Liposomal-benzocaine gel formulation: correlation between in vitro assays and in vivo topical anesthesia in volunteers

References

• Al-Melh, M. A., Andersson, L. (2007). Comparison of topical anesthetics (EMLA/Oraqix vs. benzocaine) on pain experienced during palatal needle injection. Oral Surg Oral Med Oral Pathol Oral Radiol Endod 103:16–20.
   PubMedGoogle Scholar
• Alqareer, A., Alyahya, A., Andersson, L. (2006). The effect of clove and benzocaine versus placebo as topical anesthetics. J Dent 34:747–750.
   PubMed Web of Science ®Google Scholar
• Armfield, J. M., Milgrom, P. (2011). A clinician guide to patients afraid of dental injections and numbness. SAAD Dig 27:33–39.
   PubMedGoogle Scholar
• Basra, S. K., Vives, M. J., Reilly, M. C., Reiter, M. F., Kushins, L. G. (2006). Methemoglobinemia after fiberoptic intubation in a patient with an unstable cervical fracture: a case report. J Spinal Disord Tech 19:302–304.
   PubMedGoogle Scholar
• Bhalla, J., Meechan, J. G., Lawrence, H. P., Grad, H. A., Haas, D. A. (2009). Effect of time on clinical efficacy of topical anesthesia. Anesth Prog 56:36–41.
   PubMedGoogle Scholar
• Binshtok, A. M. (2011). Mechanisms of nociceptive transduction and transmission: a machinery for pain sensation and tools for selective analgesia. Int Rev Neurobiol 97:143–177.
   PubMedGoogle Scholar
• Boogaerts, J., Declercq, A., Lafont, N., Benameur, H., Akodad, E. M., Dupont, J. C., et al. (1993). Toxicity of bupivacaine encapsulated into liposomes and injected intravenously: comparison with plain solutions. Anesth Analg 76:553–555.
   PubMed Web of Science ®Google Scholar
• Boogaerts, J. G., Lafont, N. D., Declercq, A. G., Luo, H. C., Gravet, E. T., Bianchi, J. A., et al. (1994). Epidural administration of liposome-associated bupivacaine for the management of postsurgical pain: a first study. J Clin Anesth 6:315–320.
   PubMed Web of Science ®Google Scholar
• Dahshan, A., Donovan, G. K. (2006). Severe methemoglobinemia complicating topical benzocaine use during endoscopy in a toddler: a case report and review of the literature. Pediatrics 117:806–809.
   Web of Science ®Google Scholar
• de Araujo, D. R., Cereda, C. M., Brunetto, G. B., Vomero, V. U., Pierucci, A., Neto, H. S., et al. (2008). Pharmacological and local toxicity studies of a liposomal formulation for the novel local anaesthetic ropivacaine. J Pharm Pharmacol 60:1449–1457.
   PubMed Web of Science ®Google Scholar
• de Araujo, D. R., Padula, C., Cereda, C. M., Tófoli, G. R., Brito, R. B., de Paula, E., et al. (2010). Bioadhesive films containing benzocaine: correlation between in vitro permeation and in vivo local anesthetic effect. Pharm Res 27:1677–1686.
   PubMed Web of Science ®Google Scholar
• de Melo, N. F., Grillo, R., Guilherme, V. A., de Araujo, D. R., de Paula, E., Rosa, A. H., et al. (2011). Poly(lactide-co-glycolide) nanocapsules containing benzocaine: influence of the composition of the oily nucleus on physico-chemical properties and anesthetic activity. Pharm Res 28:1984–1994.
   PubMed Web of Science ®Google Scholar
• de Paula, E., Schreier, S. (1995). Use of a novel method for determination of partition coefficients to compare the effect of local anesthetics on membrane structure. Biochim Biophys Acta 1240:25–33.
   PubMed Web of Science ®Google Scholar
• de Paula, E., Schreier, S. (1996). Molecular and physicochemical aspects of local anesthetic-membrane interaction. Braz J Med Biol Res 29:877–894.
   PubMed Web of Science ®Google Scholar
• Diaz Del Consuelo, I., Falson, F., Guy, R. H., Jacques, Y. (2005a). Transport of fentanyl through pig buccal and esophageal epithelia in vitro: influence of concentration and vehicle pH. Pharm Res 22:1525–1529.
   PubMed Web of Science ®Google Scholar
• Diaz-Del Consuelo, I., Jacques, Y., Pizzolato, G. P., Guy, R. H., Falson, F. (2005b). Comparison of the lipid composition of porcine buccal and esophageal permeability barriers. Arch Oral Biol 50:981–987.
   PubMed Web of Science ®Google Scholar
• Diaz Del Consuelo, I., Pizzolato, G. P., Falson, F., Guy, R. H., Jacques, Y. (2005c). Evaluation of pig esophageal mucosa as a permeability barrier model for buccal tissue. J Pharm Sci 94:2777–2788.
   PubMed Web of Science ®Google Scholar
• Franz-Montan, M., de Paula, E., Groppo, F., Silva, A., Ranali, J., Volpato, M. (2010a). Liposome-encapsulated ropivacaine for intraoral topical anesthesia. Oral Surg Oral Med Oral Pathol Oral Radiol Endod 110:800–804.
   PubMed Web of Science ®Google Scholar
• Franz-Montan, M., Silva, A. L. R., Cogo, K., Bergamaschi, C., Volpato, M. C., Ranali, J., et al. (2007a). Efficacy of 1% ropivacaine gel for topical anesthesia of human oral mucosa. Quintessence Int 38:601–606.
   PubMedGoogle Scholar
• Franz-Montan, M., Silva, A. L. R., Cogo, K., Bergamaschi, C. D., Volpato, M. C., Ranali, J., et al. (2007b). Liposome-encapsulated ropivacaine for topical anesthesia of human oral mucosa. Anesth Analg 104:1528–1531.
