Mucoadhesive maleimide-functionalised liposomes for drug delivery to urinary bladder

Eur J Pharm Sci. 2018 Jan 1:111:83-90. doi: 10.1016/j.ejps.2017.09.039. Epub 2017 Sep 27.

Abstract

Intravesical drug administration is used to deliver chemotherapeutic agents via a catheter to treat bladder cancer. The major limitation of this treatment is poor retention of the drug in the bladder due to periodic urine voiding. In this work, maleimide-functionalised PEGylated liposomes (PEG-Mal) were explored as mucoadhesive vehicles for drug delivery to the urinary bladder. The retention of these liposomes on freshly excised porcine bladder mucosa in vitro was compared with conventional liposomes, PEGylated liposomes, two controls (dextran and chitosan), and evaluated through Wash Out50 (WO50) values. PEG-Mal liposomes exhibited greater retention on mucosal surfaces compared to other liposomes. The penetration abilities of conventional, PEG-Mal-functionalised and PEGylated liposomal dispersions with encapsulated fluorescein sodium into the bladder mucosa ex vivo were assessed using a fluorescence microscopy technique. PEGylated liposomes were found to be more mucosa-penetrating compared to other liposomes. All liposomes were loaded with fluorescein sodium salt as a model drug and the in vitro release kinetics was evaluated. Longer drug release was observed from PEG-Mal liposomes.

Keywords: Intravesical drug delivery; Liposomes; Mucoadhesion; Mucus penetration; Urinary bladder; Wash out(50) (WO(50)).

MeSH terms

  • Animals
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacokinetics
  • Drug Liberation
  • In Vitro Techniques
  • Liposomes
  • Maleimides / chemistry*
  • Maleimides / pharmacokinetics
  • Particle Size
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / pharmacokinetics
  • Surface Properties
  • Swine
  • Urinary Bladder / metabolism*
  • Urothelium / metabolism*

Substances

  • Drug Carriers
  • Liposomes
  • Maleimides
  • maleimide
  • Polyethylene Glycols