Ion Pairs of Risedronate for Transdermal Delivery and Enhanced Permeation Rate on Hairless Mouse Skin
October 2011
in “
International journal of pharmaceutics
”
TLDR Ion-paired risedronate significantly increases skin penetration without irritation compared to risedronate alone.
In the 2011 study, researchers investigated the ability of ion-paired solutions of risedronate (RIS) with l-arginine (ARG), l-lysine (LYS), and diethylenetriamine (DETA) to enhance the transdermal delivery of RIS through hairless mouse skin. The solubility of RIS in xylene increased when paired with ARG, LYS, and DETA, with the highest solubility observed for the RIS-LYS pair at 12.0%. In vitro permeation tests showed that ion-paired RIS penetrated mouse skin approximately 36 times more effectively than RIS alone, with cumulative amounts of 475.18 ± 94.19 μg/cm2 and 511.21 ± 106.52 μg/cm2 for the 1:2 and 1:1 molar ratios, respectively, compared to only 14.13 ± 5.49 μg/cm2 for RIS alone after 24 hours. Additionally, no skin irritation was observed in hairless mice after administration of either RIS alone or ion-paired RIS, indicating the potential for transdermal delivery of RIS using an ion-paired system without adverse skin reactions.
