{"title":"用叶酸修饰的聚乙二醇化PLGA纳米颗粒靶向递送白藜芦醇用于癌症治疗：表征和体外研究。","authors":"Snehaprabha Tomar, Kapil Joshi, Vigi Chaudhary, Ragini Singh, Naveen Chaudhary, Vikram Kumar, Sudarshan Singh Lakhawat, Ashwani Kumar Yadav","doi":"10.1080/03639045.2025.2562181","DOIUrl":null,"url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to develop, characterize, and evaluate resveratrol-loaded pegylated PLGA [poly (lactic-co-glycolic acid)] nanoparticles with folate conjugation for improved drug delivery and cytotoxic efficacy against MCF7 breast cancer cells.</p><p><strong>Significance: </strong>The significance of this drug delivery system is to enhance the wetting characteristics of resveratrol and reduce nanoparticle agglomeration for maximizing therapeutic efficacy while minimizing systemic cytotoxicity using PLGA and polyethylene glycol (PEG) polymeric nanoparticles as carriers. The process of fabrication and characterization of polymeric conjugate by utilizing PLGA-PEG surface engineered with folic acid for target specificity has already been investigated.</p><p><strong>Methods: </strong>Nanoparticles were prepared by double-emulsion solvent evaporation using PPF (PLGA-PEG-FOLATE conjugate polymer) and PVA (Poly vinyl alcohol) as a stabilizer. Compatibility studies were performed using FTIR, DSC, and XRD. Formulations (NF1-NF8) were evaluated for particle size, zeta potential, drug loading, entrapment efficiency, and <i>in vitro</i> release. Surface morphology was assessed by SEM and TEM. MTT assay evaluated cytotoxicity while fluorescence microscopy analyzed cellular uptake.</p><p><strong>Results: </strong>Compatibility studies confirmed no drug-excipient interactions. NF3 exhibited optimal characteristics: particle size 332.1 nm, zeta potential -24.6 mV, entrapment efficiency 78.65 ± 0.165%, and drug loading 36.19 ± 0.154%. <i>In vitro</i> release was sustained up to 120 h (75.17 ± 0.22%), fitting zero-order kinetics with Fickian diffusion. NF3 displayed enhanced cytotoxicity (IC50 340.26 nM) compared to free resveratrol (993.29 nM). Fluorescence microscopy confirmed improved cellular uptake <i>via</i> folate conjugation.</p><p><strong>Conclusion: </strong>Resveratrol-loaded PPF nanoparticles, particularly NF3, demonstrated superior stability, sustained release, and enhanced anticancer activity, making them a promising candidate for targeted breast cancer therapy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-16"},"PeriodicalIF":2.2000,"publicationDate":"2025-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Targeted delivery of resveratrol using PEGylated PLGA nanoparticles decorated with folic acid for cancer therapy: characterization, and <i>in vitro</i> studies.\",\"authors\":\"Snehaprabha Tomar, Kapil Joshi, Vigi Chaudhary, Ragini Singh, Naveen Chaudhary, Vikram Kumar, Sudarshan Singh Lakhawat, Ashwani Kumar Yadav\",\"doi\":\"10.1080/03639045.2025.2562181\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objective: </strong>This study aimed to develop, characterize, and evaluate resveratrol-loaded pegylated PLGA [poly (lactic-co-glycolic acid)] nanoparticles with folate conjugation for improved drug delivery and cytotoxic efficacy against MCF7 breast cancer cells.</p><p><strong>Significance: </strong>The significance of this drug delivery system is to enhance the wetting characteristics of resveratrol and reduce nanoparticle agglomeration for maximizing therapeutic efficacy while minimizing systemic cytotoxicity using PLGA and polyethylene glycol (PEG) polymeric nanoparticles as carriers. The process of fabrication and characterization of polymeric conjugate by utilizing PLGA-PEG surface engineered with folic acid for target specificity has already been investigated.