{
    "abstract": "Cellulite (CLT) is one of the commonly known lipodystrophy syndromes affecting post-adolescent women worldwide. It is topographically characterized by an orange-peel, dimpled skin appearance hence, it is an unacceptable cosmetic problem. CLT can be modulated by surgical procedures such as; liposuction and mesotherapy. But, these options are invasive, expensive and risky. For these reasons, topical CLT treatments are more preferred. Caffeine (CA), is a natural alkaloid that is well-known for its prominent anti-cellulite effects. However, its hydrophilicity hinders its cutaneous permeation. Therefore, in the present study CA was loaded into solid lipid nanoparticles (SLNs) by high shear homogenization/ultrasonication. CA-SLNs were prepared using Compritol\u00ae 888 ATO and stearic acid as solid lipids, and span 60 and brij\u212235, as lipid dispersion stabilizing agents. Formulation variables were adjusted to obtain entrapment efficiency (EE\u2009>\u200975%), particle size (PS\u2009<\u2009350\u00a0nm), zeta potential (ZP\u2009<\u2009-25\u00a0mV) and polydispersity index (PDI\u2009<\u20090.5). CA-SLN-4 was selected and showed maximized EE (92.03\u2009\u00b1\u20090.16%), minimized PS (232.7\u2009\u00b1\u20091.90\u00a0nm), and optimum ZP (-25.15\u2009\u00b1\u20090.65\u00a0mV) and PDI values (0.24\u2009\u00b1\u20090.02). CA-SLN-4 showed superior CA release (99.44\u2009\u00b1\u20090.36%) compared to the rest CA-SLNs at 1\u00a0h. TEM analysis showed spherical, nanosized CA-SLN-4 vesicles. Con-LSM analysis showed successful CA-SLN-4 permeation transepidermally and via shunt diffusion. CA-SLN-4 incorporated into Noveon AA-1\u00ae hydrogel (CA-SLN-Ngel) showed accepted physical/rheological properties, and in vitro release profile. Histological studies showed that CA-SLN-Ngel significantly reduced mean subcutaneous fat tissue (SFT) thickness with 4.66 fold (p\u2009=\u20090.035) and 4.16 fold (p\u2009=\u20090.0001) compared to CA-gel, at 7th and 21st days, respectively. Also, significant mean SFT thickness reduction was observed compared to untreated group with 4.83 fold (p\u2009=\u20090.0005) and 3.83 fold (p\u2009=\u20090.0043), at 7th and 21st days, respectively. This study opened new avenue for CA skin delivery via advocating the importance of skin appendages. Hence, CA-SLN-Ngel could be a promising nanocosmeceutical gel for effective CLT treatment.",
    "authors": [
        {
            "affiliation": "Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Ahram Canadian University, 6th of October city, Giza, Egypt. shahinazeamry9@gmail.com.",
            "firstname": "Shahinaze A",
            "initials": "SA",
            "lastname": "Fouad"
        },
        {
            "affiliation": "Biolink Egypt for Chemical Industries, 6th of October city, Giza, Egypt.",
            "firstname": "Taher A",
            "initials": "TA",
            "lastname": "Badr"
        },
        {
            "affiliation": "Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.",
            "firstname": "Ahmed",
            "initials": "A",
            "lastname": "Abdelbary"
        },
        {
            "affiliation": "Department of Medical Applications of Laser (MAL), National Institute of Laser Enhanced Sciences (NILES), Cairo University, Cairo, Egypt.",
            "firstname": "Maha",
            "initials": "M",
            "lastname": "Fadel"
        },
        {
            "affiliation": "Department of Industrial Pharmacy, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Cairo, Egypt.",
            "firstname": "Rehab",
            "initials": "R",
            "lastname": "Abdelmonem"
        },
        {
