In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus

Ther Deliv. 2016;7(5):305-18. doi: 10.4155/tde-2015-0004.

Abstract

Background: The study aimed at in vivo pharmacokinetic evaluation of carvedilol loaded nanocapsules (CLN) followed by in silico predictions and establishment of IVIVC.

Method: LC/MS-MS method was developed and validated to estimate the pharmacokinetic profile of CLN. The in silico and IVIVC were established using GastroPlus.

Results: The CLN demonstrated 221.09% increase in bioavailability of carvedilol over aqueous suspension. The simulation of plasma concentration profile of CLN exhibited a sensible level of superimposition. The regional absorption of the CLN showed maximum absorption from duodenum and jejunum. The Wagner-Nelson method was found to be most suitable deconvolution method for establishing the IVIVC of CLN.

Conclusion: The study demonstrated CLN as efficient delivery system to ferry carvedilol with improved bioavailability.

Keywords: GastroPlus™; IVIVC; LC/MS-MS; Wagner–Nelson Method; carvedilol nanocapsules; in silico studies.

MeSH terms

  • Animals
  • Biological Availability
  • Carbazoles / pharmacokinetics*
  • Carvedilol
  • Computer Simulation*
  • Drug Delivery Systems / methods*
  • Male
  • Nanocapsules*
  • Propanolamines / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Carbazoles
  • Nanocapsules
  • Propanolamines
  • Carvedilol