埃多沙班包覆 beta-1,4-聚-D-葡糖胺纳米颗粒,用于靶向治疗静脉血栓的匿名斯图尔特-普罗因子。

IF 4.3 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Journal of Drug Targeting Pub Date : 2024-11-01 Epub Date: 2024-07-22 DOI:10.1080/1061186X.2024.2377611
Pavazhaviji Pazhani, Jose Prakash Dharmian, Somasundaram Arumugam, Pavithra Pazhani, Vijaya Vara Prasad Medapati
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引用次数: 0

摘要

本研究利用响应面方法学,通过研究设计方面与实验数据之间的相关性,寻找开发壳聚糖(CS)屏蔽纳米颗粒(NPs)-药物转运体的方法,以提高一水托沙坦酯(ETM)口服给药的生物利用度。利用三聚磷酸钠(TPP)对 CS 进行离子凝胶化,开发出了 ETM 负载 CS 纳米粒子(ETM-CS-NPs)。利用 Zeta 分析仪和扫描电子显微镜,对 ETM-CS-NPs 的粒度(PS)、Zeta 电位(ZP)、表面形态、多分散指数(PDI)、夹带效率(EE)和药物负载量(DL)进行了评估。使用傅立叶变换红外光谱评估了 NPs 中药物与聚合物的相互作用。响应面法和 Design-Expert 软件对 ETM-CS-NPs 进行了优化。利用响应面方法分析了 CS 量、TPP 量和冰醋酸量等自变量对 PS、PDI 和 ZP 的影响。优化后的 ETM-CS-NPs 确定了 PS(354.8 nm)、PDI(0.509)、ZP(43.7 + mV)、EE%(70.3 ± 1.3)和 DL%(9.1 ± 0.4)的最佳组合。使用活化部分凝血活酶时间(aPTT)、凝血酶原时间(PT)和凝血酶时间(TT)测定评估了 ETM-CS-NPs 的抗凝活性。总之,我们已经建立了一种实用且一致的方法,其应用已在体外得到证实,这表明该方法可用于未来研究 ETM-CS-NPs 在体内的生物分布,以进行特定的抗血栓治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Edoxaban enfolded beta-1,4-poly-d-glucosamine nanoparticles for targeting eponym Stuart-Prower factor for treatment of venous thrombosis.

The present research looked for ways to develop shielded nanoparticles (NPs)-drug transporters made of chitosan (CS) to enhance the bioavailability of edoxaban tosylate monohydrate (ETM) for oral administration by examining the correlation among design aspects and data from experiments using response surface methodology (RSM). ETM-loaded CS nanoparticles (ETM-CS-NPs) were developed using the ionic gelation of CS with tripolyphosphate (TPP). Utilising Zeta-sizer and scanning electron microscopy, the ETM-CS-NPs were evaluated for particle size (PS), zeta potential (ZP), surface morphology, polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Drug and polymer interactions in NPs were assessed using Fourier transform infra-red spectroscopy. The response surface approach and Design-Expert software optimised the ETM-CS-NPs. Using RSM, the effects of independent variables such as the amount of CS, the amount of TPP, and the amount of glacial acetic acid on PS, PDI and ZP were analysed. The optimal combination of PS (354.8 nm), PDI (0.509), ZP (43.7 + mV), % EE (70.3 ± 1.3) and % DL (9.1 ± 0.4) has been identified for the optimised ETM-CS-NPs. ETM-CS-NPs' anticoagulant activity was evaluated using activated partial thromboplastin time (aPTT), prothrombin time (PT) and thrombin time (TT) assays. In conclusion, a practical and consistent method has been established, and its application has been proven in vitro, indicating its utility for future studies of the biological distribution of ETM-CS-NPs in vivo for specific antithrombotic treatments.

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来源期刊
CiteScore
9.10
自引率
0.00%
发文量
165
审稿时长
2 months
期刊介绍: Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs. Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.
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