Biodegradable microfibers deliver the antitumor drug temozolomide to glioma C6 cells in vitro

Pharmazie. 2010 Nov;65(11):830-4.

Abstract

To develop effective implants for delivery of 3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide (temozolomide; TM) with low initial burst and less neurotoxicity, TM-loaded poly-propylene carbonate (PPC) fiber was fabricated by electrospinning. Some of the fiber sheets were then covered with alginate (ALG). Influences of several preparation parameters on drug delivery behavior were investigated. The micro-morphology of these fibers was studied using scanning electron microscopy and differential scanning calorimetry. In vitro release properties of two forms of samples were observed and their cytotoxicity against C6 glioma cells was assessed. Using strict preparation parameters, smooth and uniform fiber could only be obtained when the PPC concentration was 8 % by weight, at 20cm and a voltage of 15 kV between the nozzle and the collection instrument. Fiber diameter was about 3 microm. The initial burst of drug-fiber sheets was reduced after the fiber sheets were covered with ALG. Cytotoxicity test results suggested that both forms of drug fibers inhibit the C6 glioma cells continuously; the pure drug-fiber sheets were strongly cytotoxic. We conclude that (a) electrospinning is a reliable fabrication method for M-loaded PPC fibers; and (b) an ALG coating reduces the initial burst of the fiber sheets.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Alkylating / administration & dosage*
  • Antineoplastic Agents, Alkylating / pharmacokinetics*
  • Antineoplastic Agents, Alkylating / therapeutic use
  • Calorimetry, Differential Scanning
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Dacarbazine / administration & dosage
  • Dacarbazine / analogs & derivatives*
  • Dacarbazine / pharmacokinetics
  • Dacarbazine / therapeutic use
  • Drug Delivery Systems
  • Excipients
  • Glioma / metabolism*
  • Humans
  • Microscopy, Electron, Scanning
  • Particle Size
  • Polypropylenes
  • Temozolomide
  • Tetrazolium Salts
  • Thiazoles

Substances

  • Antineoplastic Agents, Alkylating
  • Excipients
  • Polypropylenes
  • Tetrazolium Salts
  • Thiazoles
  • polypropylene carbonate
  • Dacarbazine
  • thiazolyl blue
  • Temozolomide