Transdermal Delivery of Desmopressin Acetate from Water-in- Oil Nano/submicron Emulsion Systems

Abstract

Desmopressin acetate is a potent synthetic peptide hormone. A more acceptable route of Desmopressin acetate is a potent synthetic peptide hormone. That is administered via parenteral, intranasal, and oral routes. A more acceptable route of administration with potentially good bioavailability could be offered by transdermal delivery. The present work reports on the development of water-in-oil (w/o) microemulsions for the transdermal administration of desmopressin acetate. A water-in-oil nano/submicron emulsions for transdermal administration of desmopressin developed. Its skin penetration profiles determined using Franz-diffusion cell. Pseudo-ternary phase diagrams for emulsion regions constructed. Effects of hydrophilic-lipophilic balance (HLB), ratio of surfactants and co-surfactant mixture to oil phase (Smix/oil), and ratio of surfactants to co-surfactant (S/Cs) on skin flux evaluated. Skin flux was increased when S/Cs and Smix/oil were decreased, and HLB was increased. Optimized formulation was obtained as: HLB=8, S/Cs=3 and Smix/oil=5.4, with average particle size of 69nm. The optimized nano/submicron emulsions increased desmopressin skin flux 4.45 fold relative to drug solution.

Keywords

• desmopressin
• nano/submicron emulsion
• transdermal
• statistical evaluation
• optimization