Human serum albumin nanoparticulate system with encapsulation of gefitinib for enhanced anti-tumor effects in non-small cell lung cancer

Pang, Xiaoying; Yang, Peng; Wang, Liuchang; Jing-xu, Cao; Cheng, Yunlong; Sheng, Dongyu; Xu, Wenrong; Guo, Qin; Qian, Kan; Zhang, Qizhi; Jiang, Xinguo

doi:10.1016/j.jddst.2019.06.011

Cited by 18 publications

(4 citation statements)

References 42 publications

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“… 50 Likewise, Pang et al found that albumin nanoparticles loaded with GEF increase the early and late apoptosis of NCI–H358 cell line when compared with pure GEF. 51 In alignment with the proposed hypothesis, Wang et al developed SLN consisting of stearic acid as a lipid phase for the treatment of lung cancer. The biodistribution study showed that higher drug concentration was detected in lung tissue.…”

Section: Discussionmentioning

confidence: 94%

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: 94%

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 results revealed that the GEF-loaded formulation was able to increase the apoptotic cells population of A549 when compared with pure GEF [22]. In addition, Pang et al developed GEFloaded albumin nanoparticles which it was able to induce apoptosis in treated cells when compared with pure GEF [39]. Furthermore, Wang et al prepared SLN consisting of SA for the treatment of lung cancer.…”

Section: Apoptotic Studymentioning

confidence: 99%

Engineered Nanoscale Lipid-Based Formulation as Potential Enhancer of Gefitinib Lymphatic Delivery: Cytotoxicity and Apoptotic Studies Against the A549 Cell Line

et al. 2022

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The present study aimed to engineer a nanoscale lipid-based lymphatic drug delivery system with D-α-Tocopherol polyethylene glycol 1000 succinate to combat the lymphatic metastasis of lung cancer. The nanoscale lipid-based systems including GEF-SLN, GEF-NLC, and GEF-LE were prepared and pharmaceutically characterized. In addition, the most stable formulation (GEF-NLC) was subjected to an in vitro release study. Afterward, the optimized GEF-NLC was engineered with TPGS (GEF-TPGS-NLC) and subjected to in vitro cytotoxicity, and apoptotic studies using the A549 cells line as a surrogate model for lung cancer. The present results revealed that particle size and polydispersity index of freshly prepared formulations were ranging from 198 to 280 nm and 0.106 to 0.240, respectively, with negative zeta potential ranging from − 14 to − 27.6.mV. An in vitro release study showed that sustained drug release was attained from GEF-NLC containing a high concentration of lipid. In addition, GEF-NLC and GEF-TPGS-NLC showed remarkable entrapment efficiency above 89% and exhibited sustained release profiles. Cytotoxicity showed that IC 50 of pure GEF was 11.15 μg/ml which decreased to 7.05 μg/ml for GEF-TPGS-NLC. The apoptotic study revealed that GEF-TPGS-NLC significantly decreased the number of living cells from 67 to 58% when compared with pure GEF. The present results revealed that the nanoscale and lipid composition of the fabricated SLN, NLC, and LE could mediate the lymphatic uptake of GEF to combat the lymphatic tumor metastasis. Particularly, GEF-TPGS-NLC is a promising LDDS to increase the therapeutic outcomes of GEF during the treatment of metastatic lung cancer.

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“…Proteins are natural biomacromolecules and the good biocompatibility and nanosize allow them a good candidate for drug delivery. − Human and bovine serum albumins represent the two widely used protein carriers owing to the good water solubility and strong binding effect with small molecules like EGFR-TKIs. − A binding study revealed the high affinity of Erlo to bovine serum albumin with an equilibrium constant of 4.25 × 10 –9 at 25 °C . Inspired by the high binding efficiency of Lapa to albumin and α1-acidglycoprotein, Gao et al constructed a core–shell NP based on BSA and egg yolk lecithin to improve the solubility and antiglioma effect, where the water solubility was significantly increased from 0.007 mg/mL to more than 10 mg/mL and a better antitumor effect than Tykerb even at a lower dose (10 mg/kg vs 100 mg/kg) .…”

Section: Ddss For Enhanced Egfr-tki Deliverymentioning

confidence: 99%

Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy

Pan

et al. 2023

Mol. Pharmaceutics

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Epidermal growth factor receptor (EGFR) plays a key role in signal transduction pathways associated with cell proliferation, growth, and survival. Its overexpression and aberrant activation in malignancy correlate with poor prognosis and short survival. Targeting inhibition of EGFR by small-molecular tyrosine kinase inhibitors (TKIs) is emerging as an important treatment model besides of chemotherapy, greatly reshaping the landscape of cancer therapy. However, they are still challenged by the offtargeted toxicity, relatively limited cancer types, and drug resistance after long-term therapy. In this review, we summarize the recent progress of oral, pulmonary, and injectable drug delivery systems for enhanced and targeting TKI delivery to tumors and reduced side effects. Importantly, EGFR-TKI-based combination therapies not only greatly broaden the applicable cancer types of EGFR-TKI but also significantly improve the anticancer effect. The mechanisms of TKI resistance are summarized, and current strategies to overcome TKI resistance as well as the application of TKI in reversing chemotherapy resistance are discussed. Finally, we provide a perspective on the future research of EGFR-TKI-based cancer therapy.

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Human serum albumin nanoparticulate system with encapsulation of gefitinib for enhanced anti-tumor effects in non-small cell lung cancer

Cited by 18 publications

References 42 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

Engineered Nanoscale Lipid-Based Formulation as Potential Enhancer of Gefitinib Lymphatic Delivery: Cytotoxicity and Apoptotic Studies Against the A549 Cell Line

Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy

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