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A Self-Nanoemulsifying Drug Delivery System for Enhancing the Oral Bioavailability of Candesartan Cilexetil: Ex Vivo and In Vivo Evaluation

Research Abstract
The drug delivery of candesartan cilexetil encounters an obstacle of low absolute oral bioavailability which is attributed mainly to its low aqueous solubility and efflux by intestinal P-glycoprotein (P-gp) transporters. However, the extent of P-gp contribution in the reduced oral bioavailability of candesartan cilexetil is not clear. In this study, a previously developed candesartan cilexetil-loaded self-nanoemulsifying drug delivery system (SNEDDS) was evaluated for its ability to increase the drug oral bioavailability via the inhibition of intestinal P-gp transporters. Despite the developed SNEDDS showing P-gp inhibition activity, P-gp-mediated efflux was found to have a minor role in the reduced oral bioavailability of candesartan cilexetil. On the other hand, the high surfactant concentration used in SNEDDS formulation represents a major challenge toward their widespread application especially for chronically administered drugs. The designed acute and subacute toxicity studies revealed that the degree of intestinal mucosal damage decreases as the treatment period increases. The latter observation was attributed to the reversibility of surfactant-induced mucosal damage. Thus, the developed SNEDDS could be considered as a promising delivery system for enhancing the oral bioavailability of chronically administered drugs.
Research Authors
Khaled AboulFotouh, Ayat A. Allam, Mahmoud El-Badry, Ahmed M. El-Sayed
Research Department
Research Journal
Journal of Pharmaceutical Sciences
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 108
Research Website
https://doi.org/10.1016/j.xphs.2019.07.004
Research Year
2019

A Self-Nanoemulsifying Drug Delivery System for Enhancing the Oral Bioavailability of Candesartan Cilexetil: Ex Vivo and In Vivo Evaluation

Research Abstract
The drug delivery of candesartan cilexetil encounters an obstacle of low absolute oral bioavailability which is attributed mainly to its low aqueous solubility and efflux by intestinal P-glycoprotein (P-gp) transporters. However, the extent of P-gp contribution in the reduced oral bioavailability of candesartan cilexetil is not clear. In this study, a previously developed candesartan cilexetil-loaded self-nanoemulsifying drug delivery system (SNEDDS) was evaluated for its ability to increase the drug oral bioavailability via the inhibition of intestinal P-gp transporters. Despite the developed SNEDDS showing P-gp inhibition activity, P-gp-mediated efflux was found to have a minor role in the reduced oral bioavailability of candesartan cilexetil. On the other hand, the high surfactant concentration used in SNEDDS formulation represents a major challenge toward their widespread application especially for chronically administered drugs. The designed acute and subacute toxicity studies revealed that the degree of intestinal mucosal damage decreases as the treatment period increases. The latter observation was attributed to the reversibility of surfactant-induced mucosal damage. Thus, the developed SNEDDS could be considered as a promising delivery system for enhancing the oral bioavailability of chronically administered drugs.
Research Authors
Khaled AboulFotouh, Ayat A. Allam, Mahmoud El-Badry, Ahmed M. El-Sayed
Research Department
Research Journal
Journal of Pharmaceutical Sciences
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 108
Research Website
https://doi.org/10.1016/j.xphs.2019.07.004
Research Year
2019

A Self-Nanoemulsifying Drug Delivery System for Enhancing the Oral Bioavailability of Candesartan Cilexetil: Ex Vivo and In Vivo Evaluation

