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Parenteral drug delivery systems play a crucial role in modern therapeutics by enabling the direct administration of drugs into the systemic circulation, bypassing the gastrointestinal tract. These systems are particularly valuable for poorly absorbed oral medications that are unstable in the digestive environment or require rapid onset or sustained therapeutic levels. Delivery is achieved through intravenous, intramuscular, or subcutaneous routes, each selected based on the drug's properties...
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Intra-lymph Node Injection of Biodegradable Polymer Particles
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Injectable controlled release depots for large molecules.

Steven P Schwendeman1, Ronak B Shah2, Brittany A Bailey2

  • 1Department of Pharmaceutical Sciences, The Biointerfaces Institute, North Campus Research Complex, University of Michigan, 2800 Plymouth Road, Ann Arbor, MI 48109, USA; Department of Biomedical Engineering, The Biointerfaces Institute, North Campus Research Complex, University of Michigan, 2800 Plymouth Road, Ann Arbor, MI 48109, USA.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|June 15, 2014
PubMed
Summary
This summary is machine-generated.

Injectable biodegradable depots using poly(lactic-co-glycolic acid) (PLGA) enable long-term drug release, but face challenges for protein delivery. This review explores overcoming these barriers for advanced long-acting-release (LAR) products.

Keywords:
BiodegradableControlled releaseDepotPLGAPeptideProtein

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Area of Science:

  • Biomaterials Science
  • Pharmaceutical Technology
  • Drug Delivery Systems

Background:

  • Injectable biodegradable depots, primarily using poly(lactic-co-glycolic acid) (PLGA), are established for controlled long-term drug release.
  • Current successes are mainly with small molecules and peptides, offering significant therapeutic improvements like reduced injection frequency.
  • PLGA is a biocompatible, FDA-approved synthetic polymer widely used in medical devices and parenteral long-acting-release (LAR) products.

Purpose of the Study:

  • To review key concepts in developing injectable PLGA controlled-release depots for peptides and proteins.
  • To identify critical barriers hindering the broader application of PLGA depots for large molecular drugs.
  • To examine strategies, including those from the authors' laboratory, for overcoming these limitations in commercial LAR development.

Main Methods:

  • Review of existing literature on PLGA depot formulation and drug release mechanisms.
  • Analysis of challenges associated with encapsulating and delivering peptides and proteins from PLGA matrices.
  • Discussion of innovative approaches to enhance stability and controlled release of biologics from PLGA depots.

Main Results:

  • PLGA depots have demonstrated significant advancements in controlled release for certain drug classes.
  • Key challenges for peptide and protein delivery include drug degradation, burst release, and low encapsulation efficiency.
  • Novel formulation strategies are being developed to improve the compatibility and release kinetics of biologics from PLGA depots.

Conclusions:

  • PLGA depots represent a promising platform for long-acting injectable drug delivery.
  • Addressing the specific challenges of peptide and protein delivery is crucial for expanding the utility of PLGA LAR products.
  • Continued research and development of advanced formulation techniques are essential for the commercial success of biologic-loaded PLGA depots.