Nanofibrous silica microparticles/polymer hybrid aerogels for sustained delivery of poorly water-soluble camptothecin

J Colloid Interface Sci. 2020 May 1:567:92-102. doi: 10.1016/j.jcis.2020.01.110. Epub 2020 Jan 29.

Abstract

The surface functionalization of nanoporous silica materials with chemical agents opens up numerous possibilities, including improvement in the materials' ability to carry high payloads of drugs. In this study, KCC-1 nanofibrous silica microparticles are functionalized with methyl groups and then combined with poly(vinyl alcohol) (PVA) and poly(acrylic acid) (PAA) to produce hybrid aerogels that can deliver a poorly water-soluble anticancer drug. The synthetic steps involve freeze-drying a polymer solution of PVA and PAA that contains methyl-modified KCC-1 microparticles and then cross-linking the two polymers via a solid-state reaction. Benefiting from the incorporated methyl-modified KCC-1 microparticles, the hybrid aerogels can load and deliver a payload of camptothecin (CPT), an anticancer drug with antitumor activity but limited clinical application due to its hydrophobicity. The aerogels also show a sustained release of CPT for more than two weeks. The drug release profile can further be tuned by varying the relative amounts of PVA, PAA, and methyl-modified KCC-1. The aerogels are biocompatible to healthy cells, such as immortalized human epithelial (HaCaT), African green monkey kidney (Vero) and murine fibroblast (L929) cells. When loaded with CPT, they show potent antitumor activity against HeLa (HPV18-positive), SiHa (HPV16-positive) and C33A (HPV-negative) cancer cells, significantly inhibiting cell growth.

Keywords: Aerogels; Anticancer drug release; Camptothecin; Hybrid material; Nanofibrous silica.

MeSH terms

  • Acrylic Resins / chemistry
  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Biocompatible Materials / chemistry
  • Camptothecin / chemistry
  • Camptothecin / pharmacology*
  • Cell Line
  • Cell Proliferation / drug effects
  • Drug Delivery Systems*
  • Drug Liberation
  • Drug Screening Assays, Antitumor
  • Gels / chemistry
  • Humans
  • Mice
  • Molecular Structure
  • Nanofibers / chemistry*
  • Particle Size
  • Polyvinyl Alcohol / chemistry
  • Silicon Dioxide / chemistry
  • Solubility
  • Surface Properties

Substances

  • Acrylic Resins
  • Antineoplastic Agents, Phytogenic
  • Biocompatible Materials
  • Gels
  • carbopol 940
  • Silicon Dioxide
  • Polyvinyl Alcohol
  • Camptothecin