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Transdermal permeation and biocompatibility studies on gel formulations of benzocaine encapsulated in elastic and conventional liposomes

Grant number: 09/08860-3
Support Opportunities:Scholarships in Brazil - Post-Doctorate
Effective date (Start): September 01, 2009
Effective date (End): August 31, 2012
Field of knowledge:Biological Sciences - Pharmacology - Biochemical and Molecular Pharmacology
Principal Investigator:Eneida de Paula
Grantee:Michelle Franz Montan Braga Leite
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


Topical anesthesia is an essential procedure to reduce both pain and discomfort during diagnosis and dermatologic procedures. Our research group has showed the efficacy of a conventional liposomal gel formulation for the local anesthetics ropivacaine and benzocaine in reducing the pain caused by needle insertion in dental anesthesia at the oral mucosa (Franz-Montan et al, 2007ab). The goal of the present study is to determine the in vitro and in vivo permeation rate of elastic and conventional liposome-encapsulated benzocaine (10%) formulations, as well as its toxicity, evaluated by cultured cells tests and after topical application in rat skin. The elastic vesicles will be prepared according to the technique proposed by Honeywell-Nguyen et al. (2002a). The following formulations will be tested: placebo gel of elastic vesicles; placebo gel of conventional liposomes; conventional liposome-encapsulated 10% benzocaine gel; elastic liposome-encapsulated 10% benzocaine gel, 10% benzocaine gel and commercially available 20% benzocaine gel. The biocompatibility of the topical gel formulations will be tested through analysis of histological changes of dermis and epidermis (leukocytes infiltration and/or presence of necrosis area) after application of the formulations at the rat skin. We intend to test the anesthetic efficacy of these formulations on human volunteers, once positive results were obtained. (AU)

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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)
FRANZ-MONTAN, MICHELLE; BARONI, DANIELA; BRUNETTO, GIOVANA; VIEIRA SOBRAL, VIVIANE ROBERTA; GONCALVES DA SILVA, CAMILA MORAIS; VENANCIO, PAULO; ZAGO, PATRICIA WIZIACK; SAIA CEREDA, CINTIA MARIA; VOLPATO, MARIA CRISTINA; DE ARAUJO, DANIELE RIBEIRO; et al. Liposomal lidocaine gel for topical use at the oral mucosa: characterization, in vitro assays and in vivo anesthetic efficacy in humans. Journal of Liposome Research, v. 25, n. 1, p. 11-19, . (06/00121-9, 09/08860-3, 07/05734-1)
FRANZ-MONTAN, MICHELLE; SAIA CEREDA, CINTIA MARIA; GASPARI, ADELE; GONCALVES DA SILVA, CAMILA MORAIS; DE ARAUJO, DANIELE RIBEIRO; PADULA, CRISTINA; SANTI, PATRIZIA; NARVAES, ELIENE; NOVAES, PEDRO DUARTE; GROPPO, FRANCISCO CARLOS; et al. Liposomal-benzocaine gel formulation: correlation between in vitro assays and in vivo topical anesthesia in volunteers. Journal of Liposome Research, v. 23, n. 1, p. 54-60, . (06/00121-9, 09/08860-3)

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