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Poly(ortho esters)--from concept to reality.

Jorge Heller1, John Barr

  • 1AP Pharma, 123 Saginaw Drive, Redwood City, California 94063, USA. jorgeheller2@aol.com

Biomacromolecules
|September 14, 2004
PubMed
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Poly(ortho esters) are advanced polymers with tunable properties for controlled drug delivery. New formulations with latent acid segments offer precise erosion control for solid and gel-based systems.

Area of Science:

  • Polymer Chemistry
  • Biomaterials Science
  • Drug Delivery Systems

Background:

  • Poly(ortho esters) (POEs) have been developed since the 1970s, with four main families identified.
  • Two primary synthesis methods exist: transesterification and the addition of polyols to diketene acetals, with the latter being preferred.
  • Recent advancements include incorporating latent acid segments into the polymer backbone for controlled erosion.

Purpose of the Study:

  • To explore the synthesis and properties of novel poly(ortho esters).
  • To demonstrate the controlled release of various drugs from different polymer formulations.
  • To present preclinical toxicology data for a promising drug delivery system.

Main Methods:

  • Synthesis of poly(ortho esters) via the addition of polyols to diketene acetals.

Related Experiment Videos

  • Modification of polymer backbone with latent acid segments to control erosion rates.
  • Formulation of solid and gel-like polymers for drug encapsulation and release studies.

    • Main Results:

    • Polymers with varying chain flexibility were produced, ranging from brittle solids to gel-like materials.
    • Controlled release of 5-fluorouracil and bovine serum albumin from solid POEs was demonstrated.
    • Mepivacaine release from gel-like POEs was studied, showing potential for post-operative pain treatment.

    Conclusions:

    • Poly(ortho esters) offer versatile platforms for controlled drug delivery due to tunable erosion rates.
    • The incorporation of latent acid segments significantly enhances control over polymer degradation.
    • Further development of these POE systems, including preclinical toxicology, shows promise for clinical applications.