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载有他莫昔芬的丙烯酸树脂纳米颗粒:基于质量源于设计方法优化作为递送系统的纳米颗粒

Tamoxifen-Loaded Eudragit Nanoparticles: Quality by Design Approach for Optimization of Nanoparticles as Delivery System.

作者信息

Khattak Muzna Ali, Iqbal Zafar, Nasir Fazli, Neau Steven H, Khan Sumaira Irum, Hidayatullah Talaya, Pervez Sadia, Sakhi Mirina, Zainab Syeda Rabqa, Gohar Shazma, Alasmari Fawaz, Rahman Altafur, Maryam Gul E, Tahir Arbab

机构信息

Department of Pharmacy, University of Peshawar, Peshawar 25120, Pakistan.

Department of Pharmacy, Cecos University of IT and Emerging Sciences, Peshawar 25000, Pakistan.

出版信息

Pharmaceutics. 2023 Sep 22;15(10):2373. doi: 10.3390/pharmaceutics15102373.

DOI:10.3390/pharmaceutics15102373
PMID:37896131
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10609841/
Abstract

Nanoparticles have numerous applications as drug carriers in drug delivery. The aim of the study was to produce tamoxifen nanoparticles with a defined size and higher encapsulation for efficient tissue uptake with controlled drug release. The quality by design approach was utilized to produce tamoxifen-loaded Eudragit nanoparticles by identifying the significant process variables using the nanoprecipitation method. The process variables (amount of drug, polymer, and surfactant) were altered to analyze the influence on particle size (PS), % encapsulation efficiency (EE). The results showed that the drug and polymer individually as well as collectively have an impact on PS, while the surfactant has no impact on the PS. The %EE was influenced by the surfactant individually and in interaction with the drug. The linear regression model was endorsed to fit the data showing high R values (PS, 0.9146, %EE, 0.9070) and low values (PS, 0.0004, EE, 0.0005). The PS and EE were confirmed to be 178 nm and 90%, respectively. The nanoparticles were of spherical shape, as confirmed by SEM and TEM. The FTIR confirmed the absence of any incompatibility among the ingredients. The TGA confirmed that the NPs were thermally stable. The in vitro release predicted that the drug release followed Higuchi model.

摘要

纳米颗粒在药物递送中作为药物载体有众多应用。本研究的目的是制备具有特定尺寸和更高包封率的他莫昔芬纳米颗粒,以实现高效的组织摄取和可控的药物释放。采用质量源于设计的方法,通过纳米沉淀法确定显著的工艺变量,制备负载他莫昔芬的丙烯酸树脂纳米颗粒。改变工艺变量(药物、聚合物和表面活性剂的用量)以分析其对粒径(PS)、包封效率百分比(EE)的影响。结果表明,药物和聚合物单独以及共同对PS有影响,而表面活性剂对PS无影响。%EE受表面活性剂单独以及与药物相互作用的影响。线性回归模型被认可用于拟合数据,显示出高R值(PS为0.9146,%EE为0.9070)和低 值(PS为0.0004,EE为0.0005)。PS和EE分别被确认为178 nm和90%。通过扫描电子显微镜(SEM)和透射电子显微镜(TEM)证实纳米颗粒为球形。傅里叶变换红外光谱(FTIR)证实各成分之间不存在任何不相容性。热重分析(TGA)证实纳米颗粒具有热稳定性。体外释放预测药物释放遵循 Higuchi 模型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/d9f3895c8c68/pharmaceutics-15-02373-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/73bf240b25cc/pharmaceutics-15-02373-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/b5dae18ae4e4/pharmaceutics-15-02373-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/bccab777c809/pharmaceutics-15-02373-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/e6c0e5e356fd/pharmaceutics-15-02373-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/c6a69bb8ebf4/pharmaceutics-15-02373-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/474a91f9233f/pharmaceutics-15-02373-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/ea407e78e461/pharmaceutics-15-02373-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/d3391907d41b/pharmaceutics-15-02373-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/be57cd03a171/pharmaceutics-15-02373-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/480a04bdad2b/pharmaceutics-15-02373-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/8fdb461cf4f0/pharmaceutics-15-02373-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/d9f3895c8c68/pharmaceutics-15-02373-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/73bf240b25cc/pharmaceutics-15-02373-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/b5dae18ae4e4/pharmaceutics-15-02373-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/bccab777c809/pharmaceutics-15-02373-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/fa2ecf0c42ce/pharmaceutics-15-02373-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/e6c0e5e356fd/pharmaceutics-15-02373-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/c6a69bb8ebf4/pharmaceutics-15-02373-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/474a91f9233f/pharmaceutics-15-02373-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/ea407e78e461/pharmaceutics-15-02373-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/d3391907d41b/pharmaceutics-15-02373-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/be57cd03a171/pharmaceutics-15-02373-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/480a04bdad2b/pharmaceutics-15-02373-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/8fdb461cf4f0/pharmaceutics-15-02373-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f9/10609841/d9f3895c8c68/pharmaceutics-15-02373-g013.jpg

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