article · Pharmaceutics
Gefitinib is an oral anti-cancer drug used for advanced or metastatic non-small cell lung, colon, and breast cancers, but poor solubility and low oral bioavailability limit its clinical utility. To address these limitations, Gefitinib was incorporated into cubosomal nanoparticles using an emulsification technique, optimized through factorial design and response surface methodology. The resulting semi-cubic nanoparticles demonstrated high drug entrapment efficiency, small vesicle size, high zeta potential, and sustained release profiles. Testing in animal models demonstrated significant reductions in key colon cancer biomarkers, specifically carcinoembryonic antigen and carbohydrate antigen 19-9, alongside decreased gene expression of tissue inhibitors of metalloproteinases-1 and matrix metalloproteinases-7. Furthermore, histopathological examination confirmed improved colon tissue condition and a notable reduction in focal infiltration within the lamina propria following treatment.
Oral chemotherapy can be hindered when active drugs fail to dissolve properly in the body, preventing therapeutic amounts from reaching tumours. By packaging gefitinib inside lipid cubosomes, this formulation improves drug absorption and delivers targeted anti-tumour action directly against colon cancer markers, potentially offering a more effective oral therapy for patients managing advanced cancer.
This technology offers an oral drug delivery platform for pharmaceutical companies developing enhanced formulations of poorly soluble oncology therapies. The evidence shows successful formulation, characterisation, and preclinical in vivo testing in tissue models. Consequently, the development remains at an early, preclinical stage, requiring formal toxicology assessments, pharmacokinetics, and clinical trials before it can be considered for real-world pharmaceutical manufacture and clinical use.
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Gefitinib (GFT) is a tyrosine kinase inhibitor drug used as a first-line treatment for patients with advanced or metastatic non-small cell lung, colon, and breast cancer. GFT exhibits low solubility and hence low oral bioavailability, which restricts its clinical application. One of the most important trends in overcoming such problems is the use of a vesicular system. Cubosomes are considered one of the most important vesicular systems used to improve solubility and oral bioavailability. In this study, GFT cubosomal nanoparticles (GFT-CNPs) were prepared by the emulsification method. The selected formulation variables were analyzed and optimized by full factorial design and response surface methodology. Drug entrapment efficiency (EE%), transmission electron microscopy, particle size, polydispersity index, in vitro release and its kinetics, and the effect of storage studies were estimated. The chosen GFT-CNPs were subjected to further investigations as gene expression levels of tissue inhibitors of metalloproteinases-1 (TIMP-1) and matrix metalloproteinases-7 (MMP-7), colon biomarkers, and histopathological examination of colon tissues. The prepared GFT-CNPs were semi-cubic in shape, with high EE%, smaller vesicle size, and higher zeta potential values. The in vivo data showed a significant decrease in the serum level of embryonic antigen (CEA), carbohydrate antigen 19-9 (CA 19-9), and gene expression level of TIMP-1 and MMP-7. Histopathological examination showed enhancement in cancer tissue and highly decreased focal infiltration in the lamina propria after treatment with GFT-CNPs.
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DOI: 10.3390/pharmaceutics15020680
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