Pharmaceutical Research

, Volume 33, Issue 3, pp 729–738 | Cite as

Local, Controlled Delivery of Local Anesthetics In Vivo from Polymer - Xerogel Composites

  • Haibo Qu
  • Marius C. Costache
  • Saadet Inan
  • Alan Cowan
  • David Devore
  • Paul Ducheyne
Research Paper



Polymer-xerogel composite materials have been introduced to better optimize local anesthetics release kinetics for the pain management. In a previous study, it was shown that by adjusting various compositional and nano-structural properties of both inorganic xerogels and polymers, zero-order release kinetics over 7 days can be achieved in vitro. In this study, in vitro release properties are confirmed in vivo using a model that tests for actual functionality of the released local anesthetics.


Composite materials made with tyrosine-polyethylene glycol(PEG)-derived poly(ether carbonate) copolymers and silica-based sol–gel (xerogel) were synthesized. The in vivo release from the composite controlled release materials was demonstrated by local anesthetics delivery in a rat incisional pain model.


The tactile allodynia resulting from incision was significantly attenuated in rats receiving drug-containing composites compared with the control and sham groups for the duration during which natural healing had not yet taken place. The concentration of drug (bupivacaine) in blood is dose dependent and maintained stable up to 120 h post-surgery, the longest time point measured.


These in vivo studies show that polymer-xerogel composite materials with controlled release properties represent a promising class of controlled release materials for pain management.


composite controlled release local anesthetic sol–gel 



Analysis of variance BP bupivacaine


De-ionized water


Desaminotyrosyl tyrosine octyl ester


Fourier transform infrared spectroscopy


Gel permeation chromatography


Hydrochloride acid


High performance liquid chromatography




Nuclear magnetic resonance


Polyethylene glycol






Trifluoroacetic acid


Acknowledgments and Disclosures

This work was supported by U.S. Army contract #W81XWH-07-1-0438. The U.S. Army Medical Research Acquisition Activity, 820 Chandler Street, Fort Detrick MD 21702–5014 is the awarding and administering acquisition office. The content of the manuscript does not necessarily reflect the position or the policy of the Government, and no official endorsement should be inferred.


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Haibo Qu
    • 1
  • Marius C. Costache
    • 2
  • Saadet Inan
    • 3
  • Alan Cowan
    • 3
  • David Devore
    • 4
  • Paul Ducheyne
    • 1
  1. 1.Center for Bioactive Materials and Tissue Engineering, Department of BioengineeringUniversity of PennsylvaniaPhiladelphiaUSA
  2. 2.New Jersey Center for Biomaterials, RutgersThe State University of New JerseyPiscatawayUSA
  3. 3.Department of PharmacologyTemple UniversityPhiladelphiaUSA
  4. 4.U.S. Army Institute of Surgical ResearchFort Sam HoustonUSA

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