Biodegradable polymeric nanocomposite containing phloretin for enhanced oral bioavailability and improved myocardial ischaemic recovery.

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2024-12-01 Epub Date: 2024-10-21 DOI:10.1080/02652048.2024.2418608

Prasanti Sharma, Trishna Bal, Sandeep Kumar Singh, Neelima Sharma

{"title":"Biodegradable polymeric nanocomposite containing phloretin for enhanced oral bioavailability and improved myocardial ischaemic recovery.","authors":"Prasanti Sharma, Trishna Bal, Sandeep Kumar Singh, Neelima Sharma","doi":"10.1080/02652048.2024.2418608","DOIUrl":null,"url":null,"abstract":"Aim: The study aimed to enhance phloretin's oral absorption and systemic availability through nanoencapsulation within biodegradable polymers, improving its anti-oxidant and cardioprotective potential.Methods: Phloretin-loaded polymeric nanocomposites were prepared using ionic gelation and optimised for yield, encapsulation, loading, particle size, PdI and zeta potential. The formulation was characterised by FTIR, XRD, FESEM and MS. In-vitro drug release, stability, pharmacokinetics, biodistribution, anti-oxidant capacity, haemolysis and both in-vitro and in-vivo assessments were conducted in an ischaemia-induced rat model.Results: The average particle size, zeta potential, encapsulation and drug loading of the optimised nanoparticles were 105.8 ± 1.92 nm, -41.5 ± 1.10 mV, 92.36 ± 0.01% and 18.47 ± 0.38%, respectively. Nano-phloretin enhanced oral bioavailability, anti-oxidant capacity. In-vivo, it reduced myocardial infarct size by ∼46% versus ∼13% for free phloretin, showing significant cardiomyocyte protection and ROS suppression.Conclusion: The study demonstrates polymer-based nanoparticles as effective oral drug delivery systems capable of enhancing both systemic bioavailability and therapeutic efficacy of the encapsulated drug.","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"754-769"},"PeriodicalIF":3.0000,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of microencapsulation","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/02652048.2024.2418608","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/10/21 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}

引用次数: 0

Abstract

Aim: The study aimed to enhance phloretin's oral absorption and systemic availability through nanoencapsulation within biodegradable polymers, improving its anti-oxidant and cardioprotective potential.

Methods: Phloretin-loaded polymeric nanocomposites were prepared using ionic gelation and optimised for yield, encapsulation, loading, particle size, PdI and zeta potential. The formulation was characterised by FTIR, XRD, FESEM and MS. In-vitro drug release, stability, pharmacokinetics, biodistribution, anti-oxidant capacity, haemolysis and both in-vitro and in-vivo assessments were conducted in an ischaemia-induced rat model.

Results: The average particle size, zeta potential, encapsulation and drug loading of the optimised nanoparticles were 105.8 ± 1.92 nm, -41.5 ± 1.10 mV, 92.36 ± 0.01% and 18.47 ± 0.38%, respectively. Nano-phloretin enhanced oral bioavailability, anti-oxidant capacity. In-vivo, it reduced myocardial infarct size by ∼46% versus ∼13% for free phloretin, showing significant cardiomyocyte protection and ROS suppression.

Conclusion: The study demonstrates polymer-based nanoparticles as effective oral drug delivery systems capable of enhancing both systemic bioavailability and therapeutic efficacy of the encapsulated drug.

查看原文本刊更多论文

生物可降解聚合物纳米复合材料，含有可提高口服生物利用度和改善心肌缺血恢复的酞丁胺。

目的：该研究旨在通过在生物可降解聚合物中进行纳米包囊，增强酚络汀的口服吸收和全身可用性，从而提高其抗氧化和保护心脏的潜力：方法：采用离子凝胶法制备了载药萝芙汀的聚合物纳米复合材料，并对其产量、封装、载药量、粒度、PdI 和 zeta 电位进行了优化。傅立叶变换红外光谱（FTIR）、XRD、FESEM 和 MS 对配方进行了表征。在缺血诱导的大鼠模型中进行了体外药物释放、稳定性、药代动力学、生物分布、抗氧化能力、溶血以及体内和体外评估：结果：优化纳米颗粒的平均粒径、ZETA电位、包封率和载药量分别为 105.8 ± 1.92 nm、-41.5 ± 1.10 mV、92.36 ± 0.01% 和 18.47 ± 0.38%。纳米紫檀素提高了口服生物利用度和抗氧化能力。在体内，它使心肌梗死面积缩小了 46%，而游离的小叶紫檀素则缩小了 13%，显示出显著的心肌细胞保护和 ROS 抑制作用：该研究表明，聚合物纳米颗粒是一种有效的口服给药系统，能够提高封装药物的全身生物利用度和疗效。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.