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Fulltext The beta Burr type X distribution properties with application

Merovci F, Khaleel MA, Ibrahim NA, Shitan M

Springerplus, 2016;5(1):697.
PMID: 27347471 DOI: 10.1186/s40064-016-2271-9

We develop a new continuous distribution called the beta-Burr type X distribution that extends the Burr type X distribution. The properties provide a comprehensive mathematical treatment of this distribution. Further more, various structural properties of the new distribution are derived, that includes moment generating function and the rth moment thus generalizing some results in the literature. We also obtain expressions for the density, moment generating function and rth moment of the order statistics. We consider the maximum likelihood estimation to estimate the parameters. Additionally, the asymptotic confidence intervals for the parameters are derived from the Fisher information matrix. Finally, simulation study is carried at under varying sample size to assess the performance of this model. Illustration the real dataset indicates that this new distribution can serve as a good alternative model to model positive real data in many areas.
Fulltext Curation of an international drug proprietary names dataset

Khaleel MA, Khan AH, Ghadzi SMS, Alshakhshir S

Data Brief, 2022 Feb;40:107701.
PMID: 34988273 DOI: 10.1016/j.dib.2021.107701

A drug dataset containing international proprietary names is essential for researchers investigating different drugs from different countries worldwide. However, many websites on the internet offer free access for a single drug searching service to identify international drug trade names, but not for a list of drugs to be searched and identified. Therefore, it will be problematic if the researcher has a list of hundreds or thousands of drug trade names to be identified. In this project, we have created an International Drug Dictionary (IDD) by curating collected drug lists from open access websites belonging to official drug regulatory agencies, official healthcare systems, or recognized scientific bodies from 44 countries around the world in addition to the European public assessment reports (EPAR) and the DRUGBANK vocabulary published in the public domain. Researchers interested in pharmacovigilance, pharmacoepidemiology, or pharmacoeconomics can benefit from this dataset, especially when identifying lists of proprietary drug names, particularly of multi-national origin. To enhance its adaptability, we also mapped the IDD to the standardized drug vocabulary RxNorm. The IDD can also be used as a tool for mapping international drug trade names to RxNorm. Each drug entity in the IDD mapped to a unique identification number for each entity called Atom Unique Identifier (RXAUI) from RxNorm.
Natamycin solid lipid nanoparticles - sustained ocular delivery system of higher corneal penetration against deep fungal keratitis: preparation and optimization

Khames A, Khaleel MA, El-Badawy MF, El-Nezhawy AOH

Int J Nanomedicine, 2019;14:2515-2531.
PMID: 31040672 DOI: 10.2147/IJN.S190502

Background: Fungal keratitis (FK) is a serious pathogenic condition usually associated with significant ocular morbidity. Natamycin (NAT) is the first-line and only medication approved by the Food and Drug Administration for the treatment of FK. However, NAT suffers from poor corneal penetration, which limits its efficacy for treating deep keratitis.
Purpose: The objective of this work was to prepare NAT solid lipid nanoparticles (NAT-SLNs) to achieve sustained drug release and increased corneal penetration.
Methods: NAT-SLNs were prepared using the emulsification-ultrasonication technique. Box- Behnken experimental design was applied to optimize the effects of independent processing variables (lipid concentration [X1], surfactant concentration [X2], and sonication frequency [X3]) on particle size (R1), zeta potential (ZP; R2), and drug entrapment efficiency (EE%) (R3) as responses. Drug release profile, ex vivo corneal permeation, antifungal susceptibility, and cytotoxicity of the optimized formula were evaluated.
Results: The optimized formula had a mean particle size of 42 r.nm (radius in nanometers), ZP of 26 mV, and EE% reached ~85%. NAT-SLNs showed an extended drug release profile of 10 hours, with enhanced corneal permeation in which the apparent permeability coefficient (Papp) and steady-state flux (Jss) reached 11.59×10-2 cm h-1 and 3.94 mol h-1, respectively, in comparison with 7.28×10-2 cm h-1 and 2.48 mol h-1 for the unformulated drug, respectively. Antifungal activity was significantly improved, as indicated by increases in the inhibition zone of 8 and 6 mm against Aspergillus fumigatus ATCC 1022 and a Candida albicans clinical isolate, respectively, and minimum inhibitory concentration values that were decreased 2.5-times against both of these pathogenic strains. NAT-SLNs were found to be non-irritating to corneal tissue. NAT-SLNs had a prolonged drug release rate, that improved corneal penetration, and increased antifungal activity without cytotoxic effects on corneal tissues.
Conclusion: Thus, NAT-SLNs represent a promising ocular delivery system for treatment of deep corneal keratitis.
Fulltext Sesame Oil-Based Nanostructured Lipid Carriers of Nicergoline, Intranasal Delivery System for Brain Targeting of Synergistic Cerebrovascular Protection

Abourehab MAS, Khames A, Genedy S, Mostafa S, Khaleel MA, Omar MM, et al.

Pharmaceutics, 2021 Apr 19;13(4).
PMID: 33921796 DOI: 10.3390/pharmaceutics13040581

Nicergoline (NIC) is a semisynthetic ergot alkaloid derivative applied for treatment of dementia and other cerebrovascular disorders. The efficacy of sesame oil to slow and reverse the symptoms of neurodegenerative cognitive disorders has been proven. This work aimed to formulate and optimize sesame oil-based NIC-nanostructured lipid carriers (NIC-NLCs) for intranasal (IN) delivery with expected synergistic and augmented neuroprotective properties. The NIC-NLC were prepared using sesame oil as a liquid lipid. A three-level, three-factor Box-Behnken design was applied to statistically optimize the effect of sesame oil (%) of the total lipid, surfactant concentration, and sonication time on particle size, zeta potential, and entrapment efficacy as responses. Solid-state characterization, release profile, and ex vivo nasal permeation in comparison to NIC solution (NIC-SOL) was studied. In vivo bioavailability from optimized NIC-NLC and NIC-SOL following IN and IV administration was evaluated and compared. The optimized NIC-NLC formula showed an average particle size of 111.18 nm, zeta potential of -15.4 mV, 95.11% entrapment efficacy (%), and 4.6% loading capacity. The NIC-NLC formula showed a biphasic, extended-release profile (72% after 48 h). Permeation of the NIC-NLC formula showed a 2.3 enhancement ratio. Bioavailability studies showed a 1.67 and 4.57 fold increase in plasma and brain following IN administration. The results also indicated efficient direct nose-to-brain targeting properties with the brain-targeting efficiency (BTE%) and direct transport percentage (DTP%) of 187.3% and 56.6%, respectively, after IN administration. Thus, sesame oil-based NIC-NLC can be considered as a promising IN delivery system for direct and efficient brain targeting with improved bioavailability and expected augmented neuroprotective action for the treatment of dementia.