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  1. Article: Enhanced Codelivery of Gefitinib and Azacitidine for Treatment of Metastatic-Resistant Lung Cancer Using Biodegradable Lipid Nanoparticles.

    Elzayat, Ehab M / Sherif, Abdelrahman Y / Nasr, Fahd A / Attwa, Mohamed W / Alshora, Doaa H / Ahmad, Sheikh F / Alqahtani, Ali S

    Materials (Basel, Switzerland)

    2023  Volume 16, Issue 15

    Abstract: Lung cancer is a formidable challenge in clinical practice owing to its metastatic nature and resistance to conventional treatments. The codelivery of anticancer agents offers a potential solution to overcome resistance and minimize systemic toxicity. ... ...

    Abstract Lung cancer is a formidable challenge in clinical practice owing to its metastatic nature and resistance to conventional treatments. The codelivery of anticancer agents offers a potential solution to overcome resistance and minimize systemic toxicity. The encapsulation of these agents within nanostructured lipid carriers (NLCs) provides a promising strategy to enhance lymphatic delivery and reduce the risk of relapse. This study aimed to develop an NLC formulation loaded with Gefitinib and Azacitidine (GEF-AZT-NLC) for the treatment of metastatic-resistant lung cancer. The physicochemical properties of the formulations were characterized, and in vitro drug release was evaluated using the dialysis bag method. The cytotoxic activity of the GEF-AZT-NLC formulations was assessed on a lung cancer cell line, and hemocompatibility was evaluated using suspended red blood cells. The prepared formulations exhibited nanoscale size (235-272 nm) and negative zeta potential values (-15 to -31 mV). In vitro study revealed that the GEF-AZT-NLC formulation retained more than 20% and 60% of GEF and AZT, respectively, at the end of the experiment. Hemocompatibility study demonstrated the safety of the formulation for therapeutic use, while cytotoxicity studies suggested that the encapsulation of both anticancer agents within NLCs could be advantageous in treating resistant cancer cells. In conclusion, the GEF-AZT-NLC formulation developed in this study holds promise as a potential therapeutic tool for treating metastatic-resistant lung cancer.
    Language English
    Publishing date 2023-07-30
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2487261-1
    ISSN 1996-1944
    ISSN 1996-1944
    DOI 10.3390/ma16155364
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Correction to: Formulation of Gelucire®-Based Solid Dispersions of Atorvastatin Calcium: In Vitro Dissolution and In Vivo Bioavailability Study.

    Aldosari, Basmah N / Almurshedi, Alanood S / Alfagih, Iman M / AlQuadeib, Bushra T / Altamimi, Mohammad A / Imam, Syed Sarim / Hussain, Afzal / Alqahtani, Faleh / Elzayat, Ehab / Alshehri, Sultan

    AAPS PharmSciTech

    2022  Volume 23, Issue 7, Page(s) 278

    Language English
    Publishing date 2022-10-13
    Publishing country United States
    Document type Published Erratum
    ZDB-ID 2052070-0
    ISSN 1530-9932 ; 1530-9932
    ISSN (online) 1530-9932
    ISSN 1530-9932
    DOI 10.1208/s12249-022-02429-z
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Optimization of apigenin nanoparticles prepared by planetary ball milling

    Alshehri Abdulla Ali / Ibrahim Mohamed Abbas / Alshehri Sultan Mohamed / Alshora Doaa / Elzayat Ehab Mostafa / Almeanazel Osaid / Alsaadi Badr / El Sherbiny Gamal A. / Osman Shaaban Khalaf

    Green Processing and Synthesis, Vol 12, Iss 1, Pp 237-

    In vitro and in vivo studies

    2023  Volume 43

    Abstract: This study intended to optimize apigenin (APG) nanoparticle formulation prepared by planetary ball milling to enhance its dissolution rate and bioavailability using a design of experiment (DoE). In this study, polyvinyl pyrrolidone (PVP K30) was used as ... ...

