In Vitro and In Vivo Scalp Retention and Penetration of 99mTc-Minoxidil Solution

Abstract

The present study assessed the effect of retention on ex vivo skin and in vivo scalp penetration of radiolabeled minoxidil formulations (5% w/v). Minoxidil was radiolabeled with technetium (99mTc) with an efficiency of 99.1% using 0.2% stannous chloride as reducing agent at pH 6 and incubation temperature of 40 °C. Three different 99mTc-minoxidil formulations were prepared using aqueous ethanolic solution as vehicle. Formulation A contains 99mTc-minoxidil dissolved in vehicle, formulation B contains 10% propylene glycol (PG) and formulation C contains 10% hydroxypropyl cellulose (HPC), in addition. Results showed that addition of HPC resulted in enhanced viscosity (400 mPa.s) and significantly higher ex vivo retention (p < 0.05) and permeation (0.75±0.12%, 8 h). PG does not improve the permeation and the results (0.44±0.05%, 8 h) were not significantly different from vehicle alone (0.40±0.05%, 8 h). The results of the in vivo human scalp studies corroborated with the ex vivo results and addition of hydroxypropyl cellulose (HPH) showed significantly higher (p < 0.05) scalp retention. Post 8 h application, scalp penetration in group treated with formulation C was nearly 2.8-fold and 2.2-fold higher than those treated with formulation A and B, respectively. Further, absence of minoxidil in systemic circulation during study duration indicates safety. In conclusion, our results showed that increasing contact time of minoxidil with scalp by modifying viscosity results in reduced frequency of application and improved efficacy.