Formulation and Evaluation of Mesalamine-Quercetin Loaded Self-Nano Emulsifying Drug Delivery Systems (SNEDDS) for the Management of Colon Cancer

Abstract

Colorectal cancer (CRC) is characterized by abnormal cell growth in the colon and rectum, leading to cancer. Conventional treatments have limitations, necessitating novel approaches. To formulate and evaluate a Self-Nano Emulsifying Drug Delivery System (SNEDDS) co-loaded with mesalamine (MES) and quercetin (QUE) to enhance oral bioavailability and therapeutic efficacy against CRC. MES and QUE were co-loaded into SNEDDS using Capmul MCM, Tween-80, and Transcutol-P. The formulation was optimized using a central composite design (CCD) and evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and drug loading (DL).

In-vitro studies and anti-cancer cell line studies were conducted. The optimized SNEDDS formulation exhibited a particle size of 154.4 nm, a PDI of 0.329, and a zeta potential of -17.25 mV, reflecting good stability and uniformity. The drug loading efficiency for MES and QUE was 86.38% and 79.63%, respectively. The formulation successfully passed stability tests, including heating–cooling cycles, freeze–thaw cycles, and centrifugation, with no phase separation or drug precipitation observed. Furthermore, in vitro studies demonstrated enhanced drug release compared to a physical mixture of the drugs, with the MTT assay confirming the formulation’s non-toxicity.

Additionally, a reduction in various inflammatory markers was also noted. The formulation showed 2.8-fold, 1.7-fold, and 3.4-fold reduction in TNF-α, NO, and IL-6 levels, respectively, compared to diseased group. The MES-QUE co-loaded SNEDDS formulation significantly improves the oral bioavailability and therapeutic potential of both drugs, offering a promising strategy for CRC management.

Read also our overview article on World Cancer Day here:

excipients formulation