Abstract
Purpose: To formulate avanafil, a recently approved phosphodiesterase-5 enzyme inhibitor, in liposomal form for enhanced transdermal permeation and bioavailabilityMethods: Two preparation procedures were employed, leading to the formation of multilamellar vesicles (MLVs) and reverse-phase evaporation unilamellar vesicles (ULVs). The effects of the preparation method and lipid content on the encapsulation efficiency and particle size were studied. Studies assessing the stability, in vitro release, ex vivo permeation and in vivo bioavailability were also conducted in rats.Results: The preparation of avanafil liposomes as MLVs, the addition of cholesterol, and the use of more rigid phospholipids all increased the avanafil encapsulation efficiency within the liposomes (95.61 %). The stability studies revealed that the liposomes prepared using phospholipids with higher transition temperatures (dipalmitoyl-L-α-phospatidylcholine) were significantly more stable for a longer period of time after storage at 25 ± 0.5 ˚C and 60 ± 5 % relative humidity for a period of 2 months (p < 0.05). In vivo pharmacokinetic results from rats showed a significant increase in the bioavailability of avanafil from transdermal liposomal formulations of up to 7-fold (p < 0.05) compared to the topical drug suspension.Conclusion: The developed avanafil liposomes represent a promising transdermal drug delivery system for the treatment of erectile dysfunction.Keywords: Avanafil, Liposomes, Entrapment efficiency, Dipalmitoyl-L-α- hospatidylcholine, Erectile dysfunction
Highlights
Avanafil was recently approved by two international pharmaceutical regulating bodies, the United States Food and Drug Administration (USFDA) and the European Medicines Agency (EMA) [1]
Concerning the effects of the cholesterol content on the EE% of avanafil in liposomes, the results showed that the EE% can be increased by increasing the cholesterol (CH) content to a certain limit, above which the EE% decreases when the (CH) concentration increases
The results revealed that the avanafil encapsulation efficiency in the different prepared liposomal formulations varied depending on the method of preparation and the lipid composition used in the prepared liposomes
Summary
Avanafil was recently approved by two international pharmaceutical regulating bodies, the United States Food and Drug Administration (USFDA) and the European Medicines Agency (EMA) [1]. Avanafil is a phosphodiesterase-5 enzyme inhibitor and a second-generation erectile dysfunction medication [2,3]. Avanafil is slightly soluble in ethanol, practically insoluble in water, and soluble in 0.1 mol/L hydrochloric acid, and it undergoes a first pass effect. The utilization of novel delivery systems, including vesicular drug delivery systems such as liposomes, has recently been proposed [7]. These novel systems exhibit superior pharmacological properties [8]. Their activity depends on various factors, including their rigidity, lipid membrane composition, and encapsulation efficiency [9]. The use of vesicular drug delivery systems has been studied for both oral and dermal applications [10]
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