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Biomed Res Int. 2022 Jan 10;2022:3549061. doi: 10.1155/2022/3549061. eCollection 2022.
Plumbagin, a bioactive naphthoquinone, has demonstrated potent antitumor potential. However, plumbagin is a poorly water-soluble compound; therefore, clinical translation requires and will be facilitated by the development of a new pharmaceutical formulation. We generated an oil-in-water nanoemulsion formulation of plumbagin using a low-energy spontaneous emulsification process with propylene glycol caprylate (Capryol 90) as the oil phase and Labrasol/Kolliphor RH40 as surfactant and co-surfactant excipients. Formulation studies using Capryol 90/Labrasol/Kolliphor RH40 components, based on pseudoternary diagram and analysis of particle size distribution and polydispersity determined by dynamic light scattering (DLS), identified an optimized composition of excipients for the formulation of nanoparticles. The nanoemulsion loaded with plumbagin as an active pharmaceutical ingredient had an average hydrodynamic diameter of 30.9 nm with a narrow polydispersity. The nanoemulsion exhibited long-term stability, as well as good particle size retention in simulated physiological environments. Additionally, the plumbagin-loaded nanoemulsion showed increased cytotoxicity against PTEN-P2 prostate cancer cells compared to free drug. In conclusion, we generated a plumbagin formulation with high loading capacity, robust stability and scalable production. The new Capryol 90-based plumbagin nanoemulsion formulation demonstrated antiproliferative activity against prostate cancer cells, thus warranting further pharmaceutical development.
PMID:35047632 | PMC:PMC8763502 | DOI: 10.1155/2022/3549061