            "affiliation": "Department of Pharmaceutics and Medicinal Chemistry, Thomas J. Long School of Pharmacy & Health Sciences, University of the Pacific, Stockton, California, USA.",
            "firstname": "Bhaskara R",
            "initials": "BR",
            "lastname": "Jasti"
        },
        {
            "affiliation": "Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.",
            "firstname": "Mohamed",
            "initials": "M",
            "lastname": "El-Nabarawi"
        }
    ],
    "conclusions": null,
    "copyrights": "\u00a9 2024. The Author(s).",
    "doi": "10.1208/s12249-024-02943-2\n10.5114/ada.2018.77235\n10.5021/ad.2015.27.3.243\n10.1016/j.jddst.2021.102737\n10.1016/j.ijpharm.2023.123271\n10.1111/j.1468-3083.2012.04622.x\n10.3390/ph14090842\n10.1016/j.ijwd.2018.09.002\n10.1080/10717544.2021.1989088\n10.1159/000343174\n10.1208/s12249-018-0955-x\n10.3109/03639045.2014.980426\n10.1016/j.jddst.2020.102084\n10.1080/03639045.2017.1386206\n10.1590/s2175-97902019000218236\n10.3109/10717544.2014.903011\n10.1016/j.jsps.2021.12.018\n10.1002/jps.20335\n10.2174/1381612826666200526145706\n10.15171/apb.2016.06\n10.7324/JAPS.2020.10617\n10.3390/scipharm89020025\n10.1016/j.colsurfb.2011.07.060\n10.1016/j.biopha.2018.07.106\n10.1080/03639045.2018.1459675\n10.2147/IJN.S196771\n10.22159/ijap.2022v14i4.44681\n10.52403/ijrr.20220703\n10.1007/s13346-018-0489-5\n10.3390/cosmetics8030069\n10.3390/polym13111808\n10.3390/pharmaceutics13050682\n10.1007/s11095-019-2741-1\n10.1111/j.1473-2165.2008.00357.x\n10.1080/10717544.2023.2181747\n10.1016/j.ejpb.2010.05.003\n10.1208/s12249-014-0175-y\n10.1016/j.ijpharm.2011.12.037\n10.1208/s12249-008-9105-1\n10.3109/10731199.2011.611476\n10.1016/j.jddst.2015.04.009\n10.1016/j.jddst.2018.07.015\n10.1016/j.ejps.2012.05.010\n10.1016/0378-5173(94)90228-3\n10.1080/10717544.2019.1686087\n10.1016/j.ijpharm.2010.06.034\n10.1002/ejlt.201400650\n10.1517/17425247.2014.935335\n10.1016/j.colsurfa.2022.128774\n10.1007/s13346-022-01285-5\n10.3109/08982104.2014.911313\n10.3109/10837450.2014.882935\n10.1016/j.colsurfb.2019.01.027\n10.3109/10915818709098563\n10.1007/s11746-007-1110-0\n10.3390/gels8020129\n10.1016/j.ijpharm.2011.11.032\n10.3390/pharmaceutics13040523\n10.1016/j.addr.2012.09.021\n10.3390/pharmaceutics14081727\n10.2174/1573413711309020008\n10.1208/s12249-014-0278-5\n10.1039/C5RA06047H\n10.3390/pharmaceutics14122818\n10.1016/j.addr.2007.04.006\n10.1159/000101389\n10.1111/j.1365-2125.2007.03065.x\n10.1159/000313514\n10.2165/00137696-200604040-00004\n10.1159/000489857\n10.1007/978-3-319-53811-2\n10.1208/pt030435\n10.9734/BJPR/2013/2775\n10.1016/j.carbpol.2017.05.019\n10.1016/j.ijpharm.2015.05.075\n10.3109/10837450.2011.653821",
    "journal": "AAPS PharmSciTech",
    "keywords": [
        "Caffeine",
        "Cellulite",
        "Enhanced caffeine permeation and targeting",
        "Nanocosmeceutical gel",
        "Trans-epidermal/trans-appendageal skin reservoirs"
    ],
    "methods": null,
    "publication_date": "2024-10-10",
    "pubmed_id": "39384727\n26082579\n37499772\n38524143\n34577542\n34623203\n23075568\n29380282\n25382163\n28956468\n24735249\n35241963\n15700772\n15793804\n32452322\n30052191\n21865017\n30119227\n29614890\n30936696\n29423833\n34072642\n34068544\n18254807\n36803255\n20470882\n25035071\n22227603\n18563578\n22664358\n31736366\n20599487\n25152197\n36585559\n24779560\n24490828\n30878805\n16414573\n35200510\n22155414\n33918870\n36015353\n25591953\n36559311\n17544165\n17396054\n18070215\n20588083\n30001555\n28578949\n26043822\n22324371",
    "results": null,
    "title": "New Insight for Enhanced Topical Targeting of Caffeine for Effective Cellulite Treatment: In Vitro Characterization, Permeation Studies, and Histological Evaluation in Rats.",
    "xml": "<Element 'PubmedArticle' at 0x788502a1ccc0>"
}