    Abstract This study intended to optimize apigenin (APG) nanoparticle formulation prepared by planetary ball milling to enhance its dissolution rate and bioavailability using a design of experiment (DoE). In this study, polyvinyl pyrrolidone (PVP K30) was used as a nanoparticle stabilizer. The independent parameters of milling speed, milling ball size, and drug to solvent ratio were evaluated for their impacts on APG nanoparticles concerning the nanoparticle size (Y1), zeta potential (Y2), and drug dissolution efficiency after 60 min, notated as % DE60 (Y3). The milling ball size showed a significant antagonistic effect (P = 0.0210) on the size of APG nanoparticles, while milling speed had an agonistic effect on the zeta potential values of drug nanoparticles, ranging from low to medium speed levels. In addition, ANOVA analysis indicated that the effect of the drug-to-solvent ratio on the % DE60 of APG from the nanoparticle formulations was antagonistically significant (P = 0.015), and the quadratic effect of milling speed (AA) also had a significant antagonistic effect (P = 0.025) on the % DE60. Risk assessment analytical tools revealed that milling ball size and milling speed significantly affect the nanoparticle size. The drug/solvent ratio exerted a strong impact on % DE60. Furthermore, the maximum plasma concentration (C max) of the optimized APG nanoparticle formula increased by four folds. In addition, AUC0–t (ng·mL−1·h−1) for APG nanoparticle (353.7 ± 185.3 ng·mL−1·h−1) was higher than that noticed in the case of the untreated drug (149 ± 137.5 ng·mL−1·h−1) by more than two folds.
    Keywords apigenin ; optimization ; nanonization ; planetary ball milling ; pharmacokinetics ; Chemistry ; QD1-999
    Subject code 500
    Language English
    Publishing date 2023-02-01T00:00:00Z
    Publisher De Gruyter
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: Solubilization and thermodynamic properties of simvastatin in various micellar solutions of different non-ionic surfactants: Computational modeling and solubilization capacity.

    Shakeel, Faiyaz / Alshehri, Sultan / Ibrahim, Mohamed A / Altamimi, Mohammad / Haq, Nazrul / Elzayat, Ehab M / Shazly, Gamal A

    PloS one

    2021  Volume 16, Issue 4, Page(s) e0249485

    Abstract: The aim of this work was to solubilize simvastatin (SIM) using different micellar solutions of various non-ionic surfactants such as Tween-80 (T80), Tween-20 (T20), Myrj-52 (M52), Myrj-59 (M59), Brij-35 (B35) and Brij-58 (B58). The solubility of SIM in ... ...

    Abstract The aim of this work was to solubilize simvastatin (SIM) using different micellar solutions of various non-ionic surfactants such as Tween-80 (T80), Tween-20 (T20), Myrj-52 (M52), Myrj-59 (M59), Brij-35 (B35) and Brij-58 (B58). The solubility of SIM in water (H2O) and different micellar concentrations of T80, T20, M52, M59, B35 and B58 was determined at temperatures T = 300.2 K to 320.2 K under atmospheric pressure p = 0.1 MPa using saturation shake flask method. The experimental solubility data of SIM was regressed using van't Hoff and Apelblat models. The solubility of SIM (mole fraction) was recorded highest in M59 (1.54 x 10-2) followed by M52 (6.56 x 10-3), B58 (5.52 x 10-3), B35 (3.97 x 10-3), T80 (1.68 x 10-3), T20 (1.16 x 10-3) [the concentration of surfactants was 20 mM in H2O in all cases] and H2O (1.94 x 10-6) at T = 320.2 K. The same results were also recorded at each temperature and each micellar concentration of T80, T20, M52, M59, B35 and B58. "Apparent thermodynamic analysis" showed endothermic and entropy-driven dissolution/solubilization of SIM in H2O and various micellar solutions of T80, T20, M52, M59, B35 and B58.
    MeSH term(s) Micelles ; Models, Molecular ; Molecular Conformation ; Polyethylene Glycols/chemistry ; Simvastatin/chemistry ; Solubility ; Solvents/chemistry ; Surface-Active Agents/chemistry ; Thermodynamics ; Water/chemistry
    Chemical Substances Micelles ; Solvents ; Surface-Active Agents ; Water (059QF0KO0R) ; Polyethylene Glycols (3WJQ0SDW1A) ; polyethylene glycol monostearate (9004-99-3) ; Simvastatin (AGG2FN16EV)
    Language English
    Publishing date 2021-04-08
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1932-6203
    ISSN (online) 1932-6203
    DOI 10.1371/journal.pone.0249485
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Solubilization and thermodynamic properties of simvastatin in various micellar solutions of different non-ionic surfactants

