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. 2008;9(1):163-8.
doi: 10.1208/s12249-007-9002-z. Epub 2008 Jan 25.

Development of lapachol topical formulation: anti-inflammatory study of a selected formulation

Ana Amélia M Lira  1 , Elizângela A Sester, André Luis M Carvalho, Ruth R Strattmann, Miracy M Albuquerque, Almir G Wanderley, Davi P Santana
Affiliations

Development of lapachol topical formulation: anti-inflammatory study of a selected formulation

Ana Amélia M Lira et al. AAPS PharmSciTech. 2008.

Abstract

This study aimed at developing a topical formulation of lapachol, a compound isolated from various Bignoniaceae species and at evaluating its topical anti-inflammatory activity. The influence of the pharmaceutical form and different types of emulsifiers was evaluated by in-vitro release studies. The formulations showing the highest release rate were selected and assessed trough skin permeation and retention experiments. It was observed that the gel formulation provided significantly higher permeation and retained amount (3.9-fold) of lapachol as compared to the gel-cream formulation. Antinociceptive and antiedematogenic activities of the most promising formulation were also evaluated. Lapachol gel reduced the increase in hind-paw volume induced by carrageenan injection and reduced nociception produced by acetic acid (0.8% in water, i.p.) when used topically. These results suggest that topical delivery of lapachol from gel formulations may be an effective medication for both dermal and subdermal injuries.

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Figures

Fig. 1
Fig. 1
Release profiles of the lapachol gel obtained in an earlier study (15)
Fig. 2
Fig. 2
Release profiles of the gel (F3) and gel-cream formulations (F1 and F2)
Fig. 3
Fig. 3
Permeation profiles of lapachol from gel (F3) and gel-cream (F2) formulations
Fig. 4
Fig. 4
Distribution of lapachol in pig-ear skin layers after 24 h (asterisks, stratum corneum)
Fig. 5
Fig. 5
Percentage increase in paw volume in function of time after subplantar injection of carrageenan. Results are the mean ± S.D. for six rats. P < 0.05 as compared with control
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