Transdermal delivery of butamben using elastic and conventional liposomes

Author(s)

Saia Cereda, Cintia Maria ^[1] ; Franz-Montan, Michelle ^[1] ; Goncalves da Silva, Camila Morais ^[1] ; Casadei, Bruna Renata ^[1] ; Domingues, Cleyton Crepaldi ^[1] ; Tofoli, Giovana Radomille ^[2] ; de Araujo, Daniele Ribeiro ^[3] ; de Paula, Eneida ^[1]

Affiliation

^[1] State Univ Campinas UNICAMP, Inst Biol, Dept Biochem, BR-13083862 Campinas, SP - Brazil

^[2] Univ Sao Francisco, Lab Mol Biol & Pharmacol, BR-12916900 Braganca Paulista, SP - Brazil

^[3] Fed Univ ABC, Human & Nat Sci Ctr, BR-09210170 Santo Andre, SP - Brazil

• Document type: Journal article
• Source: Journal of Liposome Research; v. 23, n. 3, p. 228-234, SEP 2013.
• Web of Science Citations: 17

Abstract

Gel formulations containing the local anesthetic butamben (BTB) encapsulated in either conventional (BTBLUV) or elastic (BTBLUV-EL) liposomes were prepared and characterized, and then evaluated in terms of their skin permeability. Parameters measured included vesicle size and surface charge, BTB fluorescence anisotropy, encapsulation efficiency, partition coefficient and liposomal membrane organization. Encapsulation efficiencies and membrane/water partition coefficients were determined using a phase separation. The partition coefficients of the elastic and conventional formulations were 2025 +/- 234 and 1136 +/- 241, respectively. The sizes of the elastic and conventional liposomes did not change significantly (p>0.05) following incorporation of the anesthetic. As expected, the elastic liposomes presented order parameters that were lower than those of the conventional liposomes, as determined by electron paramagnetic resonance with a 5-stearic acid nitroxide probe incorporated into the bilayer. After 8 h, the fluxes into the receiving solution (mu g/cm(2)/h) were 6.95 +/- 1.60 (10% BTB), 23.17 +/- 6.09 (10% BTBLUV) and 29.93 +/- 6.54 (10% BTBLUV-EL). The corresponding time lags (h) were 1.90 +/- 0.48, 1.23 +/- 0.28 and 1.57 +/- 0.38, respectively. The permeability coefficients (10(-3) cm/h) were 1.02 +/- 0.23, 2.96 +/- 0.77 and 4.14 +/- 0.9, for 10% BTB, 10% BTBLUV and 10% BTBLUV-EL, respectively. The results demonstrate that anesthetic access through the skin can be considerably enhanced using liposomal gel formulations, compared to plain gel formulations. (AU)

• FAPESP's process: 06/00121-9 - New formulations for the controlled release of local anesthetics in dentistry: from development to clinical tests
• Grantee: Eneida de Paula
• Support Opportunities: Research Projects - Thematic Grants