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  1. Article ; Online: The Development and Optimization of Lipid-Based Self-Nanoemulsifying Drug Delivery Systems for the Intravenous Delivery of Propofol

    Mohsin Kazi / Athba Alqahtani / Majed Alharbi / Ajaz Ahmad / Muhammad Delwar Hussain / Hani Alothaid / Mohammed S. Aldughaim

    Molecules, Vol 28, Iss 1492, p

    2023  Volume 1492

    Abstract: Purpose: Propofol is a relatively short-acting potent anesthetic lipophilic drug used during short surgical procedures. Despite the success of propofol intravenous emulsions, drawbacks to such formulations include inherent emulsion instability, the lack ... ...

    Abstract Purpose: Propofol is a relatively short-acting potent anesthetic lipophilic drug used during short surgical procedures. Despite the success of propofol intravenous emulsions, drawbacks to such formulations include inherent emulsion instability, the lack of a safe vehicle to prevent sepsis, and concern regarding hyperlipidemia-related side effects. The aim of the current investigation was to develop a novel, lipid-based self-nanoemulsifying drug delivery system (SNEDDS) for propofol with improved stability and anesthetic activity for human use. Methods: A series of SNEDDS formulations were developed using naturally obtained medium-chain/long-chain mono-, di-, and triglycerides, glyceryl monocaprylate, and water-soluble cosolvents with hydrogenated castor oil constructing ternary phase diagrams for propofol. The developed SNEDDS formulations were characterized using visual observation, particle size analysis, zeta potential, transmission electron microscopy, equilibrium solubility, in vitro dynamic dispersion and stability, and in vivo sleeping disorder studies in rats. The in vivo bioavailability of the SNEDDSs in rats was also studied to compare the representative formulations with the marketed product Diprivan ® . Results: Medium-chain triglycerides (M810) with mono-diglycerides (CMCM) as an oil blend and hydrogenated castor oil (KHS15) as a surfactant were selected as key ingredients in ternary phase diagram studies. The nanoemulsifying regions were identified from the studies and a number of SNEDDSs were formulated. Results from the characterization studies demonstrated the formation of efficient nanosized particles (28–45 nm globule size, 0.10–0.20 PDI) in the optimized SNEDDS with a drug loading of 50 mg/g, which is almost 500-fold higher than free propofol. TEM analysis showed the formation of spherical and homogeneous nanoparticles of less than 50 nm. The dissolution rate of the representative SNEDDS was faster than raw propofol and able to maintain 99% propofol in aqueous solution for around 24 h. The ...
    Keywords self-nanoemulsifying drug delivery systems ; propofol ; pharmacokinetics ; sleeping disorder ; intravenous delivery ; Organic chemistry ; QD241-441
    Subject code 660
    Language English
    Publishing date 2023-02-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals

    Barkat Ali Khan / Maryam Waheed / Khaled M. Hosny / Waleed Y. Rizg / Samar S. Murshid / Majed Alharbi / Muhammad Khalid Khan

    Polymers, Vol 14, Iss 1489, p

    A Solubility Enhancement Approach

    2022  Volume 1489

    Abstract: Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. ... ...

    Abstract Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. Nanocrystals of pure KA were formulated by the top-down method under high-pressure homogenization followed by freeze drying. The nanocrystals were evaluated for stability and other physical characteristics, including zeta sizer analysis, DSC, surface morphology, XRD, drug content, solubility, FTIR and in vitro drug release. The KA nanocrystals were found to be stable when kept at exaggerated conditions. The particle size of the nanocrystals was 137.5 ± 1.7, 150 ± 2.8, and 110 ± 3.0 nm for the F1, F2 and F3 formulations, respectively. There was negative zeta potential for all the formulations. The dispersity index was 0.45 ± 0.2, 0.36 ± 0.4 and 0.41 ± 1.5 for the F1, F2 and F3, respectively. The DSC studies showed that there was no interaction between the KA and the excipients of the nanocrystals. The morphological studies confirmed the presence of rough crystalline surfaces on the nanosized particles. XRD studies showed the successful preparation of nanocrystals. The drug content was in the official range of 90 ± 10%. The solubility of KA was significantly ( p < 0.05) enhanced in the formulations of its nanocrystals as compared with pure KA powder. The ATR-FTIR studies revealed the presence of functional groups in both KA and KA-loaded nanocrystals, and no interaction was found between them. The nanocrystals released 83.93 ± 1.22% of KA in 24 h. The study concluded that the nanocrystals were successfully formulated using the top-down method followed by high-pressure homogenization. The solubility, as well as the dissolution, of the KA was enhanced, and this could improve the therapeutic effects of KA.
    Keywords sustainability of natural resources ; nanocrystals ; kojic acid ; solubility enhancement ; top-down technique ; Organic chemistry ; QD241-441
    Subject code 600
    Language English
    Publishing date 2022-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Anti-Quorum Sensing Activities of Gliptins against Pseudomonas aeruginosa and Staphylococcus aureus

