by Higuchi's model. Every batch of nanoparticles demonstrated a good drug entrapment capacity between 57.51 and 86.12%. Although the pure medication solution did not entirely stop cells from proliferating, nanoparticle formulations considerably slowed it down in the MTT assay. Unexpectedly, the FNP 6 formulation had a stronger antiproliferative effect on A549 cells than formulations with lower bioenhancer loading. The plasma level of FNP-6 in the in vivo pharmacokinetic assay was higher than that of any other formulation, including control. FNP-6 had an absolute bioavailability of 7.89 and an AUC of 6.423 g/mL. The fact that FNP-5 and FNP-6 included more bioenhancer than the other formulations could be the cause of their higher absolute bioavailability. It follows that the proliferative effect and bioavailability of an anticancer medication can be improved by the inclusion of a bioenhancer.