</p><p><strong>Methods: </strong>Nanoparticles were prepared by double-emulsion solvent evaporation using PPF (PLGA-PEG-FOLATE conjugate polymer) and PVA (Poly vinyl alcohol) as a stabilizer. Compatibility studies were performed using FTIR, DSC, and XRD. Formulations (NF1-NF8) were evaluated for particle size, zeta potential, drug loading, entrapment efficiency, and <i>in vitro</i> release. Surface morphology was assessed by SEM and TEM. MTT assay evaluated cytotoxicity while fluorescence microscopy analyzed cellular uptake.</p><p><strong>Results: </strong>Compatibility studies confirmed no drug-excipient interactions. NF3 exhibited optimal characteristics: particle size 332.1 nm, zeta potential -24.6 mV, entrapment efficiency 78.65 ± 0.165%, and drug loading 36.19 ± 0.154%. <i>In vitro</i> release was sustained up to 120 h (75.17 ± 0.22%), fitting zero-order kinetics with Fickian diffusion. NF3 displayed enhanced cytotoxicity (IC50 340.26 nM) compared to free resveratrol (993.29 nM). Fluorescence microscopy confirmed improved cellular uptake <i>via</i> folate conjugation.</p><p><strong>Conclusion: </strong>Resveratrol-loaded PPF nanoparticles, particularly NF3, demonstrated superior stability, sustained release, and enhanced anticancer activity, making them a promising candidate for targeted breast cancer therapy.</p>\",\"PeriodicalId\":11263,\"journal\":{\"name\":\"Drug Development and Industrial Pharmacy\",\"volume\":\" \",\"pages\":\"1-16\"},\"PeriodicalIF\":2.2000,\"publicationDate\":\"2025-09-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Development and Industrial Pharmacy\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/03639045.2025.2562181\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Development and Industrial Pharmacy","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/03639045.2025.2562181","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Targeted delivery of resveratrol using PEGylated PLGA nanoparticles decorated with folic acid for cancer therapy: characterization, and in vitro studies.
Objective: This study aimed to develop, characterize, and evaluate resveratrol-loaded pegylated PLGA [poly (lactic-co-glycolic acid)] nanoparticles with folate conjugation for improved drug delivery and cytotoxic efficacy against MCF7 breast cancer cells.
Significance: The significance of this drug delivery system is to enhance the wetting characteristics of resveratrol and reduce nanoparticle agglomeration for maximizing therapeutic efficacy while minimizing systemic cytotoxicity using PLGA and polyethylene glycol (PEG) polymeric nanoparticles as carriers. The process of fabrication and characterization of polymeric conjugate by utilizing PLGA-PEG surface engineered with folic acid for target specificity has already been investigated.
Methods: Nanoparticles were prepared by double-emulsion solvent evaporation using PPF (PLGA-PEG-FOLATE conjugate polymer) and PVA (Poly vinyl alcohol) as a stabilizer. Compatibility studies were performed using FTIR, DSC, and XRD. Formulations (NF1-NF8) were evaluated for particle size, zeta potential, drug loading, entrapment efficiency, and in vitro release. Surface morphology was assessed by SEM and TEM. MTT assay evaluated cytotoxicity while fluorescence microscopy analyzed cellular uptake.
Results: Compatibility studies confirmed no drug-excipient interactions. NF3 exhibited optimal characteristics: particle size 332.1 nm, zeta potential -24.6 mV, entrapment efficiency 78.65 ± 0.165%, and drug loading 36.19 ± 0.154%. In vitro release was sustained up to 120 h (75.17 ± 0.22%), fitting zero-order kinetics with Fickian diffusion. NF3 displayed enhanced cytotoxicity (IC50 340.26 nM) compared to free resveratrol (993.29 nM). Fluorescence microscopy confirmed improved cellular uptake via folate conjugation.
Conclusion: Resveratrol-loaded PPF nanoparticles, particularly NF3, demonstrated superior stability, sustained release, and enhanced anticancer activity, making them a promising candidate for targeted breast cancer therapy.
期刊介绍：
The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.
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