Potential avoidance of adverse analgesic effects using a biologically "smart" hydrogel capable of controlled bupivacaine release

Francesca Taraballi, Silvia Minardi, Bruna Corradetti, Iman K. Yazdi, Marta A. Balliano, Jeffrey L. Van Eps, Massimo Allegri, Ennio Tasciotti

Research output: Contribution to journalArticlepeer-review

22 Scopus citations


Acute pain remains a tremendous clinical and economic burden, as its prevalence and common narcotic-based treatments are associated with poorer outcomes and higher costs. Multimodal analgesia portends great therapeutic promise, but rarely allows opioid sparing, and new alternatives are necessary. Microparticles (MPs) composed of biodegradable polymers [e.g., poly(lactic-co-glycolic acid) or PLGA] have been applied for controlled drug release and acute pain treatment research. However, foreign particles' presence within inflamed tissue may affect the drug release or targeting, and/or cause a secondary inflammatory reaction. We examined how small alterations in the particulate nature of MPs affect both their uptake into and subsequent activation of macrophages. MPs composed of PLGA and chitosan (PLGA-Chi) loaded with bupivacaine (BP) were engineered at different sizes and their opsonization by J774 macrophages was assessed. Uptake of PLGA-Chi by macrophages was found to be size dependent, but they were not cytotoxic or proinflammatory in effect. Moreover, encapsulation of MPs in a thermoresponsive loading gel (pluronic F-127) effectively prevented opsonization. Finally, MPs displayed sustained, tunable release of BP up to 7 days. These results demonstrate our ability to develop a drug delivery system capable of controlled release of local anesthetics to treat acute/subacute pain while concurrently avoiding enhanced inflammation.

Original languageEnglish (US)
Pages (from-to)3724-3732
Number of pages9
JournalJournal of Pharmaceutical Sciences
Issue number11
StatePublished - Sep 29 2014
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.


  • Biomaterials
  • Controlled release
  • Drug delivery
  • Inflammation
  • Injectables
  • Microparticles
  • Pain


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