{"title":"Folate-Modified Drug-Carrying Micelles With pH-Responsiveness for Curcumin-Targeted Delivery","authors":"Xiuhong Duan, Zimeng Wang, Handa Liu, Hua Ma, Xuepeng Zhang, Lihua Liu, Hongzhou Shang, Ning Qiao","doi":"10.1002/app.57180","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>A predrug delivery system combining tumor-targeting and pH-responsive features was synthesized using baicalin (BAI), polyethylene glycol (PEG), and folic acid (FA). BAI and PEG were linked via esterification to create pH-sensitive ester bonds (<span></span>COO<span></span>) that facilitate drug release in acidic environments, while FA was attached to PEG through substitution. This system, named FA-PEG-COO-BAI (FPB), encapsulated curcumin (CUR) to form drug-loaded micelles. The impact of drug-loading conditions, such as sonication duration and initial drug dosage, on CUR/FA-PEG-COO-BAI encapsulation efficiency and drug release was investigated. In vitro studies demonstrated a maximum encapsulation rate of (73.09 ± 3.31)% and a drug-loading rate of (11.90 ± 0.69)%. Drug release from CUR/FA-PEG-COO-BAI micelles accelerated as pH decreased, confirming pH-responsive behavior. Cellular uptake and antitumor assays suggested effective tumor targeting and inhibition of proliferation. Hemolysis and cell viability assays indicated low toxicity. These findings underscore the potential of CUR/FA-PEG-COO-BAI micelles for controlled drug release and targeted therapy.</p>\n </div>","PeriodicalId":183,"journal":{"name":"Journal of Applied Polymer Science","volume":"142 29","pages":""},"PeriodicalIF":2.7000,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Applied Polymer Science","FirstCategoryId":"92","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/app.57180","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"POLYMER SCIENCE","Score":null,"Total":0}
引用次数: 0
Abstract
A predrug delivery system combining tumor-targeting and pH-responsive features was synthesized using baicalin (BAI), polyethylene glycol (PEG), and folic acid (FA). BAI and PEG were linked via esterification to create pH-sensitive ester bonds (COO) that facilitate drug release in acidic environments, while FA was attached to PEG through substitution. This system, named FA-PEG-COO-BAI (FPB), encapsulated curcumin (CUR) to form drug-loaded micelles. The impact of drug-loading conditions, such as sonication duration and initial drug dosage, on CUR/FA-PEG-COO-BAI encapsulation efficiency and drug release was investigated. In vitro studies demonstrated a maximum encapsulation rate of (73.09 ± 3.31)% and a drug-loading rate of (11.90 ± 0.69)%. Drug release from CUR/FA-PEG-COO-BAI micelles accelerated as pH decreased, confirming pH-responsive behavior. Cellular uptake and antitumor assays suggested effective tumor targeting and inhibition of proliferation. Hemolysis and cell viability assays indicated low toxicity. These findings underscore the potential of CUR/FA-PEG-COO-BAI micelles for controlled drug release and targeted therapy.
以黄芩苷(BAI)、聚乙二醇(PEG)和叶酸(FA)为原料,合成了一种结合肿瘤靶向和ph响应特性的药物前递送系统。BAI和PEG通过酯化反应连接,形成ph敏感的酯键,促进药物在酸性环境中释放,而FA通过取代连接到PEG上。该系统被命名为FA-PEG-COO-BAI (FPB),封装姜黄素(CUR)形成载药胶束。考察超声时间、初始给药剂量等载药条件对CUR/FA-PEG-COO-BAI包封效率和药物释放的影响。体外实验表明,其包封率为(73.09±3.31)%,载药率为(11.90±0.69)%。随着pH的降低,CUR/FA-PEG-COO-BAI胶束的药物释放加速,证实了pH响应行为。细胞摄取和抗肿瘤实验表明其有效靶向肿瘤和抑制增殖。溶血和细胞活力试验显示低毒性。这些发现强调了CUR/ fa - peg - co - bai胶束在控制药物释放和靶向治疗方面的潜力。
期刊介绍:
The Journal of Applied Polymer Science is the largest peer-reviewed publication in polymers, #3 by total citations, and features results with real-world impact on membranes, polysaccharides, and much more.