Summary
The inclusion complexes of 4-biphenylylacetic acid (BPAA), an anti-inflammatory agent with β-cyclodextrin (β-CyD), heptakis (2,6-di-O-methyl)-β-CyD (DM-β-CyD), and 2-hydroxypropyl-β-CyD (HP-β-CyD) in a molar ratio of 1: 1 were prepared and their topical availabilities in the hydrophilic ointment were evaluated in rats. The in vitro release of BPAA from the ointment base was remarkably enhanced by the complexations with β-CyDs in the order of β- < DM-β- ≈ HP-β-CyD. The in vivo percutaneous absorption studies in rats revealed that the greater release of BPAA from the vehicle obtained by β-CyDs not only compensates for negative effects of β-CyDs on the skin permeation of BPAA, but also delivers BPAA more effectively to the site of action. Furthermore, β-CyDs enhanced the anti-inflammatory effect of BPAA in the ointment on the acute paws oedema induced by carrageenan in rats; the enhancing efficacy of β-CyDs was in the order of β- < DM-β- < HP-β-CyD. The present data suggest that HP-β-CyD is particularly useful in improving the topical availability of BPAA in the ointment formulation tested.
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Arima, H., Adachi, H., Irie, T. et al. Improved Drug Delivery Through the Skin by Hydrophilic β-Cyclodextrins. Drug Invest. 2, 155–161 (1990). https://doi.org/10.1007/BF03259189
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DOI: https://doi.org/10.1007/BF03259189