Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex

<b>Background</b>: Rosmarinic acid (ROS) has gained notable attention for its anticancer potential; however, its limited aqueous solubility hinders its effective delivery and application in pharmaceutical formulations. <b>Methods</b>: To overcome this limitation, an inclusion...

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Main Authors: Yuan Li, Muhammad Inam, Muhammad Waqqas Hasan, Kaixin Chen, Zhongqian Zhang, Yongcheng Zhu, Jiayu Huang, Zhuowen Wu, Wenjie Chen, Min Li
Format: Article
Language:English
Published: MDPI AG 2024-11-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/16/11/1408
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author Yuan Li
Muhammad Inam
Muhammad Waqqas Hasan
Kaixin Chen
Zhongqian Zhang
Yongcheng Zhu
Jiayu Huang
Zhuowen Wu
Wenjie Chen
Min Li
author_facet Yuan Li
Muhammad Inam
Muhammad Waqqas Hasan
Kaixin Chen
Zhongqian Zhang
Yongcheng Zhu
Jiayu Huang
Zhuowen Wu
Wenjie Chen
Min Li
author_sort Yuan Li
collection DOAJ
description <b>Background</b>: Rosmarinic acid (ROS) has gained notable attention for its anticancer potential; however, its limited aqueous solubility hinders its effective delivery and application in pharmaceutical formulations. <b>Methods</b>: To overcome this limitation, an inclusion complex of ROS with β-cyclodextrin (β-CD) was prepared using the recrystallization method. The resultant ROS–β-CD complex was comprehensively characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). <b>Results:</b> The ROS–β-CD complex showed a significant improvement in the solubility and dissolution profile of ROS, underscoring its potential for enhanced bioavailability and therapeutic efficacy in pharmaceutical applications. In vitro assays were performed to assess the effects on cell viability, proliferation, apoptotic pathways, and 3D spheroid tumor models. <b>Conclusions:</b> The results demonstrated that ROS–β-CD exhibited superior anticancer properties compared to free ROS, effectively reducing the viability and proliferation of the MD-MBA-231 cell line and inducing apoptosis. This research signifies a substantial advancement in developing therapeutic strategies for TNBC, leveraging the distinct properties of the ROS–β-CD inclusion complex.
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publishDate 2024-11-01
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spelling doaj-art-d59f73d3cb0c45dea148b051497c75382024-11-26T18:17:51ZengMDPI AGPharmaceutics1999-49232024-11-011611140810.3390/pharmaceutics16111408Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion ComplexYuan Li0Muhammad Inam1Muhammad Waqqas Hasan2Kaixin Chen3Zhongqian Zhang4Yongcheng Zhu5Jiayu Huang6Zhuowen Wu7Wenjie Chen8Min Li9Department of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaGraduate School of Biomedical Engineering, ARC Centre of Excellence in Nanoscale Biophotonics, Faculty of Engineering, UNSW Sydney, Sydney, NSW 2052, AustraliaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, ChinaDepartment of Emergency, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou 510260, China<b>Background</b>: Rosmarinic acid (ROS) has gained notable attention for its anticancer potential; however, its limited aqueous solubility hinders its effective delivery and application in pharmaceutical formulations. <b>Methods</b>: To overcome this limitation, an inclusion complex of ROS with β-cyclodextrin (β-CD) was prepared using the recrystallization method. The resultant ROS–β-CD complex was comprehensively characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). <b>Results:</b> The ROS–β-CD complex showed a significant improvement in the solubility and dissolution profile of ROS, underscoring its potential for enhanced bioavailability and therapeutic efficacy in pharmaceutical applications. In vitro assays were performed to assess the effects on cell viability, proliferation, apoptotic pathways, and 3D spheroid tumor models. <b>Conclusions:</b> The results demonstrated that ROS–β-CD exhibited superior anticancer properties compared to free ROS, effectively reducing the viability and proliferation of the MD-MBA-231 cell line and inducing apoptosis. This research signifies a substantial advancement in developing therapeutic strategies for TNBC, leveraging the distinct properties of the ROS–β-CD inclusion complex.https://www.mdpi.com/1999-4923/16/11/1408rosmarinic acidcyclodextrinphysicochemicalmolecular dockinginclusion complexTNBC
spellingShingle Yuan Li
Muhammad Inam
Muhammad Waqqas Hasan
Kaixin Chen
Zhongqian Zhang
Yongcheng Zhu
Jiayu Huang
Zhuowen Wu
Wenjie Chen
Min Li
Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex
Pharmaceutics
rosmarinic acid
cyclodextrin
physicochemical
molecular docking
inclusion complex
TNBC
title Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex
title_full Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex
title_fullStr Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex
title_full_unstemmed Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex
title_short Optimizing Antitumor Effect of Triple-Negative Breast Cancer via Rosmarinic Acid–β-Cyclodextrin Inclusion Complex
title_sort optimizing antitumor effect of triple negative breast cancer via rosmarinic acid β cyclodextrin inclusion complex
topic rosmarinic acid
cyclodextrin
physicochemical
molecular docking
inclusion complex
TNBC
url https://www.mdpi.com/1999-4923/16/11/1408
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