Microneedle-Mediated Delivery of Lipid-Coated Cisplatin Nanoparticles for Efficient and Safe Cancer Therapy

Xinmiao Lan, Juncong She, Di An Lin, Yu Xu, Xuan Li, Wei Fa Yang, Vivian Wai Yan Lui, Lijian Jin, Xi Xie, Yu Xiong Su

Research output: Contribution to journalArticlepeer-review

71 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)33060-33069
Number of pages10
JournalACS Applied Materials and Interfaces
Volume10
Issue number39
DOIs
StatePublished - Oct 3 2018
Externally publishedYes

Keywords

  • cancer therapy
  • cisplatin
  • drug delivery
  • microneedle
  • nanoparticle

ASJC Scopus subject areas

  • Materials Science(all)

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