Browsing by Author "Fayad W."

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    Ethosomes and lipid-coated chitosan nanocarriers for skin delivery of a chlorophyll derivative: A potential treatment of squamous cell carcinoma by photodynamic therapy
    (Elsevier B.V., 2019) Nasr S.; Rady M.; Gomaa I.; Syrovet T.; Simmet T.; Fayad W.; Abdel-Kader M.; Institute of Pharmacology of Natural Products & Clinical Pharmacology; Ulm University; Ulm; D-89081; Germany; Department of Chemistry; School of Sciences and Engineering; American University in Cairo (AUC); Egypt; Pharmaceutical Technology Department; Faculty of Pharmacy and Biotechnology; German University in Cairo (GUC). Main Entrance of Al-Tagamoa Al-Khames New Cairo City; Egypt; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Egypt; Drug Bioassay-Cell Culture Laboratory; Pharmacognosy Department; National Research Centre; Dokki; Giza; 12622; Egypt; National Institute of Laser Enhanced Sciences (NILES); Cairo University (CU); Giza; Egypt
    Photodynamic therapy (PDT) is a localized treatment strategy used for skin cancers such as squamous cell carcinoma (SCC), the second most common form of skin cancer. PDT combines a photosensitizer, laser source and tissue oxygen. In this study, the selected photosensitizer, ferrous chlorophyllin (Fe-CHL) was loaded in ethosomes and lipid coated chitosan (PC/CHI) nanocarriers to enhance skin delivery of Fe-CHL for potential PDT of squamous carcinoma. The nanocarrier formulations were characterized and studied for their skin retention and penetration depth of Fe-CHL across mouse skin ex vivo using high performance liquid chromatography and confocal microscopy. Confocal microscope images of mouse skin showed deeper penetration of ethosomes down to the dermis when compared to PC/CHI that was confined to the epidermis, although they showed no significant difference in skin retention. Immunohistochemistry (IHC) staining with HE, ki67 and TUNEL show maintained skin structure and no cytotoxic effects of the nanocarrier gel formulations before laser exposure to mouse skin. The nanocarriers were also studied for their PDT effect against human SCC monolayer and three-dimensional (3-D) spheroids. When compared to ethosomes, PC/CHI showed higher cytotoxicity in MTT assay and live confocal microscopy showed cell disintegration after laser exposure. For 3-D spheroids, PC/CHI also showed higher cytotoxicity using acid phosphatase assay and a decrease in spheroid size was observed using light microscopy. In conclusion, both types of nanocarriers can be used for their potential treatment of SCC using PDT depending on the tumour localization in the skin. � 2019 Elsevier B.V.
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    Novel hydrazide-hydrazone and amide substituted coumarin derivatives: Synthesis, cytotoxicity screening, microarray, radiolabeling and in vivo pharmacokinetic studies
    (Pharmacologyonline, 2018) Nasr T.; Bondock S.; Rashed H.M.; Fayad W.; Youns M.; Sakr T.M.; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Helwan University; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Modern University for Technology and Information; Egypt; Department of Chemistry; Faculty of Science; Mansoura University; Mansoura; ET-35516; Egypt; Department of Chemistry; Faculty of Science; King Khalid University; Abha; 9004; Saudi Arabia; Labeled Compounds Department; Hot Labs Center; Egyptian Atomic Energy Authority; P.O. Code 13759; Cairo; Egypt; Drug Bioassay-Cell Culture Laboratory; Pharmacognosy Department; National Research Centre; Dokki; Giza 12622; Egypt; Department of Biochemistry and Molecularlar Biology; Faculty of Pharmacy; Helwan University; Egypt; Radioactive Isotopes and Generators Department; Hot Laboratories Centre; Atomic Energy Authority; P.O. Code 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA)Giza; Egypt
    The current work presents the synthesis and biological evaluation of new series of coumarin hydrazide-hydrazone derivatives that showed in vitro broad spectrum antitumor activities against resistant pancreatic carcinoma (Panc-1), hepatocellular carcinoma (HepG2) and leukemia (CCRF) cell lines using doxorubicin as reference standard. Bromocoumarin hydrazide-hydrazone derivative (BCHHD) 11b showed excellent anticancer activity against all tested cancer cell lines. Enzyme assays showed that BCHHD 11b induced apoptosis due to activation of caspases 3/7. Moreover, 11b inhibited GST and CYP3A4 in a dose dependent manner and the induced cell death could be attributed to metabolic inhibition. Moreover, 11b microarray analysis showed significant up- and down-regulation of many genes in the treated cells related to apoptosis, cell cycle, tumor growth and suppressor genes. All of the above presents BCHHD 11b as a potent anticancer agent able to overcome drug resistance. In addition, compound 11b was able to serve as a chemical carrier for 99mTc and the in vivo biodistribution study of 99mTc-11b complex revealed a remarkable targeting ability of 99mTc into solid tumor showing that 99mTc-11b might be used as a promising radiopharmaceutical imaging agent for cancer. � 2018 Elsevier Masson SAS