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Microneedle-Mediated Delivery of Lipid-Coated Cisplatin Nanoparticles for Efficient and Safe Cancer Therapy
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2018-09-11 00:00:00 , DOI: 10.1021/acsami.8b12926
Xinmiao Lan , Juncong She 1 , Di-an Lin 1 , Yu Xu , Xuan Li , Wei-fa Yang , Vivian Wai Yan Lui 2 , Lijian Jin , Xi Xie 1, 3 , Yu-xiong Su
Affiliation  

Cisplatin is the first-line chemotherapeutic agent, but its systemic toxicity and side effects severely limit its clinical use. We report a microneedle technique to mediate the transdermal delivery of lipid-coated cisplatin nanoparticles (LCC-NPs) for efficient and safe cancer therapy. Cisplatin was encapsulated by tumor-targeting pH-responsive lipid nanoparticles with a high loading rate of 80%, and the encapsulation substantially increased the solubility of cisplatin and enhanced its antitumor efficiency in vitro. The LCC-NPs were embedded in dissolvable microneedles, and released from the microneedles after inserting into the skin. This enabled the nanoparticles to pass the stratum corneum for safe local delivery. An in vivo study with a xenograft tumor animal model demonstrated that microneedle arrays loaded with cisplatin nanoparticles significantly increased cytotoxicity and apoptosis in cancer cells with an apoptotic index of 58.6%, resulting in significantly reduced tumor volume and weight. Moreover, serum platinum, pulmonary toxicity, hepatotoxicity, and nephrotoxicity were not detected in vivo, indicating that this technique is biosafe. The cisplatin-nanoparticle microneedle system developed in this study may offer promising opportunities in cancer therapy for enhancing antitumor effects and reducing systemic toxicity and side effects.

中文翻译:

微针介导的脂质包裹的顺铂纳米颗粒的有效和安全的癌症治疗。

顺铂是一线化疗药物,但其全身毒性和副作用严重限制了其临床应用。我们报告了一种微针技术,以介导脂质包覆的顺铂纳米颗粒(LCC-NPs)的透皮递送,以进行有效且安全的癌症治疗。顺铂被靶向肿瘤的pH响应脂质纳米粒包裹,载药率高达80%,该包裹大大增加了顺铂的溶解度,并提高了其体外抗肿瘤效率。LCC-NPs嵌入可溶解的微针中,并在插入皮肤后从微针中释放出来。这使纳米颗粒能够通过角质层,以安全地进行局部递送。异种移植肿瘤动物模型的体内研究表明,载有顺铂纳米颗粒的微针阵列可显着增加癌细胞的细胞毒性和凋亡,其凋亡指数为58.6%,从而显着降低了肿瘤的体积和重量。此外,在体内未检测到血清铂,肺毒性,肝毒性和肾毒性,表明该技术是生物安全的。在这项研究中开发的顺铂-纳米微粒微针系统可能在癌症治疗中提供有希望的机会,以增强抗肿瘤作用并降低全身毒性和副作用。在体内未检测到肾毒性和肾毒性,表明该技术是生物安全的。在这项研究中开发的顺铂-纳米微粒微针系统可能在癌症治疗中提供有希望的机会,以增强抗肿瘤作用并降低全身毒性和副作用。在体内未检测到肾毒性和肾毒性,表明该技术是生物安全的。在这项研究中开发的顺铂-纳米微粒微针系统可能在癌症治疗中提供有希望的机会,以增强抗肿瘤作用并降低全身毒性和副作用。
更新日期:2018-09-11
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