Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms
<b>Background:</b> Tanshinone IIA (Tan IIA) is a lipophilic active constituent derived from the rhizomes and roots of <i>Salvia miltiorrhiza Bunge</i> (Danshen), a common Chinese medicinal herb. However, clinical applications of Tan IIA are limited due to its poor solubility...
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| author | Tianying Ren Jing Wang Yingxin Ma Yichen Huang Somy Yoon Lijun Mu Ru Li Xuekun Wang Lina Zhang Pan Li Lusha Ji |
| author_facet | Tianying Ren Jing Wang Yingxin Ma Yichen Huang Somy Yoon Lijun Mu Ru Li Xuekun Wang Lina Zhang Pan Li Lusha Ji |
| author_sort | Tianying Ren |
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| description | <b>Background:</b> Tanshinone IIA (Tan IIA) is a lipophilic active constituent derived from the rhizomes and roots of <i>Salvia miltiorrhiza Bunge</i> (Danshen), a common Chinese medicinal herb. However, clinical applications of Tan IIA are limited due to its poor solubility in water. <b>Methods</b>: To overcome this limitation, we developed a calcium alginate hydrogel (CA) as a hydrophilic carrier for Tan IIA, which significantly improved its solubility. We also prepared nanoparticles with pH-responsive properties to explore their potential for controlled drug delivery. The physicochemical properties of Tan IIA/CA nanoparticles were evaluated, including their size, stability, and release profile. We also utilized RNA sequencing to further investigate the underlying anticancer mechanisms of Tan IIA/CA nanoparticles. <b>Results</b>: The Tan IIA/CA nanoparticles demonstrated enhanced solubility and exhibited potent anticancer activity in vitro. Additionally, the nanoparticles showed promising pH-responsive behavior, which is beneficial for controlled release applications. Further investigation into the molecular mechanisms revealed that the anticancer effects of Tan IIA/CA were mediated through apoptosis, ferroptosis, and autophagy pathways. <b>Conclusions:</b> This study confirms the anticancer potential and mechanisms of Tan IIA, while also presenting an innovative approach to enhance the solubility of this poorly soluble compound. The use of CA-based nanoparticles could be a valuable strategy for improving the therapeutic efficacy of Tan IIA in cancer treatment. |
| format | Article |
| id | doaj-art-aee53f4146af4cfbb384479ea7510084 |
| institution | Kabale University |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
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| series | Pharmaceutics |
| spelling | doaj-art-aee53f4146af4cfbb384479ea75100842025-01-24T13:45:47ZengMDPI AGPharmaceutics1999-49232025-01-011716610.3390/pharmaceutics17010066Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer MechanismsTianying Ren0Jing Wang1Yingxin Ma2Yichen Huang3Somy Yoon4Lijun Mu5Ru Li6Xuekun Wang7Lina Zhang8Pan Li9Lusha Ji10State Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, College of Pharmacy, Wenzhou Medical University, Wenzhou 325035, ChinaKey Laboratory for Pediatrics of Integrated Traditional and Western Medicine, Liaocheng People’s Hospital, Liaocheng 252000, ChinaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, ChinaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, ChinaCollege of Pharmacy, Chonnam National University, Gwangju 61186, Republic of KoreaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, ChinaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, ChinaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, ChinaCollege of Medicine, Liaocheng Vocational and Technical College, Liaocheng 252000, ChinaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, School of Pharmaceutical Sciences and Food Engineering, Liaocheng University, Liaocheng 252059, ChinaState Key Laboratory for Macromolecule Drugs and Large-Scale Manufacturing, College of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China<b>Background:</b> Tanshinone IIA (Tan IIA) is a lipophilic active constituent derived from the rhizomes and roots of <i>Salvia miltiorrhiza Bunge</i> (Danshen), a common Chinese medicinal herb. However, clinical applications of Tan IIA are limited due to its poor solubility in water. <b>Methods</b>: To overcome this limitation, we developed a calcium alginate hydrogel (CA) as a hydrophilic carrier for Tan IIA, which significantly improved its solubility. We also prepared nanoparticles with pH-responsive properties to explore their potential for controlled drug delivery. The physicochemical properties of Tan IIA/CA nanoparticles were evaluated, including their size, stability, and release profile. We also utilized RNA sequencing to further investigate the underlying anticancer mechanisms of Tan IIA/CA nanoparticles. <b>Results</b>: The Tan IIA/CA nanoparticles demonstrated enhanced solubility and exhibited potent anticancer activity in vitro. Additionally, the nanoparticles showed promising pH-responsive behavior, which is beneficial for controlled release applications. Further investigation into the molecular mechanisms revealed that the anticancer effects of Tan IIA/CA were mediated through apoptosis, ferroptosis, and autophagy pathways. <b>Conclusions:</b> This study confirms the anticancer potential and mechanisms of Tan IIA, while also presenting an innovative approach to enhance the solubility of this poorly soluble compound. The use of CA-based nanoparticles could be a valuable strategy for improving the therapeutic efficacy of Tan IIA in cancer treatment.https://www.mdpi.com/1999-4923/17/1/66tanshinone IIApH sensitivecalcium alginateautophagyapoptosiscancer therapy |
| spellingShingle | Tianying Ren Jing Wang Yingxin Ma Yichen Huang Somy Yoon Lijun Mu Ru Li Xuekun Wang Lina Zhang Pan Li Lusha Ji Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms Pharmaceutics tanshinone IIA pH sensitive calcium alginate autophagy apoptosis cancer therapy |
| title | Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms |
| title_full | Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms |
| title_fullStr | Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms |
| title_full_unstemmed | Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms |
| title_short | Preparation of pH-Responsive Tanshinone IIA-Loaded Calcium Alginate Nanoparticles and Their Anticancer Mechanisms |
| title_sort | preparation of ph responsive tanshinone iia loaded calcium alginate nanoparticles and their anticancer mechanisms |
| topic | tanshinone IIA pH sensitive calcium alginate autophagy apoptosis cancer therapy |
| url | https://www.mdpi.com/1999-4923/17/1/66 |
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