Design and Development of Solid Self-Microemulsifying Drug Delivery of Gefitinib

Dhairyasheel, Ghadge; Yadav, Adhikrao Vyankatrao; Varsha, Gharge

doi:10.5958/2231-5713.2018.00031.4

Cited by 8 publications

(4 citation statements)

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“…It was found that GEF exhibited the highest solubility in oleic acid (LC-FA) when compared with olive and castor oil (LC-triglycerides. 28 In contrast, Nayek et al found that GEF exhibited much higher solubility in phospholipid (LC-DG) than GMS (LC-MG), while LC-FA was not involved in the study. This could be attributed to the use of different solubility evaluation methods.…”

Section: Discussionmentioning

confidence: 84%

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

Sherif¹,

Harisa²,

Alanazi³

et al. 2022

IJN

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Purpose The present study aimed to develop gefitinib-loaded solid lipid nanoparticles (GEF-SLN), and GEF-loaded PEGylated SLN (GEF-P-SLN) for targeting metastatic lung cancer through the lymphatic system. Methods The prepared SLNs were characterized in terms of physicochemical properties, entrapment efficiency, and in-vitro release. Furthermore, ex-vivo permeability was investigated using the rabbit intestine. Cytotoxicity and apoptotic effects were studied against A549 cell lines as a model for lung cancer. Results The present results revealed that the particle size and polydispersity index of the prepared formulations range from 114 to 310 nm and 0.066 to 0.350, respectively, with negative zeta-potential (−14 to −27.6). Additionally, SLN and P-SLN showed remarkable entrapment efficiency above 89% and exhibited sustained-release profiles. The permeability study showed that GEF-SLN and GEF-P-SLN enhanced the permeability of GEF by 1.71 and 2.64-fold, respectively, compared with GEF suspension. Cytotoxicity showed that IC 50 of pure GEF was 3.5 μg/mL, which decreased to 1.95 and 1.8 μg/mL for GEF-SLN and GEF-P-SLN, respectively. Finally, the apoptotic study revealed that GEF-P-SLN decreased the number of living cells from 49.47 to 3.43 when compared with pure GEF. Conclusion These results concluded that GEF-P-SLN is a promising approach to improving the therapeutic outcomes of GEF in the treatment of metastatic lung cancer.

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Section: Discussionmentioning

confidence: 84%

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

Sherif¹,

Harisa²,

Alanazi³

et al. 2022

IJN

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“…The obtained results were in alignment with the findings shown by Dhairyasheel et al, who reported that GEF solubility depends on the type of liquid oils. Maximum GEF solubility was detected in LCFA, while it was minimum in the case of LCT [ 18 ]. Likewise, Shahba et al studied the solubility of a weakly basic drug in SNEDDS formulations.…”

Section: Resultsmentioning

confidence: 99%

Optimization of Gefitinib-Loaded Nanostructured Lipid Carrier as a Biomedical Tool in the Treatment of Metastatic Lung Cancer

et al. 2023

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Gefitinib (GEF) is utilized in clinical settings for the treatment of metastatic lung cancer. However, premature drug release from nanoparticles in vivo increases the exposure of systemic organs to GEF. Herein, nanostructured lipid carriers (NLC) were utilized not only to avoid premature drug release but also due to their inherent lymphatic tropism. Therefore, the present study aimed to develop a GEF-NLC as a lymphatic drug delivery system with low drug release. Design of experiments was utilized to develop a stable GEF-NLC as a lymphatic drug delivery system for the treatment of metastatic lung cancer. The in vitro drug release of GEF from the prepared GEF-NLC formulations was studied to select the optimum formulation. MTT assay was utilized to study the cytotoxic activity of GEF-NLC compared to free GEF. The optimized GEF-NLC formulation showed favorable physicochemical properties: <300 nm PS, <0.2 PDI, <−20 ZP values with >90% entrapment efficiency. Interestingly, the prepared formulation was able to retain GEF with only ≈57% drug release within 24 h. Furthermore, GEF-NLC reduced the sudden exposure of cultured cells to GEF and produced the required cytotoxic effect after 48 and 72 h incubation time. Consequently, optimized formulation offers a promising approach to improve GEF’s therapeutic outcomes with reduced systemic toxicity in treating metastatic lung cancer.

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“…These drugs are monoclonal antibodies like cetuximab and nimotuzumab, and tyrosine kinase inhibitors (TKIs) like erlotinib, gefitinib, and afatinib. 44 45 …”

Section: Drugs Targeting the Epidermal Growth Factor Receptormentioning

confidence: 99%

“…These drugs are monoclonal antibodies like cetuximab and nimotuzumab, and tyrosine kinase inhibitors (TKIs) like erlotinib, gefitinib, and afatinib. 44,45 The monoclonal antibodies act by binding to the extracellular domain of the EGFR that inhibits the link between ligands and results in the inhibition of signal transmission into the cell. Cetuximab is an immunoglobulin G1 (IgG1) monoclonal antibody that is used as first-line treatment, in association with radiotherapy, for advanced head and neck squamous cell carcinoma.…”

Section: Drugs Targeting the Epidermal Growth Factor Receptormentioning

confidence: 99%

Role of Molecular Targeted Therapeutic Drugs in Treatment of Oral Squamous Cell Carcinoma: Development and Current Strategies—A Review Article

Singh

Patel

2022

Glob Med Genet

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Because of active advancement in the field of biomedicine, people have in-depth knowledge of biological nature of malignant tumors and are able to recognized the overexpression of different molecules such as vascular endothelial growth factor receptor, cyclin-dependent kinase, and programmed cell death receptor. Presently, various targeted therapeutic drugs are used in different clinical trials in those patients suffering from oral squamous cell carcinoma. In this review, we converse about the various targeted therapeutic drugs and their advancement in the treatment of oral squamous cell carcinoma. This review scrutinizes the existing documentation in the literature related to the targeted therapies for oral squamous cell carcinoma. English language articles were searched in various databases such as PubMed, Scopus, Science Direct, and Google Scholar. The keywords used for searching are “oral squamous cell carcinoma,” “targeted therapy,” and “therapeutic drugs.”

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Design and Development of Solid Self-Microemulsifying Drug Delivery of Gefitinib

Cited by 8 publications

References 0 publications

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

Optimization of Gefitinib-Loaded Nanostructured Lipid Carrier as a Biomedical Tool in the Treatment of Metastatic Lung Cancer

Role of Molecular Targeted Therapeutic Drugs in Treatment of Oral Squamous Cell Carcinoma: Development and Current Strategies—A Review Article

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