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      Sublingual fast dissolving niosomal films for enhanced bioavailability and prolonged effect of metoprolol tartrate

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      Drug Design, Development and Therapy

      Dove Medical Press

      anti-hypertensive, β1- antagonist, pharmacokinetics

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          Abstract

          The aim of the present work was to prepare and evaluate sublingual fast dissolving films containing metoprolol tartrate-loaded niosomes. Niosomes were utilized to allow for prolonged release of the drug, whereas the films were used to increase the drug’s bioavailability via the sublingual route. Niosomes were prepared using span 60 and cholesterol at different drug to surfactant ratios. The niosomes were characterized for size, zeta-potential, and entrapment efficiency. The selected niosomal formulation was incorporated into polymeric films using hydroxypropyl methyl cellulose E15 and methyl cellulose as film-forming polymers and Avicel as superdisintegrant. The physical characteristics (appearance, texture, pH, uniformity of weight and thickness, disintegration time, and palatability) of the prepared films were studied, in addition to evaluating the in vitro drug release, stability, and in vivo pharmacokinetics in rabbits. The release of the drug from the medicated film was fast (99.9% of the drug was released within 30 minutes), while the drug loaded into the niosomes, either incorporated into the film or not, showed only 22.85% drug release within the same time. The selected sublingual film showed significantly higher rate of drug absorption and higher drug plasma levels compared with that of commercial oral tablet. The plasma levels remained detectable for 24 hours following sublingual administration, compared with only 12 hours after administration of the oral tablet. In addition, the absolute bioavailability of the drug (ie, relative to intravenous administration) following sublingual administration was found to be significantly higher (91.06%±13.28%), as compared with that after oral tablet administration (39.37%±11.4%). These results indicate that the fast dissolving niosomal film could be a promising delivery system to enhance the bioavailability and prolong the therapeutic effect of metoprolol tartrate.

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          Most cited references 57

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          Nano-niosomes as nanoscale drug delivery systems: an illustrated review.

          The field of nanochemistry research has shown a great progress in the developing of novel nanocarriers as potential drug delivery systems. Niosome is a class of molecular cluster formed by self-association of non-ionic surfactants in an aqueous phase. The unique structure of niosome presents an effective novel drug delivery system (NDDS) with ability of loading both hydrophilic and lipophilic drugs. Numerous research articles have been published in scientific journals, reporting valuable results of individual case studies in this context. However, surveying and discussing the recent, rapidly growing reported studies along with their theoretical principals is required for the fully understanding and exploring the great potential of this approach. To this aim, we have provided an illustrated and comprehensive study from the view of a supramolecular chemist, interested in the synthesizing and studying chemical aggregates on the nanoscale for the development of nanotechnological clusters including niosomes. First, a connectional review of the molecular structure and physicochemical properties of niosome forming non-ionic surfactants and additive agents have been discussed. Second, a systematic survey of niosome preparation and loading methods, administration routes, characterization of niosomes, their toxicity studies and mechanism of drug release; used in recent articles have been performed. Copyright © 2014 Elsevier B.V. All rights reserved.
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            Niosomes from 80s to present: the state of the art.

            Efficient and safe drug delivery has always been a challenge in medicine. The use of nanotechnology, such as the development of nanocarriers for drug delivery, has received great attention owing to the potential that nanocarriers can theoretically act as "magic bullets" and selectively target affected organs and cells while sparing normal tissues. During the last decades the formulation of surfactant vesicles, as a tool to improve drug delivery, brought an ever increasing interest among the scientists working in the area of drug delivery systems. Niosomes are self assembled vesicular nanocarriers obtained by hydration of synthetic surfactants and appropriate amounts of cholesterol or other amphiphilic molecules. Just like liposomes, niosomes can be unilamellar or multilamellar, are suitable as carriers of both hydrophilic and lipophilic drugs and are able to deliver drugs to the target site. Furthermore, niosomal vesicles, that are usually non-toxic, require less production costs and are stable over a longer period of time in different conditions, so overcoming some drawbacks of liposomes. The niosome properties are specifically dictated by size, shape, and surface chemistry which are able to modify the drug's intrinsic pharmacokinetics and eventual drug targeting to the areas of pathology. This up-to-date review deals with composition, preparation, characterization/evaluation, advantages, disadvantages and application of niosomes.
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              Effect of some formulation parameters on flurbiprofen encapsulation and release rates of niosomes prepared from proniosomes.

              Proniosomal gels or solutions of flurbiprofen were developed based on span 20 (Sp 20), span 40 (Sp 40), span 60 (Sp 60), and span 80 (Sp 80) without and with cholesterol. Nonionic surfactant vesicles (niosomes) formed immediately upon hydrating proniosomal formulae. The entrapment efficiency (EE%) of flurbiprofen (a poorly soluble drug) was either determined by exhaustive dialysis of freshly prepared niosomes or centrifugation of freeze-thawed vesicles. The influence of different processing and formulation variables such as surfactant chain length, cholesterol content, drug concentration, total lipid concentration, negatively or positively charging lipids, and the pH of the dispersion medium on flurbiprofen EE% was demonstrated. Also, the release of the prepared niosomes in phosphate buffer (pH 7.4) was illustrated. Results indicated that the EE% followed the trend Sp 60 (C(18))>Sp 40 (C(16))>Sp 20 (C(12))>Sp 80 (C(18)). Cholesterol increased or decreased the EE% depending on either the type of the surfactant or its concentration within the formulae. The maximum loading efficiency was 94.61% when the hydrating medium was adjusted to pH 5.5. Increasing total lipid or drug concentration also increased the EE% of flurbiprofen into niosomes. However, incorporation of either dicetyl phosphate (DCP) which induces negative charge or stearyl amine (SA) which induces positive charge decreased the EE% of flurbiprofen into niosomal vesicles. Finally, in vitro release data for niosomes of Sp 40 and Sp 60 showed that the release profiles of flurbiprofen from niosomes of different cholesterol contents is an apparently biphasic release process. As a result, this study suggested the potential of proniosomes as stable precursors for the immediate preparation of niosomal carrier systems.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2016
                02 August 2016
                : 10
                : 2421-2433
                Affiliations
                Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
                Author notes
                Correspondence: Gihan Fetih, Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, 71526, Egypt, Tel +20 10 0557 3833, Fax +20 88 2080 711, Email gfetih@ 123456yahoo.com
                Article
                dddt-10-2421
                10.2147/DDDT.S113775
                4977085
                27536063
                © 2016 Allam and Fetih. 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.

                Categories
                Original Research

                Pharmacology & Pharmaceutical medicine

                anti-hypertensive, pharmacokinetics, β1- antagonist

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