    Maan T. Khayat / Hisham A. Abbas / Tarek S. Ibrahim / Ahdab N. Khayyat / Majed Alharbi / Khaled M. Darwish / Sameh S. Elhady / El-Sayed Khafagy / Martin K. Safo / Wael A. H. Hegazy

    Biomedicines, Vol 10, Iss 1169, p

    2022  Volume 1169

    Abstract: The development of bacterial resistance to traditional antibiotics constitutes an emerging public health issue. Promising approaches have been innovated to conquer bacterial resistance, and targeting bacterial virulence is one of these approaches. ... ...

    Abstract The development of bacterial resistance to traditional antibiotics constitutes an emerging public health issue. Promising approaches have been innovated to conquer bacterial resistance, and targeting bacterial virulence is one of these approaches. Bacterial virulence mitigation offers several merits, as antivirulence agents do not affect the growth of bacteria and hence do not induce bacteria to develop resistance. In this direction, numerous drugs have been repurposed as antivirulence agents prior to their clinical use alone or in combination with traditional antibiotics. Quorum sensing (QS) plays a key role in controlling bacterial virulence. In the current study, dipeptidase inhibitor-4 (DPI-4) antidiabetic gliptins were screened for their antivirulence and anti-quorum sensing (anti-QS) activities against Gram-negative Pseudomonas aeruginosa and Gram-positive Staphylococcus aureus . Upon assessing their antibiofilm activities, the ten tested gliptins significantly diminished biofilm formation. In particular, sitagliptin exhibited the most efficient antibiofilm activity, so it was chosen as a representative of all gliptins to further investigate its antivirulence activity. Sitagliptin significantly protected mice from P. aeruginosa and S. aureus pathogenesis. Furthermore, sitagliptin downregulated QS-encoding genes in P. aeruginosa and S. aureus . To test the anti-QS activities of gliptins, a detailed molecular docking study was conducted to evaluate the gliptins’ binding affinities to P. aeruginosa and S. aureus QS receptors, which helped explain the anti-QS activities of gliptins, particularly sitagliptin and omarigliptin. In conclusion, this study evaluates the possible antivirulence and anti-QS activities of gliptins that could be promising novel candidates for the treatment of aggressive Gram-negative or -positive bacterial infections either alone or as adjuvants to other antibiotics.
    Keywords antivirulence ; bacterial resistance ; gliptins ; quorum sensing ; industrial development ; Biology (General) ; QH301-705.5
    Subject code 572
    Language English
    Publishing date 2022-05-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: Sodium Citrate Alleviates Virulence in Pseudomonas aeruginosa

    Maan T. Khayat / Tarek S. Ibrahim / Ahdab N. Khayyat / Majed Alharbi / Moataz A. Shaldam / Khadijah A. Mohammad / El-Sayed Khafagy / Dalia A. El-damasy / Wael A. H. Hegazy / Hisham A. Abbas

    Microorganisms, Vol 10, Iss 1046, p

    2022  Volume 1046

    Abstract: The development of bacterial resistance is an insistent global health care issue, especially in light of the dwindled supply of new antimicrobial agents. This mandates the development of new innovative approaches to overcome the resistance development ... ...

