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PLGA encapsulated γ-cyclodextrin-meropenem inclusion complex formulation for oral delivery

Aun Raza1, Jared A Miles2, Fekade Bruck Sime1

  • 1School of Pharmacy, The University of Queensland, Woolloongabba 4102, Australia; Centre for Translational Anti-infective Pharmacodynamics, School of Pharmacy, The University of Queensland, Woolloongabba 4102, QLD, Australia.

International Journal of Pharmaceutics
|February 4, 2021
PubMed

Insights

This study developed novel meropenem-loaded nanoparticles using gamma-cyclodextrin and PLGA to enhance antibiotic stability and delivery. The new system protects meropenem from degradation, improving its effectiveness against resistant bacteria.

Area of Science:

  • Biomaterials Science
  • Pharmaceutical Sciences
  • Nanotechnology

Background:

  • Meropenem (MER) is a critical antibiotic for resistant bacterial infections.
  • Clinical use of MER is limited by its instability in aqueous solutions and gastric environments, and short plasma half-life.
  • Novel drug delivery systems are needed to overcome MER's limitations.

Purpose of the Study:

  • To develop a multi-material delivery system for meropenem (MER) using gamma-cyclodextrin (γ-CD) and poly lactic-co-glycolic acid (PLGA).
  • To enhance MER's stability, control its release, and maintain its antibacterial activity.
  • To overcome challenges associated with MER's chemical instability and short plasma half-life.

Main Methods:

  • Formation of MER-γ-CD inclusion complex using a liquid CO2 method.
  • Encapsulation of MER-γ-CD into PLGA nanoparticles (MER-γ-CD NPs) via double emulsion solvent evaporation.
  • Characterization of inclusion complex and nanoparticles using FTIR, XRD, DSC, SEM, 1H NMR, and DLS.
  • In vitro release studies and apparent permeability coefficient (Papp) measurements.
  • Assessment of antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa.

Main Results:

  • Successful formation of MER-γ-CD inclusion complex and MER-γ-CD NPs confirmed by multiple characterization techniques.
  • Drug loading and entrapment efficiency for MER-γ-CD were 21.9% and 92.2%, respectively; for MER-γ-CD NPs, they were 3.6% and 42.1%.
  • In vitro release showed controlled release of MER from NPs, with 23.6% active drug released in 8 hours.
  • Apparent permeability coefficients indicated no significant negative impact of the delivery system on drug transport.
  • MER-γ-CD NPs retained significant antibacterial activity against S. aureus and P. aeruginosa.

Conclusions:

  • The developed MER-γ-CD NPs effectively protect meropenem from degradation by gastric pH.
  • The nanoparticle system offers controlled drug release, potentially improving therapeutic outcomes.
  • MER-γ-CD NPs maintain the essential antibacterial efficacy of meropenem, presenting a promising strategy for treating resistant infections.
Keywords:
CyclodextrinsLiquid CO(2)MeropenemOral antibioticsOral drug deliveryPLGA nanoparticles

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