Publications by authors named "Yasser A Hassan"

4 Publications

  • Page 1 of 1

Co-delivery of imidazolium Zn(II)salen and Origanum Syriacum essential oil by shrimp chitosan nanoparticles for antimicrobial applications.

Carbohydr Polym 2021 May 18;260:117834. Epub 2021 Feb 18.

Department of Pharmaceutics, Faculty of Pharmacy, Port Said University, 42526, Port Said, Egypt.

This study reports preparation and physicochemical characterization of natural antimicrobials (Origanum Syriacum essential oil (OSEO), shrimp chitosan nanoparticles (CSNPs)) and new imidazolium ionic liquid-supported Zn(II)Salen. These antimicrobials were separately or co-encapsulated by CSNPs to fabricate novel antimicrobial nanoplatforms "NPFs" (OSEO-loaded CSNPs (NPF-1), Zn(II)Salen-loaded CSNPs (NPF-2), and Zn(II)[email protected] CSNPs (NPF-3)). The finding of loading, encapsulation, and antimicrobial release studies confirm the suitability of CSNPs for nanoencapsulation of Zn(II)Salen and OSEO. All NPFs can significantly suppress the growth of microbial species with performances dependent upon the microbial strain and nanoplatform concentration. The susceptibility of microbes toward new antimicrobials was as follows; Gram-positive bacteria > Gram-negative bacteria > fungi. The amazing physicochemical features of new nanoplatforms and their bioactive ingredients (Zn(II)Salen, OSEO, and CSNPs) signify the importance of our designs for developing a new generation of nanopharmaceuticals supported both natural products and biogenic ionic metal cofactors, targeting the multidrug resistant (MDR) pathogens.
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http://dx.doi.org/10.1016/j.carbpol.2021.117834DOI Listing
May 2021

Enhancing the Low Oral Bioavailability of Sulpiride via Fast Orally Disintegrating Tablets: Formulation, Optimization and In Vivo Characterization.

Pharmaceuticals (Basel) 2020 Dec 5;13(12). Epub 2020 Dec 5.

Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi Arabia.

Sulpiride (SUL) is a dopamine D-receptor antagonist used for management of GIT disturbance and it has anti-psychotic activities based on the administered dose. SUL undergoes P-glycoprotein efflux, which lead to poor bioavailability and erratic absorption. Therefore, the objective of this research was an attempt to enhance the oral bioavailability of SUL via formulation of fast disintegrating tablets (SUL-FDTs) with a rapid onset of action. A 3 full-factorial design was performed for optimization of SUL-FDTs using desirability function. The concentration of superdisintegrant (X) and Prosolv (X) were selected as independent formulation variables for the preparation and optimization of SUL-FDTs using direct compression technique. The prepared SUL-FDTs were investigated regarding their mechanical strength, disintegration time, drug release and in vivo pharmacokinetic analysis in rabbits. The optimized formulation has hardness of 4.58 ± 0.52 KP, friability of 0.73 ± 0.158%, disintegration time of 37.5 ± 1.87 s and drug release of 100.51 ± 1.34% after 30 min. In addition, the optimized SUL-FDTs showed a significant ( < 0.01) increase in C and AUC() and a relative bioavailability of about 9.3 fold compared to the commercial product. It could be concluded that SUL-FDTs are a promising formulation for enhancing the oral bioavailability of SUL concomitant with a fast action.
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http://dx.doi.org/10.3390/ph13120446DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7762047PMC
December 2020

Radioiodination and in vivo assessment of the potential of newly synthesized pyrrolizine-5-carboxamides derivative in tumor model.

Appl Radiat Isot 2020 Dec 8;166:109369. Epub 2020 Aug 8.

Labeled Compounds Dept. Hot Labs Center, Atomic Energy Authority, Cairo, Egypt; Faculty of Pharmacy, Albayan University, Baghdad, Iraq.

Recently, pyrrolizine derivatives have been reported to possess numerous anticancer activities. In a previous study, (EZ)-6-((4-chlorobenzylidene)-amino)-7-cyano-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine carboxamide (EZPCA) compound was synthesized and the cytotoxic activity of EZPCA toward COX-2 enzyme (overexpressed in cancer cells) was reported. In order to assess the suitability of this compound as a promising pilot structure for in vivo applications, EZPCA was radiolabeled with radioiodine-131 (I) and various factors affecting radiolabeling process were studied. Quality control studies of [I]iodo-EZPCA were performed using paper chromatography and HPLC was used as a co-chromatographic technique for confirming the radiochemical yield. Biodistribution studies of [I]iodo-EZPCA were undertaken in normal and tumor bearing mice. The radiochemical yield percentage of [I]iodo-EZPCA was 94.20 ± 0.12%. The biodistribution results showed evident tumor uptake of [I]iodo-EZPCA with promising target/non-target (T/NT) ratios. As a conclusion, these data suggest that [I]iodo-EZPCA had high binding efficiency, high tumor uptake and sufficient stability to be used be used in diagnostic studies.
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http://dx.doi.org/10.1016/j.apradiso.2020.109369DOI Listing
December 2020

Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization.

AAPS PharmSciTech 2018 May 12;19(4):1712-1719. Epub 2018 Mar 12.

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.

Domperidone (DOP) is extensively applied orally in the management of nausea and vomiting. Upon oral administration, its bioavailability is very poor due to its poor solubility in alkaline media. Therefore, the aim of this work was to investigate DOP-loaded solid lipid nanoparticles (DOP-SLNs) in order to sustain its release pattern and to enhance oral bioavailability. DOP-SLNs were prepared using four different lipids. Prepared DOP-SLNs were characterized for "polydispersity index (PDI), particle size, zeta potential, % entrapment efficiency (% EE), and drug release behavior." Differential scanning calorimetry (DSC) study was carried out to illustrate the physical form of DOP and excipients. The morphology of DOP-SLNs was confirmed by scanning electron microscopy (SEM). Pharmacokinetic study on optimized DOP-SLN in comparison to tablet was performed in rats. The "particle size, PDI, zeta potential, and % EE" of optimized formulation (F5) were recorded as 201.4 nm, 0.071, - 6.2 mV, and 66.3%, respectively. DSC thermograms suggested amorphous state of DOP in various SLNs. Surface morphology of SLNs using SEM suggested spherical shape of the nanoparticles within nanometer size range. In vitro release studies confirmed that all SLN formulations possessed a sustained release over a period of 12 h (51.3% from optimized formulation) in comparison with immediate release from conventional tablets (100% after 90 min). Pharmacokinetic study showed significant enhancement in oral absorption of DOP from optimized SLN in comparison with DOP tablet. The enhancement in relative bioavailability of DOP from optimized SLN was 2.62-fold in comparison with DOP tablet.
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http://dx.doi.org/10.1208/s12249-018-0987-2DOI Listing
May 2018