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靶向聚合原卟啉纳米颗粒:优化、评价及体内肝脏摄取以改善疟疾治疗。

Targeted polymeric primaquine nanoparticles: optimization, evaluation, and in-vivo liver uptake for improved malaria treatment.

机构信息

Institute of Pharmaceutical Research (IPR), GLA University, Mathura, Uttar Pradesh, India.

ShriRam College of Pharmacy, National Expressway, Banmore Gwalior, Madhya Pradesh, India.

出版信息

J Biomater Sci Polym Ed. 2024 Dec;35(18):2867-2883. doi: 10.1080/09205063.2024.2391225. Epub 2024 Sep 1.

DOI:10.1080/09205063.2024.2391225
PMID:39217616
Abstract

Primaquine (PQ) is a widely used antimalarial drug, but its high dosage requirements can lead to significant tissue damage and adverse gastrointestinal and hematological effects. Recent studies have shown that nanoformulations can enhance the bioavailability of pharmaceuticals, thereby increasing efficacy, reducing dosing frequency, and minimizing toxicity. In this study, PQ-loaded PLGA nanoparticles (PQ-NPs) were prepared using a modified double emulsion solvent evaporation technique (w/o/w). The PQ-NPs exhibited a mean particle size of 228 ± 2.6 nm, a zeta potential of +27.4 mV, and an encapsulation efficiency of 81.3 ± 3.5%. Scanning electron microscopy (SEM) confirmed their spherical morphology, and the release profile demonstrated continuous drug release over 72 h. Differential scanning calorimetry (DSC) thermograms indicated that the drug was present in the nanoparticles, with improved physical stability. Fourier-transform infrared spectroscopy (FTIR) analysis showed no interactions between the various substances in the NPs. studies in Swiss albino mice infected with revealed that the nanoformulated PQ was 20% more effective than the standard oral dose. Biodistribution studies indicated that 80% of the NPs accumulated in the liver, highlighting their potential for targeted drug delivery. This research demonstrates the successful development of a nanomedicine delivery system for antimalarial drugs, offering a promising strategy to enhance treatment efficacy while reducing adverse effects.

摘要

伯氨喹(PQ)是一种广泛使用的抗疟药物,但它的高剂量要求会导致显著的组织损伤和不良的胃肠道及血液学效应。最近的研究表明,纳米制剂可以提高药物的生物利用度,从而提高疗效、减少给药频率,并最大限度地降低毒性。在本研究中,使用改良的双乳液溶剂蒸发技术(w/o/w)制备了载伯氨喹 PLGA 纳米粒(PQ-NPs)。PQ-NPs 的平均粒径为 228±2.6nm,Zeta 电位为+27.4mV,包封效率为 81.3±3.5%。扫描电子显微镜(SEM)证实了其球形形态,释放曲线表明药物在 72h 内持续释放。差示扫描量热法(DSC)热图谱表明药物存在于纳米粒中,具有改善的物理稳定性。傅里叶变换红外光谱(FTIR)分析表明 NPs 中各物质之间没有相互作用。在感染的瑞士白化小鼠中进行的研究表明,纳米制剂的 PQ 比标准口服剂量更有效 20%。生物分布研究表明,80%的 NPs 积聚在肝脏中,这突出了它们在靶向药物递送中的潜力。这项研究展示了抗疟药物纳米医学递送系统的成功开发,为提高治疗效果同时降低不良反应提供了一种有前景的策略。

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