Research Abstract
The drug delivery of candesartan cilexetil encounters an obstacle of low absolute oral bioavailability which is attributed mainly to its low aqueous solubility and efflux by intestinal P-glycoprotein (P-gp) transporters. However, the extent of P-gp contribution in the reduced oral bioavailability of candesartan cilexetil is not clear. In this study, a previously developed candesartan cilexetil-loaded self-nanoemulsifying drug delivery system (SNEDDS) was evaluated for its ability to increase the drug oral bioavailability via the inhibition of intestinal P-gp transporters. Despite the developed SNEDDS showing P-gp inhibition activity, P-gp-mediated efflux was found to have a minor role in the reduced oral bioavailability of candesartan cilexetil. On the other hand, the high surfactant concentration used in SNEDDS formulation represents a major challenge toward their widespread application especially for chronically administered drugs. The designed acute and subacute toxicity studies revealed that the degree of intestinal mucosal damage decreases as the treatment period increases. The latter observation was attributed to the reversibility of surfactant-induced mucosal damage. Thus, the developed SNEDDS could be considered as a promising delivery system for enhancing the oral bioavailability of chronically administered drugs.
Research Authors
Khaled AboulFotouh, Ayat A. Allam, Mahmoud El-Badry, Ahmed M. El-Sayed
Research Department
Research Journal
Journal of Pharmaceutical Sciences
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 108
Research Website
https://doi.org/10.1016/j.xphs.2019.07.004
Research Year
2019

Nanomedicine Fight against Antibacterial Resistance: An Overview of the Recent Pharmaceutical Innovations

Research Abstract
Based on the recent reports of World Health Organization, increased antibiotic resistance prevalence among bacteria represents the greatest challenge to human health. In addition, the poor solubility, stability, and side effects that lead to inefficiency of the current antibacterial therapy prompted the researchers to explore new innovative strategies to overcome such resilient microbes. Hence, novel antibiotic delivery systems are in high demand. Nanotechnology has attracted considerable interest due to their favored physicochemical properties, drug targeting efficiency, enhanced uptake, and biodistribution. The present review focuses on the recent applications of organic (liposomes, lipid-based nanoparticles, polymeric micelles, and polymeric nanoparticles), and inorganic (silver, silica, magnetic, zinc oxide (ZnO), cobalt, selenium, and cadmium) nanosystems in the domain of antibacterial delivery. We provide a concise description of the characteristics of each system that render it suitable as an antibacterial delivery agent. We also highlight the recent promising innovations used to overcome antibacterial resistance, including the use of lipid polymer nanoparticles, nonlamellar liquid crystalline nanoparticles, anti-microbial oligonucleotides, smart responsive materials, cationic peptides, and natural compounds. We further discuss the applications of antimicrobial photodynamic therapy, combination drug therapy, nano antibiotic strategy, and phage therapy, and their impact on evading antibacterial resistance. Finally, we report on the formulations that made their way towards clinical application.
Research Authors
Nermin E. Eleraky , Ayat Allam , Sahar B. Hassan and Mahmoud M. Omar
Research Department
Research Journal
Pharmaceutics, doi:10.3390/pharmaceutics12020142
Research Member
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 12, Article 142
Research Website
NULL
Research Year
2020

Nanomedicine Fight against Antibacterial Resistance: An Overview of the Recent Pharmaceutical Innovations

Research Abstract
Based on the recent reports of World Health Organization, increased antibiotic resistance prevalence among bacteria represents the greatest challenge to human health. In addition, the poor solubility, stability, and side effects that lead to inefficiency of the current antibacterial therapy prompted the researchers to explore new innovative strategies to overcome such resilient microbes. Hence, novel antibiotic delivery systems are in high demand. Nanotechnology has attracted considerable interest due to their favored physicochemical properties, drug targeting efficiency, enhanced uptake, and biodistribution. The present review focuses on the recent applications of organic (liposomes, lipid-based nanoparticles, polymeric micelles, and polymeric nanoparticles), and inorganic (silver, silica, magnetic, zinc oxide (ZnO), cobalt, selenium, and cadmium) nanosystems in the domain of antibacterial delivery. We provide a concise description of the characteristics of each system that render it suitable as an antibacterial delivery agent. We also highlight the recent promising innovations used to overcome antibacterial resistance, including the use of lipid polymer nanoparticles, nonlamellar liquid crystalline nanoparticles, anti-microbial oligonucleotides, smart responsive materials, cationic peptides, and natural compounds. We further discuss the applications of antimicrobial photodynamic therapy, combination drug therapy, nano antibiotic strategy, and phage therapy, and their impact on evading antibacterial resistance. Finally, we report on the formulations that made their way towards clinical application.
Research Authors
Nermin E. Eleraky , Ayat Allam , Sahar B. Hassan and Mahmoud M. Omar
Research Department
Research Journal
Pharmaceutics, doi:10.3390/pharmaceutics12020142
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 12, Article 142
Research Website
NULL
Research Year
2020

