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      The effectiveness of ursolic acid niosomes with chitosan coating for prevention of liver damage in mice induced by n-nitrosodiethylamine

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          Abstract

          Ursolic acid (UA) is a pentacyclic triterpene carboxylic acid which produces various effects, including anti-cancer, hepatoprotective, antioxidant and anti-inflammatory. However, UA demonstrates poor water solubility and permeability. Niosomes have been reported to improve the bioavailability of low water-soluble drugs. This study aimed to investigate the protective action of UA-niosomes with chitosan layers against liver damage induced by N-Nitrosodiethylamine (NDEA). UA niosomes were prepared using a thin layer hydration method, with chitosan being added by vortexing the mixtures. For the induction of liver damage, the mice were administered NDEA intraperitoneally (25 mg/kgBW). They were given niosomes orally (11 mg UA/kgBW) seven and three days prior to NDEA induction and subsequently once a week with NDEA induction for four weeks. The results showed that chitosan layers increased the particle sizes, PDI, and ζ-potentials of UA niosomes. UA niosomes with chitosan coating reduced the SGOT and SGPT level. The histopathological evaluation of liver tissue showed an improvement with reduced bile duct inflammation and decreasing pleomorphism and enlargement of hepatocyte cell nuclei in UA niosomes with the chitosan coating treated group. It can be concluded that UA niosomes with chitosan coating improved the efficacy of preventive UA therapy in liver-damaged mice induced with NDEA.

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          Impact of Particle Size and Polydispersity Index on the Clinical Applications of Lipidic Nanocarrier Systems

          Lipid-based drug delivery systems, or lipidic carriers, are being extensively employed to enhance the bioavailability of poorly-soluble drugs. They have the ability to incorporate both lipophilic and hydrophilic molecules and protecting them against degradation in vitro and in vivo. There is a number of physical attributes of lipid-based nanocarriers that determine their safety, stability, efficacy, as well as their in vitro and in vivo behaviour. These include average particle size/diameter and the polydispersity index (PDI), which is an indication of their quality with respect to the size distribution. The suitability of nanocarrier formulations for a particular route of drug administration depends on their average diameter, PDI and size stability, among other parameters. Controlling and validating these parameters are of key importance for the effective clinical applications of nanocarrier formulations. This review highlights the significance of size and PDI in the successful design, formulation and development of nanosystems for pharmaceutical, nutraceutical and other applications. Liposomes, nanoliposomes, vesicular phospholipid gels, solid lipid nanoparticles, transfersomes and tocosomes are presented as frequently-used lipidic drug carriers. The advantages and limitations of a range of available analytical techniques used to characterize lipidic nanocarrier formulations are also covered.
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            Endocytosis and exocytosis of nanoparticles in mammalian cells

            Engineered nanoparticles that can be injected into the human body hold tremendous potential to detect and treat complex diseases. Understanding of the endocytosis and exocytosis mechanisms of nanoparticles is essential for safe and efficient therapeutic application. In particular, exocytosis is of significance in the removal of nanoparticles with drugs and contrast agents from the body, while endocytosis is of great importance for the targeting of nanoparticles in disease sites. Here, we review the recent research on the endocytosis and exocytosis of functionalized nanoparticles based on various sizes, shapes, and surface chemistries. We believe that this review contributes to the design of safe nanoparticles that can efficiently enter and leave human cells and tissues.
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              Ursolic Acid—A Pentacyclic Triterpenoid with a Wide Spectrum of Pharmacological Activities

              Ursolic acid (UA) is a natural terpene compound exhibiting many pharmaceutical properties. In this review the current state of knowledge about the health-promoting properties of this widespread, biologically active compound, as well as information about its occurrence and biosynthesis are presented. Particular attention has been paid to the application of ursolic acid as an anti-cancer agent; it is worth noticing that clinical tests suggesting the possibility of practical use of UA have already been conducted. Amongst other pharmacological properties of UA one can mention protective effect on lungs, kidneys, liver and brain, anti-inflammatory properties, anabolic effects on skeletal muscles and the ability to suppress bone density loss leading to osteoporosis. Ursolic acid also exhibits anti-microbial features against numerous strains of bacteria, HIV and HCV viruses and Plasmodium protozoa causing malaria.
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                Author and article information

                Contributors
                andang-m@ff.unair.ac.id
                Journal
                Sci Rep
                Sci Rep
                Scientific Reports
                Nature Publishing Group UK (London )
                2045-2322
                10 December 2022
                10 December 2022
                2022
                : 12
                : 21397
                Affiliations
                [1 ]GRID grid.440745.6, ISNI 0000 0001 0152 762X, Department of Pharmaceutical Sciences, Faculty of Pharmacy, , Universitas Airlangga, ; Surabaya, 60115 Indonesia
                [2 ]GRID grid.440745.6, ISNI 0000 0001 0152 762X, Stem Cell Research and Development Center, , Universitas Airlangga, ; Surabaya, 60115 Indonesia
                [3 ]GRID grid.440745.6, ISNI 0000 0001 0152 762X, Master Program of Pharmaceutical Sciences, Faculty of Pharmacy, , Universitas Airlangga, ; Surabaya, 60115 Indonesia
                [4 ]GRID grid.440745.6, ISNI 0000 0001 0152 762X, Department of Veterinary Science, Faculty of Veterinary Medicine, , Universitas Airlangga, ; Surabaya, 60115 Indonesia
                Article
                26085
                10.1038/s41598-022-26085-2
                9741648
                36496469
                1e03ce6d-1441-4d61-b6cc-1bb51d4a809f
                © The Author(s) 2022

                Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.

                History
                : 26 September 2022
                : 9 December 2022
                Funding
                Funded by: the Ministry of Education, Culture, Research, and Technology of the Republic of Indonesia.
                Award ID: No. 672/UN3/2022
                Award Recipient :
                Categories
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                © The Author(s) 2022

                Uncategorized
                medical research,nanoscience and technology
                Uncategorized
                medical research, nanoscience and technology

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