Polyphenolic compounds such as curcumin and quercetin are naturally occurring antioxidants that inhibit free radicals, reduce superoxide anions and peroxides, and inhibit low-density lipoprotein oxidation and lipid peroxidation. Preliminary studies have shown that these compounds can be used to treat and prevent chronic conditions such as cancer and type II diabetes, but their activities are limited due to their poor solubilities resulting in low oral bioavailability. This makes it difficult for either compound to reach active sites outside of the gastrointestinal tract. While it is difficult to increase the solubility of either drug on its own, it is increasingly more difficult to simultaneously increase the solubility of both compounds. However, once achieved, the combined formulation will provide the additive and/or synergistic advantages associated with their respective activities. Novel lipid (compritol, squalene and cataplex) formulations of curcumin-quercetin and their combinations using various excipients such as polyethylene glycol (PEG-400) and surfactants (Polysorbate 80 and Poloxamer 188) were prepared. Formulations were prepared using high sheer homogenization and ultrasonication technique respectively. Lipid formulations were characterized by particle size and zeta potential and UV-spectroscopic methodology was used for the simultaneous detection of curcumin and quercetin in the developed lipid formulations. Long term stability of these formulation will be evaluated for three weeks by storing at 4°C and at 25 °C. Further, the in vitro release of curcumin and quercetin will be carried out with Slide-A-Lyzer Dialysis Cassettes and skin penetration studies will be conducted using Franz diffusion cell. Overall, curcumin-quercetin loaded lipid nanoparticles were successfully formulated with average lipid nanoparticle size of 200-300 nm. Preliminary results have shown increased solubility and long-term stability of the polyphenolic compounds. These formulations will be further utilized for <i>in vitro</i> and <i>in vivo</i> testing against melanoma cell line.

Development, characterization, and stability evaluation: Lipid-based formulations of polyphenol combinations

ACS Spring 2022

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