Nanomedicine Fight against Antibacterial Resistance: An Overview of the Recent Pharmaceutical Innovations

Research Abstract
Based on the recent reports of World Health Organization, increased antibiotic resistance prevalence among bacteria represents the greatest challenge to human health. In addition, the poor solubility, stability, and side effects that lead to inefficiency of the current antibacterial therapy prompted the researchers to explore new innovative strategies to overcome such resilient microbes. Hence, novel antibiotic delivery systems are in high demand. Nanotechnology has attracted considerable interest due to their favored physicochemical properties, drug targeting efficiency, enhanced uptake, and biodistribution. The present review focuses on the recent applications of organic (liposomes, lipid-based nanoparticles, polymeric micelles, and polymeric nanoparticles), and inorganic (silver, silica, magnetic, zinc oxide (ZnO), cobalt, selenium, and cadmium) nanosystems in the domain of antibacterial delivery. We provide a concise description of the characteristics of each system that render it suitable as an antibacterial delivery agent. We also highlight the recent promising innovations used to overcome antibacterial resistance, including the use of lipid polymer nanoparticles, nonlamellar liquid crystalline nanoparticles, anti-microbial oligonucleotides, smart responsive materials, cationic peptides, and natural compounds. We further discuss the applications of antimicrobial photodynamic therapy, combination drug therapy, nano antibiotic strategy, and phage therapy, and their impact on evading antibacterial resistance. Finally, we report on the formulations that made their way towards clinical application.
Research Authors
Nermin E. Eleraky , Ayat Allam , Sahar B. Hassan and Mahmoud M. Omar
Research Department
Research Journal
Pharmaceutics, doi:10.3390/pharmaceutics12020142
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 12, Article 142
Research Website
NULL
Research Year
2020

A Determination Approach for Rivastigmine by Lepidocrocite Nanoparticles Supported on N-Chitosan Carbon Nanosheets/Anti-Fouling PAS: Application to Biosensing

Research Abstract
In the present work, a triple amplified biosensor was constructed for ultrasensitive and selective analysis of an acetylcholinesterase inhibitor; rivastigmine (RIV) in human serum. The modified biosensor based on fabrication of pencil graphite electrode (PGE) with lepidocrocite nanoparticles (γ-FeOOH) dispersed in N-chitosan carbon nanosheets (N@CCNS). Pyrrolidinium acid sulfate (PAS) as an ionic liquid was added to amplify the signal of RIV. The physical properties of the modified electrodes were characterized by powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM) and energy dispersive X-ray (EDX) spectroscopy. The cyclic voltammetry (CV), differential pulse voltammetry (DPV) and electrochemical impedance spectroscopy (EIS) were used to evaluate the performance of the modified electrode. Parameters affecting performance of the modified sensor were evaluated such as pH, scan rate, casting volume, concentration of nanocomposite …etc. The modified sensor showed a fast and sensitive electrochemical response to RIV sensing with wide linear range (3.0–90.0 nM), low detection limit (0.99 nM) and excellent anti-interference ability. Moreover, the fabricated sensor was successfully applied for determination of RIV in pharmaceutical tablets and spiked human serum and the obtained results are quite satisfactory.
Research Authors
Fardous A. Mohamed, Pakinaz Y. Khashaba, Reem Y. Shahin and Mohamed M. El-Wekil
Research Journal
Journal of The Electrochemical Society, DOI: 10.1149/2.0961902jes
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 166, No. 2
Research Website
NULL
Research Year
2019

A Determination Approach for Rivastigmine by Lepidocrocite Nanoparticles Supported on N-Chitosan Carbon Nanosheets/Anti-Fouling PAS: Application to Biosensing

