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Updated: Apr 7, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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Aprepitant loaded solid preconcentrated microemulsion for enhanced bioavailability: A comparison with micronized

Sunil Kamboj1, Radhika Sharma1, Kuldeep Singh1

  • 1Pharmaceutics Division, Dept. of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, India.

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|July 14, 2015
PubMed
Summary

Developing solid preconcentrated microemulsions (S-PCM) significantly enhanced the solubility and permeability of aprepitant (APT). This novel S-PCM formulation offers a superior alternative to traditional micronization for improving oral bioavailability.

Keywords:
Apparent permeabilityOral bioavailabilityPreconcentrated microemulsion (PCM)Simplex lattice designSpray drying

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Formulation Development

Background:

  • Aprepitant (APT) exhibits poor water solubility and moderate permeability, limiting its oral bioavailability.
  • Enhancing solubility and permeability is crucial for improving the therapeutic efficacy of APT.

Purpose of the Study:

  • To improve the solubility and permeability of aprepitant (APT) using a Quality by Design (QbD) approach.
  • To develop and characterize a novel solid preconcentrated microemulsion (S-PCM) formulation for APT.

Main Methods:

  • Employed a Quality by Design (QbD) approach with simplex lattice mixture design to formulate S-PCM.
  • Utilized desirability function for numerical optimization of S-PCM formulations.
  • Characterized formulations using spectral analysis (PXRD, ATR-FTIR, DSC), particle size, zeta potential, PDI, emulsification time, and Transmission Electron Microscopy (TEM).

Main Results:

  • S-PCM formulations confirmed amorphous state of APT with desirable physicochemical properties (droplet size: 150-180 nm, zeta potential: -13 to -15 mV, PDI: 0.211-0.238).
  • Demonstrated 2-fold and 5-fold enhancement in solubility and permeability, respectively, compared to micronized APT.
  • Pharmacokinetic studies in rabbits showed a 1.5-fold increase in bioavailability for S-PCM compared to micronized APT.

Conclusions:

  • The developed S-PCM formulation effectively enhances the solubility, permeability, and oral bioavailability of aprepitant.
  • S-PCM technology presents a promising and potentially superior alternative to conventional micronization for aprepitant formulations.