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      Finasteride nano-transferosomal gel formula for management of androgenetic alopecia: ex vivo investigational approach

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          Finasteride (FIN) is known as type II 5α-reductase inhibitor, which has been approved for the treatment and prevention of androgenetic alopecia. Administration of FIN by oral route has led to undesirable systemic side effects that include mood disturbance, gynecomastia, decreased libido, erectile dysfunction, and ejaculation disorder. The aim was to improve FIN delivery through skin layers and hair follicles that could possibly reduce its major side effects resulting from long-term oral administration for the treatment and prevention of male pattern baldness.

          Materials and methods

          FIN was formulated as nano-transferosomal (NTF) gel formulations (F1–3). The prepared formulations were characterized for encapsulation efficiency, particle size, ex vivo skin permeation, and kinetic modeling. In addition, visualization of NTF skin penetration using a fluorescence laser microscope was carried out for the selected formula (F2).

          Results and discussion

          The results showed that FIN encapsulation efficiency percentage was 69.72 ± 8.36, 89.43 ± 6.82, and 93.1 ± 1.93 for F1, F2, and F3, respectively. FIN-NTF average vesicle sizes were 299.6 ± 45.6, 171 ± 25.6, and 197.4 ± 29.1 nm for F1, F2, and F3, respectively. FIN-NTF formulations (F1–3) showed enhancement and improvement in the amount of FIN permeated compared with raw FIN gel formula. The NTF formula revealed uniform fluorescence (rhodamine) intensity across rat skin, which indicated improved delivery through skin layers compared with control gel formula.


          These results indicated that NTF gel formula showed the ability to boost FIN delivery across skin layers and could be applied as an alternative for oral therapy.

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          Most cited references 28

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          Role of edge activators and surface charge in developing ultradeformable vesicles with enhanced skin delivery.

          Transfersomes are highly efficient edge activator (EA)-based ultraflexible vesicles capable of, non-invasively, trespassing skin by virtue of their high, self-optimizing deformability. This investigation presents different approaches for the optimization of Transfersomes for enhanced transepidermal delivery of Diclofenac sodium (DS). Different methods of preparation, drug and lipid concentrations and vesicle compositions were employed, resulting in ultraflexible vesicles with diverse membrane characteristics. Evaluation of Transfersomes was implemented in terms of their shapes, sizes, entrapment efficiencies (EE%), relative deformabilities and in vitro skin permeation. Transfersomes prepared with 95:5% (w/w) (PC:EA) ratio showed highest EE% (Span 85>Span 80>Na cholate>Na deoxycholate>Tween 80). Whereas, those prepared using 85:15% (w/w) ratio showed highest deformability (Tween 80 was superior to bile salts and spans). Transfersomes were proved significantly superior in terms of, the amount of drug deposited in the skin and the amount permeated, with an enhancement ratio of 2.45, when compared to a marketed product. The study proved that the type and concentration of EA, as well as, the method of preparation had great influences on the properties of Transfersomes. Hence, optimized Transfersomes can significantly increase transepidermal flux and prolong the release of DS, when applied non-occlusively. Copyright 2010 Elsevier B.V. All rights reserved.
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            New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers, Transfersomes.

             G Cevc,  G Blume (2001)
            Transfenac, a lotion-like formulation of diclofenac, is described. It consists of pharmaceutically acceptable ingredients and mediates the agent transport through intact skin and into the target tissues. Therapeutically meaningful drug concentrations in the target tissue are reached even when the administered drug dose in Transfenac is below 0.5 mg/kg body weight. Ultradeformable agent carriers, called Transfersomes, form the basis of Transfenac. These Transfersomes are proposed to cross the skin spontaneously under the influence of transepidermal water activity gradient (see [Biochim. Biophys. Acta 1104 (1992) 226]). Diclofenac association with ultradeformable carriers permits it to have a longer effect and to reach 10-times higher concentrations in the tissues under the skin in comparison with the drug from a commercial hydrogel. For example, Transfenac achieves intramuscular agent concentrations between 0.5 and 2 microg/g and 2 and 20 microg/g at t=12 h, depending on the tissue depth, when it is administered in the dose range 0.25-2 mg/kg of rat body weight. A much higher drug concentration in a hydrogel (1.25-10 mg/kg body weight) creates the drug level of only <0.5 microg/g in the muscle. The drug concentration in the rat patella for these two types of formulation is between 1 microg/g and 5 microg/g or 0.4 microg/g, respectively. The relative advantage of diclofenac delivery by means of ultradeformable carriers increases with the treated muscle thickness and with decreasing drug dose, as seen in mice, rats and pigs; this can be explained by assuming that the drug associated with carriers is cleared less efficiently by the dermal capillary plexus. In pigs it suffices to use 0.3 mg of diclofenac in highly deformable vesicles per kg body weight, spread over an area of 25 cm(2), to ensure therapeutic drug concentration in a 5-cm thick muscle specimen, collected under the agent application site. When the drug is used in a hydrogel at 8 times higher dose, the average intramuscular concentration is at least three times lower and subtherapeutic. This suggests that diclofenac in Transfersomes has the potential to replace combined oral/topical diclofenac administration in humans.
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              Liposomes--a selective drug delivery system for the topical route of administration. Lotion dosage form.


                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                23 July 2018
                : 12
                : 2259-2265
                [1 ]Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia, oaahmed@ 123456kau.edu.sa
                [2 ]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt, oaahmed@ 123456kau.edu.sa
                Author notes
                Correspondence: Osama AA Ahmed, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, PO Box 80260, Jeddah 21589, Saudi Arabia, Email oaahmed@ 123456kau.edu.sa
                © 2018 Ahmed and Rizq. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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