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PEGylated Biodegradable Polyesters for PGSS Microparticles Formulation: Processability, Physical and Release

D R Perinelli, M Cespi, G Bonacucina

  • 1Department of Biomolecular Sciences, University of Urbino, Piazza Rinascimento, 6, Urbino (PU) 61029, Italy. luca.casettari@uniurb.it.

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Biodegradable PEGylated di-block copolymers were used with the Particles from Gas Saturated Solution (PGSS) technique to create microparticles. The addition of these copolymers enhanced protein release rates, demonstrating a feasible method for drug delivery applications.

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Area of Science:

  • Biomaterials Engineering
  • Drug Delivery Systems
  • Supercritical Fluid Technology

Background:

  • Particles from Gas Saturated Solution (PGSS) is an emerging technique utilizing supercritical carbon dioxide (scCO2) for microparticle production, suitable for encapsulating sensitive biomolecules.
  • Poly(lactide acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) are common polymers in PGSS, with properties tunable by additives like polyethylene glycol (PEG).

Purpose of the Study:

  • To investigate the impact of biodegradable PEGylated di-block copolymers on microparticle characteristics and drug release using the PGSS method.
  • To evaluate the processability and performance of novel copolymer formulations in scCO2.

Main Methods:

  • Synthesis of mPEG5kDa-P(L)LA and mPEG5kDa-P(L)LGA copolymers with comparable molecular weights.
  • Preparation of microparticles using PGSS with varying copolymer content (9% and 81%).
  • Characterization of particle size, morphology, yield, and in vitro release of bovine serum albumin (BSA) as a model protein.

Main Results:

  • PEGylated copolymers exhibited good processability within the PGSS technique without negatively impacting microparticle physical properties.
  • The concentration of PEGylated copolymers directly influenced the drug release profile, with higher content accelerating BSA release.
  • Microparticle formulations demonstrated controlled release characteristics influenced by copolymer composition.

Conclusions:

  • The PGSS technique is effective for producing microparticles using PEGylated di-block copolymers.
  • Mild operating conditions (low pressure and temperature) are feasible for this PGSS application.
  • The incorporation of PEGylated copolymers offers a viable strategy for modulating drug release kinetics in microparticle-based delivery systems.