• Plos One · Jan 2017

    Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time.

    • da Silva Camila Morais Gonçalves CMG Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas, SP, Brazil., Michelle Franz-Montan, Cíntia Elisabeth Gomez Limia, Lígia Nunes de Morais Ribeiro, Mário Antônio Braga, Viviane Aparecida Guilherme, da Silva Camila Batista CB Department of Physiological Sciences, Piracicaba Dental School, University of Campinas, UNICAMP, Piracicaba, SP, Brazil., Bruna Renata Casadei, Cereda Cíntia Maria Saia CMS Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas, SP, Brazil., and Eneida de Paula.
    • Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas, SP, Brazil.
    • Plos One. 2017 Jan 1; 12 (10): e0185828.

    AbstractRopivacaine is a local anesthetic with similar potency but lower systemic toxicity than bupivacaine, the most commonly used spinal anesthetic. The present study concerns the development of a combined drug delivery system for ropivacaine, comprised of two types of liposomes: donor multivesicular vesicles containing 250 mM (NH4)2SO4 plus the anesthetic, and acceptor large unilamellar vesicles with internal pH of 5.5. Both kinds of liposomes were composed of hydrogenated soy-phosphatidylcholine:cholesterol (2:1 mol%) and were prepared at pH 7.4. Dynamic light scattering, transmission electron microscopy and electron paramagnetic resonance techniques were used to characterize the average particle size, polydispersity, zeta potential, morphology and fluidity of the liposomes. In vitro dialysis experiments showed that the combined liposomal system provided significantly longer (72 h) release of ropivacaine, compared to conventional liposomes (~45 h), or plain ropivacaine (~4 h) (p <0.05). The pre-formulations tested were significantly less toxic to 3T3 cells, with toxicity increasing in the order: combined system < ropivacaine in donor or acceptor liposomes < ropivacaine in conventional liposomes < plain ropivacaine. The combined formulation, containing 2% ropivacaine, increased the anesthesia duration up to 9 h after subcutaneous infiltration in mice. In conclusion, a promising drug delivery system for ropivacaine was described, which can be loaded with large amounts of the anesthetic (2%), with reduced in vitro cytotoxicity and extended anesthesia time.

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