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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Main Authors: Tianying Ren, Jing Wang, Yingxin Ma, Yichen Huang, Somy Yoon, Lijun Mu, Ru Li, Xuekun Wang, Lina Zhang, Pan Li, Lusha Ji
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/1/66
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Summary:<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.
ISSN:1999-4923