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Aliskiren Hemifumarate Proliposomes for Improved Oral Drug Delivery: Formulation Development, In Vitro and In Vivo

Priyanka Kunamaneni1, Surya Kovvasu1, Steven Yeung1

  • 1Department of Pharmaceutical Sciences, College of Pharmacy, Western University of Health Sciences, Pomona, CA 91766, USA.

Molecules (Basel, Switzerland)
|August 12, 2022
PubMed
Summary

This study developed proliposomal formulations for aliskiren hemifumarate (AKH), enhancing its bioavailability. Optimized AKH proliposomes showed a 230% increase in relative bioavailability compared to the pure drug suspension.

Keywords:
Caco-2PAMPAaliskiren hemifumaratepharmacokinetic studiesproliposomes

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Aliskiren hemifumarate (AKH) exhibits poor oral bioavailability, limiting its therapeutic efficacy.
  • Proliposomal formulations offer a promising strategy to overcome bioavailability challenges for poorly soluble drugs.

Purpose of the Study:

  • To develop and characterize proliposomal formulations of aliskiren hemifumarate (AKH).
  • To evaluate the in vitro and in vivo performance of AKH proliposomes to enhance drug absorption.

Main Methods:

  • Proliposomes were prepared using a solvent evaporation method with lipids including soy phosphatidylcholine (SPC), dimyristoylphosphatidylcholine (DMPC), dimyristoylphosphatidylglycerol sodium (DMPG Na), stearylamine, and cholesterol.
  • Formulations were assessed for particle size, zeta potential, in vitro drug release, and in vitro permeability using PAMPA and Caco-2 cell models.
  • In vivo pharmacokinetic studies were conducted in Sprague-Dawley rats to determine relative bioavailability.

Main Results:

  • An optimized proliposome formulation (drug/DMPC/cholesterol/stearylamine at 1:5:0.025:0.050 w/w/w/w) exhibited desirable particle size, high zeta potential, and high encapsulation efficiency.
  • Proliposomal AKH demonstrated significantly enhanced in vitro permeability compared to pure AKH.
  • In vivo studies revealed a 230% relative bioavailability for the optimized AKH proliposome formulation compared to pure AKH suspension.

Conclusions:

  • Proliposomal formulation significantly improves the absorption rate and extent of aliskiren hemifumarate.
  • The developed proliposomes represent an effective drug delivery system for enhancing the oral bioavailability of poorly bioavailable drugs like AKH.