Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time.
Ropivacaine 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 vesi...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2017-01-01
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| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC5628885?pdf=render |
| _version_ | 1828285940162887680 |
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| author | Camila Morais Gonçalves da Silva Michelle Franz-Montan Cíntia Elisabeth Gomez Limia Lígia Nunes de Morais Ribeiro Mário Antônio Braga Viviane Aparecida Guilherme Camila Batista da Silva Bruna Renata Casadei Cíntia Maria Saia Cereda Eneida de Paula |
| author_facet | Camila Morais Gonçalves da Silva Michelle Franz-Montan Cíntia Elisabeth Gomez Limia Lígia Nunes de Morais Ribeiro Mário Antônio Braga Viviane Aparecida Guilherme Camila Batista da Silva Bruna Renata Casadei Cíntia Maria Saia Cereda Eneida de Paula |
| author_sort | Camila Morais Gonçalves da Silva |
| collection | DOAJ |
| description | Ropivacaine 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. |
| first_indexed | 2024-04-13T09:22:59Z |
| format | Article |
| id | doaj.art-2ca87c0bf1c04cddb29348cebabf6e1a |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-04-13T09:22:59Z |
| publishDate | 2017-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-2ca87c0bf1c04cddb29348cebabf6e1a2022-12-22T02:52:31ZengPublic Library of Science (PLoS)PLoS ONE1932-62032017-01-011210e018582810.1371/journal.pone.0185828Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time.Camila Morais Gonçalves da SilvaMichelle Franz-MontanCíntia Elisabeth Gomez LimiaLígia Nunes de Morais RibeiroMário Antônio BragaViviane Aparecida GuilhermeCamila Batista da SilvaBruna Renata CasadeiCíntia Maria Saia CeredaEneida de PaulaRopivacaine 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.http://europepmc.org/articles/PMC5628885?pdf=render |
| spellingShingle | Camila Morais Gonçalves da Silva Michelle Franz-Montan Cíntia Elisabeth Gomez Limia Lígia Nunes de Morais Ribeiro Mário Antônio Braga Viviane Aparecida Guilherme Camila Batista da Silva Bruna Renata Casadei Cíntia Maria Saia Cereda Eneida de Paula Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. PLoS ONE |
| title | Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. |
| title_full | Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. |
| title_fullStr | Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. |
| title_full_unstemmed | Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. |
| title_short | Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. |
| title_sort | encapsulation of ropivacaine in a combined donor acceptor ionic gradient liposomal system promotes extended anesthesia time |
| url | http://europepmc.org/articles/PMC5628885?pdf=render |
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