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      Transfersomes as versatile and flexible nano-vesicular carriers in skin cancer therapy: the state of the art

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          ABSTRACT

          Introduction: The skin acts as a barrier and prevents transcutaneous delivery of therapeutic agents. Transfersomes are novel vesicular systems that are several times more elastic than other vesicular systems. These are composed of edge activator, phospholipids, ethanol, and sodium cholate and are applied in a non-occlusive manner.

          Areas covered: This article covers information such as merits/demerits of transfersomes, regulatory aspects of materials used in preparation, different methods of preparation, mechanism of action, review of clinical investigations performed, marketed preparations available, research reports, and patent reports related to transfersomes.

          Expert opinion: Research over the past few years has provided a better understanding of transfersomal permeation of therapeutic agents across stratum corneum barrier. Transfersomes provides an essential feature of their application to variety of compositions in order to optimize the permeability of a range of therapeutic molecules. This is evidenced by the fact that there are several Transfersome products being processed in advanced clinical trials. It is noteworthy that a number of Transfersome products for dermal and transdermal delivery will gain a global market success in near future.

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          Most cited references114

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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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            Nonmelanoma skin cancer in the United States: incidence.

            Because death from nonmelanoma skin cancer is uncommon, quantification of its morbidity is particularly important. Although its incidence is increasing rapidly, the most recent nationwide estimates are 16 years old. The purpose of this study was to estimate the 1994 nonmelanoma skin cancer incidence in the United States. We updated the 16-year-old incidence estimates to reflect the growth and changing age distribution of the population and the increases in age-adjusted incidence rates documented in two population-based studies. The projected 1994 incidence of nonmelanoma skin cancer in the United States is 900,000 to 1,200,000 cases, similar in magnitude to the overall incidence of noncutaneous cancers. Nonmelanoma skin cancer imposes an enormous public health burden on the U.S. population. Quantification of its morbidity and its prevention are important priorities.
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              Nanotechnology and the transdermal route: A state of the art review and critical appraisal.

              The skin is refractive to most molecules, especially hydrophilic ones, despite the existence of trans-barrier pathways. It is essential to maintain this protective barrier even after breaching skin surface for purposes of transdermal drug delivery to cope with cutaneous microbiota. Mechanical abraders or local energy dischargers (porators) or else hard, sharp objects (perforators, micro-needles) can punch a limited number (approximately 10(2)cm(-2)) of relatively wide (> or =10(3)nm) openings in the skin barrier, which then lets transiently (approximately 1 day) small drug quantities ( or =10(3)nm) ballistic droplets or particles also insert small drug amounts (approximately 1mg) into the upper skin through the > or =10(6)cm(2) pores they create. The latter "skin breaching" method is approved for use in humans, whereas the hard nano-sized (5 nm-10 microm) skin perforators are still in development for transdermal drug delivery. Alternatively, controlled and reliable drug delivery across skin barrier can be achieved with sufficiently deformable and stable nano-sized carriers. Such "soft" skin penetrators are typically composite colloids. As such they must obtain, or retain, their ability to act as drug carriers on, in, and ideally below skin barrier(s). If properly designed and applied, such self-regulating, ultra-adaptable, and stable hetero-aggregates can open spontaneously and carry drugs through < or =10(9)cm(-2) cutaneous pores in the primary skin barrier and minimise cutaneous drug clearance; this permits deep/targeted deposition and prolonged action of the carrier-transported drugs. Therapeutic products based on ultra-adaptable, self-regulating, nano-sized (approximately 10(2)nm) carriers are under development. The first one is already approved in Switzerland. Copyright 2009. Published by Elsevier B.V.
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                Author and article information

                Journal
                Nano Rev Exp
                Nano Rev Exp
                ZANO
                zano20
                Nano Reviews & Experiments
                Taylor & Francis
                2002-2727
                2017
                07 June 2017
                : 8
                : 1
                : 1325708
                Affiliations
                Pharmaceutics, Guru Ramdas Khasla Institute of Science & Technology, Pharmacy , Jabalpur, India
                Author notes
                CONTACT Gopal Rai drgopalrai78@ 123456gmail.com Pharmaceutics, Guru Ramdas Khasla Institute of Science & Technology, Pharmacy , Kukrikheda, Barela, Jabalpur, MP483001, India
                Author information
                http://orcid.org/0000-0003-0570-5846
                Article
                1325708
                10.1080/20022727.2017.1325708
                6167026
                30410704
                4dc390af-9e46-43a7-aba0-86d4a77bad61
                © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.

                This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial License ( http://creativecommons.org/licenses/by-nc/4.0/), which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : 14 February 2017
                : 28 April 2017
                Page count
                Figures: 2, Tables: 3, References: 128, Pages: 19
                Categories
                Review

                transfersomes,transdermal drug delivery​,phospholipid,actinic keratoses,basal cell carcinoma,squamous cell carcinoma,melanoma,kaposi’s sarcoma

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