Celecoxib-Loaded Solid Lipid Nanoparticles for Colon Delivery: Formulation Optimization and In Vitro Assessment of Anti-Cancer Activity

This work aimed to optimize a celecoxib (CXB)-loaded solid lipid nanoparticles (SLN) colon delivery system for the enhancement of anticancer activity. An ultrasonic melt-emulsification method was employed in this work for the preparation of SLN. The physical attributes were characterized for their particle sizes, charges, morphology, and entrapment efficiency (%EE), in addition to DSC and FTIR. The in vitro drug release profiles were evaluated, and the anticancer activity was examined utilizing an MTT assay in three cancer cell lines: the colon cancer HT29, medulloblastoma Daoy, and hepatocellular carcinoma HepG2 cells. All of the prepared SLN formulations had nanoscale particle sizes ranging from 238 nm to 757 nm. High zeta-potential values (mv) within −30 s mv were reported. The %EE was in the range 86.76–96.6%. The amorphous nature of the SLN-entrapped CXB was confirmed from SLN DSC thermograms. The in vitro release profile revealed a slow constant rate of release with no burst release, which is unusual for SLN. Both the F9 and F14 demonstrated almost complete CXB release within 24 h, with only 25% completed within the first 5 h. F9 caused a significant percentage of cell death in the three cancer cell lines tested after 24 h of incubation and maintained this effect for 72 h. The prepared CXB-loaded SLN exhibited unique properties such as slow release with no burst and a high %EE. The anticancer activity of one formulation was extremely significant in all tested cancer cell lines at all incubation times, which is very promising.

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Materials

Celecoxib (CXB) was purchased from FDC Limited, Maharashtra, India. Softisan 154, Dynasan 114, Imwitor 308 were purchased from Sasol Germany GmbH (Witten, Germany). Tween 80, Sodium deoxycholate, stearic acid and MTT (3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide) were obtained from Sigma–Aldrich Chemical Company (St. Louis, MO, USA). DMEM/high glucose, DMEM/F12, fetal bovine serum (FBS), penicillin/streptomycin, L-glutamine, non-essential amino acids and HEPES reagent were purchased from Gibco, Invitrogen (Eugene, OR, USA). Additionally, 96-well plates, T-25 and T-75 flasks, as well as serological pipettes and pipette tips were obtained from TPP Techno Plastic Products AG (Trasadingen, Switzerland). Cremophor EL was purchased from BASF, Ludwigshafen, Germany. All other chemicals were of analytical grade.

Alajami, H.N.; Fouad, E.A.; Ashour, A.E.; Kumar, A.; Yassin, A.E.B. Celecoxib-Loaded Solid Lipid Nanoparticles for Colon Delivery: Formulation Optimization and In Vitro Assessment of Anti-Cancer Activity. Pharmaceutics 2022, 14, 131. https://doi.org/10.3390/pharmaceutics14010131