Synthesis and Characterization of Novel Amphiphilic Peptide and its Application in the Development of Niosomal Formulation as a Drug Delivery Carrier for Curcumin

IF 2.7 4区 化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR
Humira Karim, Khadija Rehman, Sadiq Noor Khan, Ali Asgher Shuja, Tasmina Kanwal, Shabana Usman Simjee, Muhammad Raza Shah, Farzana Shaheen
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Abstract

Developing effective therapy for cancer using a natural product like curcumin (CR) is an active area of research. The efficacy of CR against different types of cancers is significantly impeded by its non-specificity, low aqueous solubility, and high metabolism. In this study, novel amphiphilic peptide (AMP) was synthesized and their potential to carry CR into cancer cells via niosomal vesicles was examined. The synthesized AMP was characterized using several techniques such as FAB-MS, HRFAB-MS, 1H-, and 13C-NMR spectroscopy, which was then used to produce niosomal vesicles. CR-loaded AMP niosomal vesicles (CR-AMP-Vesicles) were also characterized in terms of size, zeta potential, PDI, and surface morphology. CR-AMP-Vesicles exhibited a smaller size of about 387.70 nm with 77.32% CR encapsulation and a regulated drug release profile. The AMP and AMP-Vesicles are reported for the first time. Moreover, we are the first to develop AMP-CR-Vesicles and to report the activity of the developed AMP-CR-Vesicles against chronic myeloid leukemia cell lines. The anticancer activity of the formulation was evaluated against chronic myeloid leukemia cell lines which exhibited a promising response with the IC50 of 25 µM. Furthermore, the cytotoxicity of produced vesicles on human normal fibroblast 3T3 cells was studied and found to be non-cytotoxic. The overall results indicate that the developed novel CR-AMP-Vesicles are very effective and promising. The novel formulation has the potential for broader applications along with the fact that the developed niosomes have the potential to substantially reduce the cytotoxicity of bioactive compounds against normal cells while maintaining biological activity.

Abstract Image

新型两亲肽的合成与表征及其在开发作为姜黄素给药载体的 Niosomal 制剂中的应用
利用姜黄素(CR)等天然产品开发有效的癌症疗法是一个活跃的研究领域。姜黄素的非特异性、低水溶性和高代谢性严重阻碍了它对不同类型癌症的疗效。本研究合成了新型两亲肽 (AMP),并考察了它们通过niosomal囊泡携带CR进入癌细胞的潜力。研究人员利用多种技术,如 FAB-MS、HRFAB-MS、1H-和 13C-NMR 光谱,对合成的 AMP 进行了表征,然后将其用于生产纳米囊泡。此外,还从大小、ZETA电位、PDI和表面形态等方面对负载CR的AMP小泡(CR-AMP-Vesicles)进行了表征。CR-AMP-囊泡的尺寸较小,约为 387.70 nm,CR 包封率为 77.32%,药物释放情况良好。这是首次报道 AMP 和 AMP-囊泡。此外,我们还首次开发了 AMP-CR 囊泡,并报告了所开发的 AMP-CR 囊泡对慢性髓性白血病细胞系的活性。我们评估了制剂对慢性髓性白血病细胞株的抗癌活性,结果显示其抗癌活性很好,IC50 为 25 µM。此外,还研究了制备的囊泡对人类正常成纤维细胞 3T3 细胞的细胞毒性,结果发现这些囊泡没有细胞毒性。总体结果表明,所开发的新型 CR-AMP 囊泡非常有效,前景广阔。这种新型配方具有更广泛的应用潜力,而且所开发的纳米囊泡有可能在保持生物活性的同时,大大降低生物活性化合物对正常细胞的细胞毒性。
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来源期刊
Journal of Cluster Science
Journal of Cluster Science 化学-无机化学与核化学
CiteScore
6.70
自引率
0.00%
发文量
166
审稿时长
3 months
期刊介绍: The journal publishes the following types of papers: (a) original and important research; (b) authoritative comprehensive reviews or short overviews of topics of current interest; (c) brief but urgent communications on new significant research; and (d) commentaries intended to foster the exchange of innovative or provocative ideas, and to encourage dialogue, amongst researchers working in different cluster disciplines.
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