Khaled Mohamed Hosny1,2 
,
Hibah Mubarak Aldawsari1
For correspondence:- Khaled Hosny Email: Elswaify2000@yahoo.com Tel:+966592722634
Received: 18 December 2014 Accepted: 19 March 2015 Published: 26 April 2015
Citation: Hosny KM, Aldawsari HM. Avanafil liposomes as transdermal drug delivery for erectile dysfunction treatment: Preparation, characterization, and in vitro, ex vivo and in vivo studies. Trop J Pharm Res 2015; 14(4):559-565 doi: 10.4314/tjpr.v14i4.1
© 2015 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
Purpose: To formulate avanafil, a recently approved phosphodiesterase-5 enzyme inhibitor, in liposomal form for enhanced transdermal permeation and bioavailability
Methods: 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 I0;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.
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