    Abstract The development of bacterial resistance is an insistent global health care issue, especially in light of the dwindled supply of new antimicrobial agents. This mandates the development of new innovative approaches to overcome the resistance development obstacle. Mitigation of bacterial virulence is an interesting approach that offers multiple advantages. Employing safe chemicals or drugs to mitigate bacterial virulence is an additive advantage. In the current study, the in vitro antivirulence activities of citrate were evaluated. Significantly, sodium citrate inhibited bacterial biofilm formation at sub-MIC concentrations. Furthermore, sodium citrate decreased the production of virulence factors protease and pyocyanin and diminished bacterial motility. Quorum sensing (QS) is the communicative system that bacterial cells utilize to communicate with each other and regulate the virulence of the host cells. In the present study, citrate in silico blocked the Pseudomonas QS receptors and downregulated the expression of QS-encoding genes. In conclusion, sodium citrate showed a significant ability to diminish bacterial virulence in vitro and interfered with QS; it could serve as a safe adjuvant to traditional antibiotic treatment for aggressive resistant bacterial infections such as Pseudomonas aeruginosa infections.
    Keywords Pseudomonas aeruginosa ; sodium citrate ; bacterial virulence ; quorum sensing ; bacterial resistance ; industrial developments ; Biology (General) ; QH301-705.5
    Subject code 572
    Language English
    Publishing date 2022-05-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: The impact of the “Brain Drain” involving Saudi physicians

    Marya Alsuhaibani / Amjad Alharbi / Saleh K Alqaryan / Turki Aldress / Majed Alharbi / Sami Alharethy

    Journal of Nature and Science of Medicine, Vol 1, Iss 2, Pp 69-

    A cross-sectional study

    2018  Volume 73

    Abstract: Objectives: This study aimed to elucidate the brain drain phenomenon involving Saudi medical students by assessing their characteristics and intentions and related factors. Materials and Methods: A cross-sectional survey-based study conducted at Qassim ... ...

    Abstract Objectives: This study aimed to elucidate the brain drain phenomenon involving Saudi medical students by assessing their characteristics and intentions and related factors. Materials and Methods: A cross-sectional survey-based study conducted at Qassim University, Saudi Arabia. The subjects included 150 prefinal or final year medical students, who completed a modified version of a questionnaire developed by Akl et al. Results: Ninety-six students intended to study abroad with 48 and 33 planning to study in Canada and the USA, respectively. Country preference differed according to class ranking, and 69% and 33.3% of students in the top and bottom thirds of the class intended to study in Canada (P = 0.047). Male students were more likely to express the intention to study abroad. However, women were significantly more likely to remain abroad relative to males (P < 0.001). The only factor associated with intention to study abroad was the year of study and those in the final year were 60% less likely to express an intention to study abroad relative to those in prefinal years (P = 0.012). Conclusion: Most of our individuals intended to study abroad. It was varied according to gender differences. The primarily destination is Canada. This could present a challenge in meeting the high demand for staff in the health-care service in Saudi Arabia and exacerbate the current shortage of physicians in future.
    Keywords brain drain ; medical student ; training abroad ; Medicine ; R ; Public aspects of medicine ; RA1-1270
    Language English
    Publishing date 2018-01-01T00:00:00Z
    Publisher Wolters Kluwer Medknow Publications
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Smartphones and professionalism

    Saleh Alqaryan / Mohannad Alkhalifa / Majed Alharbi / Somaya Alabaishi / Turki Aldrees

    International Journal of Medical Research and Health Sciences, Vol 5, Iss 9, Pp 198-

    A cross-sectional study on interns and final-year medical students

    2016  Volume 202

    Abstract: The smartphone is a powerful tool that can be used to improve the health care system as long as certain checks and balances are implemented. It is commonly used by health care providers and medical students. A cross-sectional study conducted at Qassim ... ...

    Abstract The smartphone is a powerful tool that can be used to improve the health care system as long as certain checks and balances are implemented. It is commonly used by health care providers and medical students. A cross-sectional study conducted at Qassim University, Saudi Arabia. Final-year medical students and interns were included. A survey was distributed and divided into three sections: personal technology, experiences of using smartphones during clinical rotations, and attitudes about the usage of smartphones for clinical work. A total of 156 interns and students participated in the study. All of them owned a smartphone. Three-quarters of the respondents used their mobile for personal purposes, while 71.2% used them to look up medical references and resources. Respondents also used personal mobiles to keep in contact with team members regarding patient- (29.5%) and non-patientrelated issues (26.3%). Some 16% of participants did not have any security features on their smartphones. Over half the participants did not get proper instructions about using their smartphones from either their medical college or senior residents or consultants. There is a lot to be done in this area, as certain regulations need to be carried out to lead toward a world that is pro-technology, health centered, and safe.
    Keywords Smartphones ; Medical Education ; technology ; professionalism ; Medical Students ; Medicine ; R ; Medicine (General) ; R5-920
    Language English
    Publishing date 2016-09-01T00:00:00Z
    Publisher Sumathi Publications
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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