    Faiyaz Shakeel / Sultan Alshehri / Mohamed A Ibrahim / Mohammad Altamimi / Nazrul Haq / Ehab M Elzayat / Gamal A Shazly

    PLoS ONE, Vol 16, Iss 4, p e

    Computational modeling and solubilization capacity.

    2021  Volume 0249485

    Abstract: The aim of this work was to solubilize simvastatin (SIM) using different micellar solutions of various non-ionic surfactants such as Tween-80 (T80), Tween-20 (T20), Myrj-52 (M52), Myrj-59 (M59), Brij-35 (B35) and Brij-58 (B58). The solubility of SIM in ... ...

    Abstract The aim of this work was to solubilize simvastatin (SIM) using different micellar solutions of various non-ionic surfactants such as Tween-80 (T80), Tween-20 (T20), Myrj-52 (M52), Myrj-59 (M59), Brij-35 (B35) and Brij-58 (B58). The solubility of SIM in water (H2O) and different micellar concentrations of T80, T20, M52, M59, B35 and B58 was determined at temperatures T = 300.2 K to 320.2 K under atmospheric pressure p = 0.1 MPa using saturation shake flask method. The experimental solubility data of SIM was regressed using van't Hoff and Apelblat models. The solubility of SIM (mole fraction) was recorded highest in M59 (1.54 x 10-2) followed by M52 (6.56 x 10-3), B58 (5.52 x 10-3), B35 (3.97 x 10-3), T80 (1.68 x 10-3), T20 (1.16 x 10-3) [the concentration of surfactants was 20 mM in H2O in all cases] and H2O (1.94 x 10-6) at T = 320.2 K. The same results were also recorded at each temperature and each micellar concentration of T80, T20, M52, M59, B35 and B58. "Apparent thermodynamic analysis" showed endothermic and entropy-driven dissolution/solubilization of SIM in H2O and various micellar solutions of T80, T20, M52, M59, B35 and B58.
    Keywords Medicine ; R ; Science ; Q
    Subject code 660
    Language English
    Publishing date 2021-01-01T00:00:00Z
    Publisher Public Library of Science (PLoS)
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Formulation, In Vitro and In Vivo Evaluation of Gefitinib Solid Dispersions Prepared Using Different Techniques

    Sultan Alshehri / Abdullah Alanazi / Ehab M. Elzayat / Mohammad A. Altamimi / Syed S. Imam / Afzal Hussain / Faleh Alqahtani / Faiyaz Shakeel

    Processes, Vol 9, Iss 1210, p

    2021  Volume 1210

    Abstract: Gefitinib (Gef) is a poorly water-soluble antitumor drug, which shows poor absorption/bioavailability after oral administration. Therefore, this study was carried out to develop Gef solid dispersions (SDs) using different carriers and different ... ...

