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Liposome-based drug delivery systems for ropivacaine encapsulated by remote (pH and ion gradient) loading.

Grant number: 11/21735-3
Support Opportunities:Scholarships in Brazil - Doctorate
Effective date (Start): March 01, 2012
Effective date (End): January 31, 2015
Field of knowledge:Biological Sciences - Pharmacology - Biochemical and Molecular Pharmacology
Principal Investigator:Eneida de Paula
Grantee:Camila Morais Gonçalves da Silva
Host Institution: Instituto de Biologia (IB). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
Associated research grant:06/00121-9 - New formulations for the controlled release of local anesthetics in dentistry: from development to clinical tests, AP.TEM


Ropivacaine (RVC), an amino-amide local anesthetic (LA), has been increasingly used in clinical practice since 1985, withlower toxicity than bupivacaine (BVC), the drug of choice for surgical procedures. In the main line of investigation of our research group (Biomembranes, Biochemistry department, IB/Unicamp)i.e, preparation of sustained release systems for local anesthetics, this project intends to improve encapsulation, to prolong anesthesia time and to reduce the toxicity of ropivacaine, using liposomes with internal-external transmembrane gradient as well as a combination of (donor/acceptor) liposomes It should be noted that our group has been working in the development of new pharmaceutical forms for RVC in carriers such as PLGA nanospheres (Moraes et al. Intl. J. Pharm. 331:99, 2007), egg phosphatidylcholine/cholesterol liposomes (de Araújo et al., J. Pharm. Pharmacol., 60:1, 2008) and beta-cyclodextrins (de Araújo et al. Quim. Nova 31:1775, 2008) with promising results regarding the anesthesia effect, in animal models. In this study, liposomes prepared with ion gradients or in combination (donor/acceptor), will be tested in vitro and in vivo, and their effectiveness will be compared to the commercial RVC formulations currently available. Through a simple, inexpensive and innovative process, we intend to increase the loading of RVC into the liposomes, to extend anesthesia time and to reduce the toxicity of ropivacaine, aiming the clinical treatment of pain (in surgical and post-operative procedures) with a possible technological product.

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
GONCALVES DA SILVA, CAMILA MORAIS; FRANZ-MONTAN, MICHELLE; GOMEZ LIMIA, CINTIA ELISABETH; DE MORAIS RIBEIRO, LIGIA NUNES; BRAGA, MARIO ANTONIO; GUILHERME, VIVIANE APARECIDA; DA SILVA, CAMILA BATISTA; CASADEI, BRUNA RENATA; SAIA CEREDA, CINTIA MARIA; DE PAULA, ENEIDA. Encapsulation of ropivacaine in a combined (donor-acceptor, ionic-gradient) liposomal system promotes extended anesthesia time. PLoS One, v. 12, n. 10, . (11/21735-3, 14/14457-5)
GONCALVES DA SILVA, CAMILA MORAIS; FRACETO, LEONARDO FERNANDES; FRANZ-MONTAN, MICHELLE; COUTO, VERONICA MUNIZ; CASADEI, BRUNA RENATA; SAIA CEREDA, CINTIA MARIA; DE PAULA, ENEIDA. Development of egg PC/cholesterol/alpha-tocopherol liposomes with ionic gradients to deliver ropivacaine. Journal of Liposome Research, v. 26, n. 1, p. 1-10, . (11/21735-3)
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
SILVA, Camila Morais Gonçalves da. Liposome-based drug delivery systems for ropivacaine encapsulated by remote (ion gradient) loading. 2015. Doctoral Thesis - Universidade Estadual de Campinas (UNICAMP). Instituto de Biologia Campinas, SP.

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