Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro
Non-small-cell lung cancer (NSCLC) is the main cause of cancer-related deaths worldwide, with a low five-year survival rate, posing a serious threat to human health. In recent years, the delivery of antitumor drugs using a nanostructured lipid carrier (NLC) has become a subject of research. This stu...
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2023-09-01
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author | Xiaoxue Wang Jinli Liu Yufei Ma Xinyu Cui Cong Chen Guowei Zhu Yue Sun Lei Tong |
author_facet | Xiaoxue Wang Jinli Liu Yufei Ma Xinyu Cui Cong Chen Guowei Zhu Yue Sun Lei Tong |
author_sort | Xiaoxue Wang |
collection | DOAJ |
description | Non-small-cell lung cancer (NSCLC) is the main cause of cancer-related deaths worldwide, with a low five-year survival rate, posing a serious threat to human health. In recent years, the delivery of antitumor drugs using a nanostructured lipid carrier (NLC) has become a subject of research. This study aimed to develop an apigenin (AP)-loaded nanostructured lipid carrier (AP-NLC) by melt sonication using glyceryl monostearate (GMS), glyceryl triacetate, and poloxamer 188. The optimal prescription of AP-NLC was screened by central composite design response surface methodology (CCD-RSM) based on a single-factor experiment using encapsulation efficiency (EE%) and drug loading (DL%) as response values and then evaluated for its antitumor effects on NCI-H1299 cells. A series of characterization analyses of AP-NLC prepared according to the optimal prescription were carried out using transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). Subsequent screening of the lyophilization protectants revealed that mannitol could better maintain the lyophilization effect. The in vitro hemolysis assay of this formulation indicated that it may be safe for intravenous injection. Moreover, AP-NLC presented a greater ability to inhibit the proliferation, migration, and invasion of NCI-H1299 cells compared to AP. Our results suggest that AP-NLC is a safe and effective nano-delivery vehicle that may have beneficial potential in the treatment of NSCLC. |
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spelling | doaj.art-0d413b41a2d7433ba2f32833d03eb1f02023-11-19T12:10:46ZengMDPI AGMolecules1420-30492023-09-012818666810.3390/molecules28186668Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In VitroXiaoxue Wang0Jinli Liu1Yufei Ma2Xinyu Cui3Cong Chen4Guowei Zhu5Yue Sun6Lei Tong7Department of Pharmacy, Mudanjiang Medical University, Mudanjiang 157000, ChinaThe Affiliated Hongqi Hospital, Mudanjiang Medical University, Mudanjiang 157000, ChinaDepartment of Pharmacy, Mudanjiang Medical University, Mudanjiang 157000, ChinaDepartment of Public Health, Mudanjiang Medical University, Mudanjiang 157000, ChinaDepartment of Pharmacy, Mudanjiang Medical University, Mudanjiang 157000, ChinaDepartment of Pharmacy, Mudanjiang Medical University, Mudanjiang 157000, ChinaDepartment of Pharmacy, Mudanjiang Medical University, Mudanjiang 157000, ChinaDepartment of Pharmacy, Mudanjiang Medical University, Mudanjiang 157000, ChinaNon-small-cell lung cancer (NSCLC) is the main cause of cancer-related deaths worldwide, with a low five-year survival rate, posing a serious threat to human health. In recent years, the delivery of antitumor drugs using a nanostructured lipid carrier (NLC) has become a subject of research. This study aimed to develop an apigenin (AP)-loaded nanostructured lipid carrier (AP-NLC) by melt sonication using glyceryl monostearate (GMS), glyceryl triacetate, and poloxamer 188. The optimal prescription of AP-NLC was screened by central composite design response surface methodology (CCD-RSM) based on a single-factor experiment using encapsulation efficiency (EE%) and drug loading (DL%) as response values and then evaluated for its antitumor effects on NCI-H1299 cells. A series of characterization analyses of AP-NLC prepared according to the optimal prescription were carried out using transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). Subsequent screening of the lyophilization protectants revealed that mannitol could better maintain the lyophilization effect. The in vitro hemolysis assay of this formulation indicated that it may be safe for intravenous injection. Moreover, AP-NLC presented a greater ability to inhibit the proliferation, migration, and invasion of NCI-H1299 cells compared to AP. Our results suggest that AP-NLC is a safe and effective nano-delivery vehicle that may have beneficial potential in the treatment of NSCLC.https://www.mdpi.com/1420-3049/28/18/6668apigeninnanostructured lipid carrierNSCLCNCI-H1299 |
spellingShingle | Xiaoxue Wang Jinli Liu Yufei Ma Xinyu Cui Cong Chen Guowei Zhu Yue Sun Lei Tong Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro Molecules apigenin nanostructured lipid carrier NSCLC NCI-H1299 |
title | Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro |
title_full | Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro |
title_fullStr | Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro |
title_full_unstemmed | Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro |
title_short | Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro |
title_sort | development of a nanostructured lipid carrier based drug delivery strategy for apigenin experimental design based on ccd rsm and evaluation against nsclc in vitro |
topic | apigenin nanostructured lipid carrier NSCLC NCI-H1299 |
url | https://www.mdpi.com/1420-3049/28/18/6668 |
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