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Sustained-release amorphous solid dispersions.

Julien Maincent1, Robert O Williams2

  • 1Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, A1920, Austin, TX, 78712, USA.

Drug Delivery and Translational Research
|March 3, 2018
PubMed
Summary
This summary is machine-generated.

Amorphous solid dispersions (ASDs) offer improved drug solubility but face stability challenges. This review explores manufacturing sustained-release ASDs, detailing formulation approaches and their inherent difficulties.

Keywords:
Amorphous solid dispersionsControlled releaseSupersaturationSustained release

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Area of Science:

  • Pharmaceutical Science
  • Drug Delivery Systems
  • Materials Science

Background:

  • Amorphous solid dispersions (ASDs) are increasingly utilized to enhance the solubility of poorly soluble drugs.
  • The thermodynamic instability of ASDs leads to drug recrystallization, posing formulation challenges.
  • Most research has focused on immediate-release ASDs, with sustained-release formulations being a recent area of investigation.

Purpose of the Study:

  • To review the challenges associated with manufacturing sustained-release amorphous solid dispersions (ASDs).
  • To discuss various formulation approaches investigated for sustained-release ASDs.
  • To analyze the advantages and disadvantages of different polymer and lipid-based systems.

Main Methods:

  • Literature review of research on sustained-release ASDs.
  • Analysis of formulation strategies including hydrophilic polymers, hydrophobic polymers, and lipid-based systems.
  • Discussion of challenges such as intramatrix recrystallization, drug-polymer gelling, and dissolution rate limitations.

Main Results:

  • Sustained-release ASDs can reduce administration frequency and toxicity by preventing high drug concentrations.
  • These systems can improve bioavailability by decreasing drug reprecipitation.
  • Key challenges include intramatrix recrystallization, drug release inhibition due to polymer gelling, and low supersaturation from slow dissolution.

Conclusions:

  • Manufacturing sustained-release ASDs presents significant hurdles, including stability and controlled drug release.
  • Hydrophilic polymers, hydrophobic polymers, and lipid-based systems offer distinct advantages and drawbacks for sustained-release ASD formulation.
  • Further research is needed to optimize formulation strategies for effective and stable sustained-release ASDs.