Preparation and Evaluation of Paclitaxel-Loaded PEGylated Niosomes Composed of Sorbitan Esters

Biol Pharm Bull. 2023;46(10):1479-1483. doi: 10.1248/bpb.b23-00188.

Abstract

Niosomes are non-ionic surfactant (NIS)-based bilayer vesicles and, like liposomes, have great potential as drug-delivery systems. Our previous study revealed that polyethylene glycol (PEG) niosomes using different sorbitan ester (Span) surfactants (sorbitan monoester, Span 20, 40, 60, 80; sorbitan triester, Span 65) distributed within tumors similarly to PEG liposomes. The aim of this study was to encapsulate efficiently an anti-cancer drug, paclitaxel (PTX) into Span PEG niosomes, and evaluate PTX release profiles and anti-tumor efficacy of PTX-loaded Span PEG niosomes. Niosome sizes ranged between 100-150 nm, and the PTX encapsulation efficiency was more than 50%. All niosomes examined, in the presence of serum, yielded sustained PTX-release profiles. PTX release at 24 and 48 h from Span 80 PEG niosomes was significantly the highest among the other Span PEG niosomes examined. In C26 tumor-bearing mice, PTX-loaded Span 40 PEG niosomes (the lowest PTX release in vitro) suppressed tumor growth while PTX-loaded Span 80 PEG niosomes (the highest PTX release in vitro) did not. Thus, we succeeded in the control of PTX release from Span PEG niosomes by modifying the component of niosomes, and it influenced the effects of drugs loaded into niosomes. This demonstrates that the excellent NIS physicochemical properties of Spans make them an ideal candidate for anti-cancer drug-carrier niosomes.

Keywords: anti-tumor activity; niosome; paclitaxel; sorbitan ester.

MeSH terms

  • Animals
  • Antineoplastic Agents* / pharmacology
  • Drug Carriers
  • Liposomes* / chemistry
  • Mice
  • Paclitaxel / pharmacology
  • Polyethylene Glycols / chemistry
  • Surface-Active Agents

Substances

  • Liposomes
  • Paclitaxel
  • Polyethylene Glycols
  • Antineoplastic Agents
  • Drug Carriers
  • Surface-Active Agents