Preparation and clinical evaluation of nano-transferosomes for treatment of erectile dysfunction

Abstract

Maha Fadel M Ali,1 Heba F Salem,2 Hany F Abdelmohsen,3 Sameh K Attia4 1Pharmaceutical Technology Unit, Medical Applications of Lasers Department, National Institute of Laser Enhanced Science, Cairo University, Cairo, Egypt; 2Pharmaceutics and Industrial Pharmacy Department, 3Clinical Pharmacy Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; 4Dermatology and Andrology Department, Faculty of Medicine, Minia University, Minia, Egypt Objective: The goal of the present study was to formulate topical nanocarriers of the low-cost vasodilator, papaverine hydrochloride (PH), as an alternative to the painful penile injections. The injections are used for both diagnosis and treatment of erectile dysfunction. Transdermal nano-transferosome (T), the ultraflexible nanoliposome, was used as a nanocarrier to enhance the penetration of the papaverine to the penis. Methods: Different nano formulas were prepared and characterized for their encapsulation efficiency, particle size, zeta potential, and cumulative drug release. The formula acquired the best characteristics was incorporated into 2% (w/v) hydroxypropyl methylcellulose hydrogel base. The gel containing transferosomal papaverine hydrochloride (PH) and that containing free PH were clinically compared using color flow Doppler measurements. Results: The results revealed that transferosome 3 (T3) had the highest entrapment efficiency approaching 72%, low particle size of 220 nm, and zeta potential of -33.4 mV. The formula released 73% of its initial drug content within 2 hours. The clinical evaluation showed the increase in the cavernous artery diameter from 0.53 mm to 0.78 mm and the increase in the peak systolic flow velocity from 5.95 cm/second to 12.2 cm/second, both of which were found to be significant at P<0.05. Conclusion: It is evident from the study that the transferosomes can be used as a carrier of papaverine hydrochloride for both diagnosis and treatment of the erectile dysfunction. This new strategy could be used successfully in the treatment of erectile dysfunction and in male impotency. Keywords: transferosomes, Color Doppler, transdermal delivery, papaverine hydro­chloride