   PubMed Web of Science ®Google Scholar
• Franz-Montan, M., Silva, A. L. R., Fraceto, L. F., Volpato, M. C., de Paula, E., Ranali, J., et al. (2010b). Liposomal encapsulation improves the duration of soft tissue anesthesia but does not induce pulpal anesthesia. J Clin Anesth 22:313–317.
   PubMed Web of Science ®Google Scholar
• Grillo, R., de Melo, N. F. S., de Araújo D. R., de Paula E., Dias Filho N. L., Rosa A. H., et al. (2009). Validation of an HPLC method for quantitative determination of benzocaine in PHBV-microparticles and PLA-nanoparticles. Lat Am J Pharm 28:393–399.
   Web of Science ®Google Scholar
• Hegedus, F., Herb, K. (2005). Benzocaine-induced methemoglobinemia. Anesth Prog 52:136–139.
   PubMedGoogle Scholar
• Jaffery, Z., Ananthasubramaniam, K. (2008). A rare side effect of transesophageal echocardiography: methemoglobinemia from topical benzocaine anesthesia. Eur J Echocardiogr 9:289–290.
   PubMedGoogle Scholar
• Kwok, S., Fischer, J. L., Rogers, J. D. (2008). Benzocaine and lidocaine induced methemoglobinemia after bronchoscopy: a case report. J Med Case Reports 2:16.
   PubMedGoogle Scholar
• López-Pinto, J. M., González-Rodríguez, M. L., Rabasco, A. M. (2005). Effect of cholesterol and ethanol on dermal delivery from DPPC liposomes. Int J Pharm 298:1–12.
   PubMed Web of Science ®Google Scholar
• Maestrelli, F., Capasso, G., González-Rodríguez, M. L., Rabasco, A. M., Ghelardini, C., Mura, P. (2009). Effect of preparation technique on the properties and in vivo efficacy of benzocaine-loaded ethosomes. J Liposome Res 19:253–260.
   PubMed Web of Science ®Google Scholar
• Martin, M. D., Ramsay, D. S., Whitney, C., Fiset, L., Weinstein, P. (1994). Topical anesthesia: differentiating the pharmacological and psychological contributions to efficacy. Anesth Prog 41:40–47.
   PubMedGoogle Scholar
• Meechan, J. G. (2002). Effective topical anesthetic agents and techniques. Dent Clin North Am 46:759–766.
   PubMedGoogle Scholar
• Mohanraj, V. J., Chen, Y. (2006). Nanoparticles—a review. Trop J Pharm Res 5:561–573.
   Google Scholar
• Mura, P., Capasso, G., Maestrelli, F., Furlanetto, S. (2008). Optimization of formulation variables of benzocaine liposomes using experimental design. J Liposome Res 18:113–125.
   PubMed Web of Science ®Google Scholar
• Mura, P., Maestrelli, F., González-Rodríguez, M. L., Michelacci, I., Ghelardini, C., Rabasco, A. M. (2007). Development, characterization and in vivo evaluation of benzocaine-loaded liposomes. Eur J Pharm Biopharm 67:86–95.
   PubMed Web of Science ®Google Scholar
• Nusstein, J. M., Beck, M. (2003). Effectiveness of 20% benzocaine as a topical anesthetic for intraoral injections. Anesth Prog 50:159–163.
   PubMedGoogle Scholar
• Primosch, R. E., Rolland-Asensi, G. (2001). Comparison of topical EMLA 5% oral adhesive to benzocaine 20% on the pain experienced during palatal anesthetic infiltration in children. Pediatr Dent 23:11–14.
   PubMedGoogle Scholar
• Rosa, A. L., Sverzut, C. E., Xavier, S. P., Lavrador, M. A. (1999). Clinical effectiveness of lidocaine and benzocaine for topical anesthesia. Anesth Prog 46:97–99.
   PubMedGoogle Scholar
• Saha, S. A., Kordouni, M. R., Siddiqui, M., Arora, R. R. (2006). Methemoglobinemia-induced cardio-respiratory failure secondary to topical anesthesia. Am J Ther 13:545–549.
   PubMedGoogle Scholar
• Shojaei, A. H. (1998). Buccal mucosa as a route for systemic drug delivery: a review. J Pharm Pharm Sci 1:15–30.
   PubMedGoogle Scholar
• Silva, A. L. R., Franz-Montan, M., Groppo, F. C., Volpato, M. C., Ranali, J., Fraceto, L. F., et al. (2008). Pharmaceutical composition comprising a local anesthetic and a carboxyvinyl polymer. Patent no.: WO/2008/138089.
   Google Scholar
• Squier, C., Brogden, K. (2011). Human oral mucosa: development, structure, and function. West Sussex: UK: Wiley-Blackwell.
   Google Scholar
• Squier, C. A., Kremer, M. J. (2001). Biology of oral mucosa and esophagus. J Natl Cancer Inst Monogr 29:7–15.
   PubMedGoogle Scholar
• Trapp, L., Will, J. (2010). Acquired methemoglobinemia revisited. Dent Clin North Am 54:665–675.
   PubMedGoogle Scholar
• Verma, D. D., Verma, S., Blume, G., Fahr, A. (2003a). Liposomes increase skin penetration of entrapped and non-entrapped hydrophilic substances into human skin: a skin penetration and confocal laser scanning microscopy study. Eur J Pharm Biopharm 55:271–277.
   PubMed Web of Science ®Google Scholar
• Verma, D.D., Verma, S., Blume, G., Fahr, A. (2003b). Particle size of liposomes influences dermal delivery of substances into skin. Int J Pharm 258:141–151.
   PubMed Web of Science ®Google Scholar