Research Abstract
In the present work, a triple amplified biosensor was constructed for ultrasensitive and selective analysis of an acetylcholinesterase inhibitor; rivastigmine (RIV) in human serum. The modified biosensor based on fabrication of pencil graphite electrode (PGE) with lepidocrocite nanoparticles (γ-FeOOH) dispersed in N-chitosan carbon nanosheets (N@CCNS). Pyrrolidinium acid sulfate (PAS) as an ionic liquid was added to amplify the signal of RIV. The physical properties of the modified electrodes were characterized by powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM) and energy dispersive X-ray (EDX) spectroscopy. The cyclic voltammetry (CV), differential pulse voltammetry (DPV) and electrochemical impedance spectroscopy (EIS) were used to evaluate the performance of the modified electrode. Parameters affecting performance of the modified sensor were evaluated such as pH, scan rate, casting volume, concentration of nanocomposite …etc. The modified sensor showed a fast and sensitive electrochemical response to RIV sensing with wide linear range (3.0–90.0 nM), low detection limit (0.99 nM) and excellent anti-interference ability. Moreover, the fabricated sensor was successfully applied for determination of RIV in pharmaceutical tablets and spiked human serum and the obtained results are quite satisfactory.
Research Authors
Fardous A. Mohamed, Pakinaz Y. Khashaba, Reem Y. Shahin and Mohamed M. El-Wekil
Research Journal
Journal of The Electrochemical Society, DOI: 10.1149/2.0961902jes
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 166, No. 2
Research Website
NULL
Research Year
2019

A Determination Approach for Rivastigmine by Lepidocrocite Nanoparticles Supported on N-Chitosan Carbon Nanosheets/Anti-Fouling PAS: Application to Biosensing

Research Abstract
In the present work, a triple amplified biosensor was constructed for ultrasensitive and selective analysis of an acetylcholinesterase inhibitor; rivastigmine (RIV) in human serum. The modified biosensor based on fabrication of pencil graphite electrode (PGE) with lepidocrocite nanoparticles (γ-FeOOH) dispersed in N-chitosan carbon nanosheets (N@CCNS). Pyrrolidinium acid sulfate (PAS) as an ionic liquid was added to amplify the signal of RIV. The physical properties of the modified electrodes were characterized by powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM) and energy dispersive X-ray (EDX) spectroscopy. The cyclic voltammetry (CV), differential pulse voltammetry (DPV) and electrochemical impedance spectroscopy (EIS) were used to evaluate the performance of the modified electrode. Parameters affecting performance of the modified sensor were evaluated such as pH, scan rate, casting volume, concentration of nanocomposite …etc. The modified sensor showed a fast and sensitive electrochemical response to RIV sensing with wide linear range (3.0–90.0 nM), low detection limit (0.99 nM) and excellent anti-interference ability. Moreover, the fabricated sensor was successfully applied for determination of RIV in pharmaceutical tablets and spiked human serum and the obtained results are quite satisfactory.
Research Authors
Fardous A. Mohamed, Pakinaz Y. Khashaba, Reem Y. Shahin and Mohamed M. El-Wekil
Research Journal
Journal of The Electrochemical Society, DOI: 10.1149/2.0961902jes
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 166, No. 2
Research Website
NULL
Research Year
2019

Spectrodensitometric Determination of Rivastigmine After Vortex Assisted Magnetic Solid Phase Extraction

Research Abstract
A highly sensitive and cost-effective HPTLC method was developed for the determination of rivastigmine hydrogen tartarate (RIV) in bulk and capsules. Moreover, magnetic solid phase extraction procedure (MSPE) was performed for analysis of RIV in human plasma to preconcentrate RIV and decrease interference from plasma constituents. The magnetic nanoparticles (MNPs) were prepared by co-precipitation process and characterized by scanning electron microscope (SEM), Fourier transform infrared spectroscopy (FTIR), powdered X-ray diffraction (PXRD) and dynamic light scattering (DLS). These prepared MNPs have shown high extraction efficiency and all parameters affecting the adsorption of RIV on the MNPs were fully investigated. The method was validated according to FDA bio-analytical guidelines and was found to be linear over the range of 30.2–648 ng/spot. The LLOQ and LOD were 26.2 and 8.6 ng/spot, respectively.
Research Authors
Fardous A.Mohamed, Pakinaz Y.Khashaba, Mohamed M.El-Wekil, Reem Y.Shahin
Research Journal
Microchemical Journal
Research Publisher
Elsevier
Research Rank
1
Research Vol
Vol. 147
Research Website
https://doi.org/10.1016/j.microc.2019.03.085
Research Year
2019
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