Development of PEGylated solid lipid nanoparticles of pentoxifylline for their beneficial pharmacological potential in pathological cardiac hypertrophy

Artif Cells Nanomed Biotechnol. 2016 Dec;44(8):1901-1908. doi: 10.3109/21691401.2015.1111234. Epub 2015 Dec 2.

Abstract

Objective: The present study was designed to develop PEGylated solid lipid nanoparticles (SLNs) of pentoxifylline (with increased t½) for the management of cardiac hypertrophy.

Materials and methods: PEGylated SLNs were prepared by melt emulsification method and characterised by zeta potential, polydispersity index, entrapment efficiency, in vitro release and pharmacokinetic profile. Hypertrophy was assessed as increase in tumour necrosis factor-alpha, mean arterial blood pressure, LV protein content and left ventricular end diastolic pressure.

Result: PEGylated SLNs (F19) with increased t½ were developed and characterised. F19 attenuates hypertrophy assessed in terms of parameters employed.

Conclusion: Thus, PEGylated SLNs (F19) of pentoxifylline have enhanced t½ and consequently more significantly preclude cardiac hypertrophy as compared to pentoxifylline.

Keywords: PEGylation; cardiac remodelling; circulation; left ventricle; nanoparticles; pentoxifylline.

MeSH terms

  • Animals
  • Cardiomegaly / drug therapy*
  • Cardiomegaly / metabolism
  • Disease Models, Animal
  • Lipids* / chemistry
  • Lipids* / pharmacokinetics
  • Lipids* / pharmacology
  • Male
  • Nanoparticles / chemistry*
  • Pentoxifylline* / chemistry
  • Pentoxifylline* / pharmacokinetics
  • Pentoxifylline* / pharmacology
  • Polyethylene Glycols* / chemistry
  • Polyethylene Glycols* / pharmacokinetics
  • Polyethylene Glycols* / pharmacology
  • Rats
  • Rats, Wistar

Substances

  • Lipids
  • Polyethylene Glycols
  • Pentoxifylline
  • polyethylene glycol 1000