    Abstract Gefitinib (Gef) is a poorly water-soluble antitumor drug, which shows poor absorption/bioavailability after oral administration. Therefore, this study was carried out to develop Gef solid dispersions (SDs) using different carriers and different techniques in order to enhance its dissolution and oral absorption/bioavailability. Various SD formulations of Gef were established using fusion and microwave methods utilizing Soluplus, Kollidone VA64, and polyethylene glycol 4000 (PEG 4000) as the carriers. Developed SDs of Gef were characterized physicochemically and evaluated for in vitro dissolution and in vivo pharmacokinetic studies. The physicochemical evaluation revealed the formation of Gef SDs using fusion and microwave methods. In vitro dissolution studies indicated significant release of Gef from all SDs compared to the pure Gef. Optimized SD of Gef (S2-MW) presented significant release of Gef (82.10%) compared with pure Gef (21.23%). The optimized Gef SD (S2) was subjected to in vivo pharmacokinetic evaluation in comparison with pure Gef in rats. The results indicated significant enhancement in various pharmacokinetic parameters of Gef from an optimized SD S2 compared to the pure Gef. In addition, Gef-SD S2 resulted in remarkable improvement in bioavailability compared to the pure Gef. Overall, this study suggested that the prepared Gef-SD by microwave method showed marked enhancement in dissolution and bioavailability.
    Keywords gefitinib ; fusion method ; microwave method ; polymeric carriers ; pharmacokinetics ; solid dispersion ; Chemical technology ; TP1-1185 ; Chemistry ; QD1-999
    Subject code 500
    Language English
    Publishing date 2021-07-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  7. Article ; Online: Nicotine and cotinine quantification after a 4-week inhalation of electronic cigarette vapors in male and female mice using UPLC-MS/MS.

    Alasmari, Fawaz / Alasmari, Abdullah F / Elzayat, Ehab / Alotaibi, Majed M / Alotaibi, Farraj M / Attwa, Mohamed W / Alanazi, Fars K / Abdelgadir, Elkhatim H / Ahmad, Syed Rizwan / Alqahtani, Faleh / Al-Rejaie, Salim S / Alshammari, Musaad A

    Saudi medical journal

    2022  Volume 43, Issue 7, Page(s) 678–686

    Abstract: Objectives: To detect the cotinine and nicotine serum concentrations of female and male C57BL/6J mice after a 4-week exposure to electronic (e)-cigarette vapors using ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS).: ... ...

    Abstract Objectives: To detect the cotinine and nicotine serum concentrations of female and male C57BL/6J mice after a 4-week exposure to electronic (e)-cigarette vapors using ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS).
    Methods: This experimental study was carried out at an animal facility and laboratories, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia, between January and August 2020. A 4-week exposure to e-cigarettes was carried out using male and female mice and serum samples were obtained for cotinine and nicotine quantification using UPLC-MS/MS. The chromatographic procedures involved the use of a BEH HSS T3 C18 column (100 mm x 2.1 mm, 1.7 μm) with acetonitrile as a mobile phase and 0.1% formic acid (2:98 v/v).
    Results: The applied methodology has highly efficient properties of detection, estimation, and extraction, where the limit of quantification (LOQ) for nicotine was 0.57 ng/mL and limit of detection (LOD) for nicotine was 0.19 ng/mL, while the LOQ for cotinine was 1.11 ng/mL and LOD for cotinine was 0.38 ng/mL. The correlation coefficient was r
    Conclusion: This study showed that the gender factor might play a crucial role in nicotine metabolism.
    MeSH term(s) Animals ; Chromatography, High Pressure Liquid/methods ; Chromatography, Liquid/methods ; Cotinine/chemistry ; Cotinine/metabolism ; E-Cigarette Vapor ; Electronic Nicotine Delivery Systems ; Female ; Humans ; Male ; Mice ; Mice, Inbred C57BL ; Nicotine ; Tandem Mass Spectrometry/methods
    Chemical Substances E-Cigarette Vapor ; Nicotine (6M3C89ZY6R) ; Cotinine (K5161X06LL)
    Language English
    Publishing date 2022-07-13
    Publishing country Saudi Arabia
    Document type Journal Article
    ZDB-ID 392302-2
    ISSN 1658-3175 ; 0379-5284
    ISSN (online) 1658-3175
    ISSN 0379-5284
    DOI 10.15537/smj.2022.43.7.20220142
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Enhanced Dissolution of Luteolin by Solid Dispersion Prepared by Different Methods

