Heat-treated emulsions with cross-linking bovine serum albumin interfacial films and different dextran surfaces: effect of paclitaxel delivery

J Pharm Sci. 2013 Apr;102(4):1307-17. doi: 10.1002/jps.23468. Epub 2013 Feb 6.

Abstract

In this study, a type of biocompatible and biodegradable oil-in-water emulsion for hydrophobic drug delivery was evaluated in vitro and in vivo. Bovine serum albumin (BSA)-dextran conjugates with different dextran molecular weights and different conjugation degrees were used as the emulsifier and stabilizer. Paclitaxel (PTX), a hydrophobic antitumor drug, was effectively loaded inside the oil droplets via high-pressure homogenization. The emulsions were heated at 90°C for 1 h to eliminate the anaphylaxis of BSA. By virtue of the cross-linked BSA films at the oil-water interfaces produced by the heat treatment and the hydrophilic dextran surfaces, the emulsions are stable in blood serum, as well as stable against long-term storage. In vitro cytotoxicity study verifies that the unloaded emulsions are biocompatible and the PTX-loaded emulsions have similar antitumor activity as PTX solution. In vivo investigation of murine ascites hepatoma H22-tumor-bearing mice demonstrates that the PTX-loaded emulsion with shorter and denser dextran surface has better tumor inhibition and survivability efficacy than the commercial PTX injection.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Antineoplastic Agents, Phytogenic / therapeutic use
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / pathology
  • Cattle
  • Cell Survival / drug effects
  • Dextrans / chemistry*
  • Drug Carriers / chemistry*
  • Emulsions / chemistry
  • Hot Temperature
  • Humans
  • KB Cells
  • Liver / drug effects
  • Liver / pathology
  • Liver Neoplasms / drug therapy*
  • Liver Neoplasms / pathology
  • Male
  • Mice
  • Mice, Inbred ICR
  • Paclitaxel / administration & dosage*
  • Paclitaxel / pharmacology
  • Paclitaxel / therapeutic use
  • Serum Albumin, Bovine / chemistry*

Substances

  • Antineoplastic Agents, Phytogenic
  • Dextrans
  • Drug Carriers
  • Emulsions
  • Serum Albumin, Bovine
  • Paclitaxel