¾ The F-C formulation had the highest retention of betamethasone in the skin and the highest 12-hour and 
24-hour permeation of betamethasone through the skin into the receptor fluid.  

¾ The F-10 formulation had the second highest retention of betamethasone in total skin and relatively low 
permeation of betamethasone into the receptor fluid (Figure 2).  

¾ The F-10 formulation had skin layer betamethasone concentrations of 33 ng, 18 ng, and 14 ng in the 
stratum corneum, epidermis, and dermis, respectively (Figure 1). 

¾ The skin layer concentrations of the F-C formulation were 37 ng, 43 ng, and 34 ng, and those of the F-A 
formulation were 5 ng, 17 ng, and 14 ng in the stratum corneum, epidermis, and dermis (Figure 1).

¾ The formulation with the best balance of penetration, permeation, retention, and low absorption 
(F-10/DFD-01) was selected for additional evaluation.

Permeation analysis of novel steroid vehicles to 
deliver and retain steroid in skin layers associated with psoriasis

Leon Kircik, MD1; Franklin Okumu, PhD2; Sateesh Kandavilli, PhD2
1DermResearch, PLLC, Louisville, KY; 2Promius Pharma, a subsidiary of Dr. Reddy’s Laboratories, Princeton, NJ

Introduction

¾ It is possible to tailor the formulation of topical treatment vehicle to facilitate delivery of active drug to the 
site of skin disease pathology. 

¾ Psoriasis is a condition primarily affecting the epidermal layers of the skin. Developing a vehicle that 
optimizes steroid delivery to the affected psoriatic skin layers, while reducing permeation of the steroid 
into the systemic circulation could be beneficial in the treatment of psoriasis. 

¾ This study was designed to evaluate various vehicle formulations on the penetration and retention of 
betamethasone dipropionate in the skin to identify the formulation with the best balance of penetration 
into the epidermis and low systemic absorption.

Conclusions

¾ The F-10 (DFD-01) formulation containing oleyl alcohol, sorbitan monostearate, polyoxyl 20 cetostearyl 
ether, cetostearyl alcohol, and mineral oil, demonstrated a good balance of betamethasone retention in 
the skin, with low systemic absorption. 

¾ This vehicle is designed to achieve retention of steroid in skin layers to maximize local efficacy while 
minimizing systemic absorption of steroid.

Methods 

Figure 1. Penetration of Total Betamethasones after 24 Hours 

¾ A base vehicle formulation containing water, sorbitan monostearate, polyoxyl 20 cetostearyl ether, 
cetostearyl alcohol, mineral oil, propylparaben, methylparaben, butylated hydroxyl toluene, and 
hydroxyethyl cellulose was developed. 

¾ All formulations contained betamethasone dipropionate, 0.05%. Vehicle formulation variants included 
eladiyl alcohol (F-A), hexanol (F-B), dodecanol (F-C), octadecanol (F-D), docosanol (F-E), or oleyl 
alcohol (F-10).

¾ Test agents were applied to human cadaver skin in static Franz-cell chambers containing receptor fluid 
(4% BSA and 0.01% gentamicin). Permeation of betamethasone into the receptor fluid was measured at 
0, 2, 6, 10, 12 and 24 hours. At 24 hours, the distribution of betamethasone and its metabolites in the 
stratum corneum, epidermis, and dermis was analyzed using LC-MS/MS. 

Financial Support: This study was funded and sponsored by the Dr. Reddy’s Laboratories group of companies.  DRL Publication #   787                                                                                                                          

Results 

Figure 2. Retention of Total Betamethasones after 24 Hours 


	FC17PosterPromiusKircikPermeation.pdf