Lira Ana Amélia M, Sester Elizângela A, Carvalho André Luis M, Strattmann Ruth R, Albuquerque Miracy M, Wanderley Almir G, Santana Davi P
NUDFAC, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, Pernambuco, Brazil.
AAPS PharmSciTech. 2008;9(1):163-8. doi: 10.1208/s12249-007-9002-z. Epub 2008 Jan 25.
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.
本研究旨在开发一种从多种紫葳科植物中分离得到的化合物拉帕醇的局部用制剂，并评估其局部抗炎活性。通过体外释放研究评估了药物剂型和不同类型乳化剂的影响。选择释放速率最高的制剂，并通过皮肤渗透和滞留实验进行评估。观察到与凝胶乳膏制剂相比，凝胶制剂的拉帕醇渗透量和滞留量显著更高（3.9倍）。还评估了最有前景的制剂的抗伤害感受和抗水肿活性。局部使用时，拉帕醇凝胶减少了角叉菜胶注射引起的后爪体积增加，并减轻了乙酸（0.8%水溶液，腹腔注射）产生的伤害感受。这些结果表明，从凝胶制剂局部递送拉帕醇可能是治疗皮肤和皮下损伤的有效药物。
