Abstract
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.
Highlights
Licensee MDPI, Basel, Switzerland.Celecoxib (CXB) is a selective inhibitor of the COX-2 enzyme and it is and has been approved by the Food and Drug Administration (FDA) for the treatment of the symptoms of osteoarthritis and rheumatoid arthritis [1,2,3]
The particle sizes of all solid lipid nanoparticles (SLN) formulations were in the submicron range, with the highest value 757 nm ± 24.13 for F8 and the smallest value 192.6 nm ± 3.3 for F2
The incorporation of CXB into SLN formulations was optimized using a variety of lipids and surfactants to achieve optimal formulations with superior properties such as high EE, low nanosize, and a uniform release profile suitable for colon delivery
Summary
Celecoxib (CXB) is a selective inhibitor of the COX-2 enzyme and it is and has been approved by the Food and Drug Administration (FDA) for the treatment of the symptoms of osteoarthritis and rheumatoid arthritis [1,2,3]. CXB has been shown to have significant chemo-preventive activity in colon carcinogenesis and breast cancer [1,2,3]. COX-2 expression in cancer cells has been demonstrated in a number of animal models [4]. A number of studies have shown that CXB, either alone or in combination with cetuximab, published maps and institutional affil-.
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