    Sultan Alshehri / Syed Sarim Imam / Mohammad A. Altamimi / Afzal Hussain / Faiyaz Shakeel / Ehab Elzayat / Kazi Mohsin / Mohamed Ibrahim / Fars Alanazi

    ACS Omega, Vol 5, Iss 12, Pp 6461-

    Physicochemical Characterization and Antioxidant Activity

    2020  Volume 6471

    Keywords Chemistry ; QD1-999
    Language English
    Publishing date 2020-03-01T00:00:00Z
    Publisher American Chemical Society
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  9. Article: Case - Management of bullet retained in penile shaft after drive-by shooting.

    Levitt, Max / Ying, Thomas / Elzayat, Ehab Abdalla

    Canadian Urological Association journal = Journal de l'Association des urologues du Canada

    2021  Volume 16, Issue 3, Page(s) E181–E183

    Language English
    Publishing date 2021-10-21
    Publishing country Canada
    Document type Journal Article
    ZDB-ID 2431403-1
    ISSN 1911-6470
    ISSN 1911-6470
    DOI 10.5489/cuaj.7480
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Enhanced Dissolution of Luteolin by Solid Dispersion Prepared by Different Methods: Physicochemical Characterization and Antioxidant Activity.

    Alshehri, Sultan / Imam, Syed Sarim / Altamimi, Mohammad A / Hussain, Afzal / Shakeel, Faiyaz / Elzayat, Ehab / Mohsin, Kazi / Ibrahim, Mohamed / Alanazi, Fars

    ACS omega

    2020  Volume 5, Issue 12, Page(s) 6461–6471

    Abstract: Luteolin (LT) is a poorly soluble bioactive compound that suffered bioavailability problems after oral administration. Hence, the aim of the proposed research work was to formulate and investigate various solid dispersions (SDs) of LT in order to enhance ...

    Abstract Luteolin (LT) is a poorly soluble bioactive compound that suffered bioavailability problems after oral administration. Hence, the aim of the proposed research work was to formulate and investigate various solid dispersions (SDs) of LT in order to enhance its dissolution and bioactivity. LT-SD was prepared using polyethylene glycol 4000 (PEG 4000) as a carrier at the mass ratios of 1:1, 1:2, and 1:4. LT-SD was prepared using different methods including fusion (FU), solvent evaporation (SE), and microwave irradiation (MI) methods. The prepared LT-SD was duly characterized in terms of differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM), infrared (IR) spectroscopy, and nuclear magnetic resonance (NMR) and evaluated for dissolution and in vitro antioxidant activity. The results of DSC, XRD, SEM, IR, and NMR suggested the formation of LT-SD. After 90 min of the dissolution study, the results displayed that the % release of LT from prepared SD was significantly higher compared with the pure LT and its physical mixture dispersion (PMD). LT-SD prepared using the MI method displayed the maximum release of LT (i.e., 97.78 ± 4.41%) at a 1:2 mass ratio of LT:PEG 4000. The LT-SD prepared using the SE method displayed the maximum release of 93.78 ± 3.98% at a mass ratio of 1:4 of LT:PEG 4000. The SD prepared by the MI method showed enhanced dissolution due to higher aqueous solubility and the reduction of particle size. The solid-state characterization studies (DSC, XRD, SEM, IR, and NMR studies) suggested the morphological conversion of LT into the amorphous form from the crystalline state. The results of the antioxidant study revealed that the formation LT-SD displayed significantly higher radical scavenging activity than the pure LT. Therefore, SD obtained using PEG 4000 could be a potential strategy for maximizing the solubility, in vitro dissolution, and therapeutic efficacy of LT.
    Language English
    Publishing date 2020-03-20
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.9b04075
    Database MEDical Literature Analysis and Retrieval System OnLINE

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