11 results on '"Anwer, Md. Khalid"'
Search Results
2. A Validated UPLC-MS/MS Method for Rapid Quantification of Umifenovir in Plasma Samples and Its Greenness Assessment.
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Iqbal, Muzaffar, Imam, Faisal, Ali, Essam A., Kalam, Mohd Abul, Alhudaithi, Sulaiman S., and Anwer, Md. Khalid
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COVID-19 treatment ,VIRUS diseases ,AMMONIUM acetate ,COMPOSITE columns ,BIOAVAILABILITY ,DRUGS - Abstract
Umifenovir is one of the most often prescribed antiviral medications for the prevention and treatment of COVID-19 and other viral infections. Herein, a UPLC-MS/MS method is developed through using ibrutinib as an internal standard (IS) for quantifying umifenovir in plasma samples. Both umifenovir and the IS were analytically separated on an Acquity BEH C18 column with a total run time of only 2.5 min. At a flow rate of 0.3 mLmin
−1 , acetonitrile:15 mM ammonium acetate (80:20) was employed as the mobile phase composition. Electrospray ionization in positive mode was used for ionization of the samples. Detection and quantification were performed in multiple reaction monitoring mode with parent-to-daughter ionization of 477.05 → 279.02 and 441.16 → 84.4 for umifenovir and the IS, respectively. The method was validated through following international guidelines for bioanalytical method validation, and all parameters were within the acceptable limits. Moreover, the eco-scale method using AGREE software was used for the evaluation of greenness, and results showed that the method is very environmentally friendly. The validated assay was successfully employed in the bioavailability assessment of a newly developed formulation of kneaded ternary umifenovir/β-cyclodextrin with 1% poloxamer 188 (KDB). [ABSTRACT FROM AUTHOR]- Published
- 2023
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3. Molecular complexes of aspirin with humic acid extracted from shilajit and their characterization
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Anwer, Md. Khalid, Agarwal, Suraj P., Ali, Asgar, and Sultana, Yasmin
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- 2010
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4. Development of Chitosan-Coated PLGA-Based Nanoparticles for Improved Oral Olaparib Delivery: In Vitro Characterization, and In Vivo Pharmacokinetic Studies.
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Anwer, Md. Khalid, Ali, Essam A., Iqbal, Muzaffar, Ahmed, Mohammed Muqtader, Aldawsari, Mohammed F., Saqr, Ahmed Al, Alalaiwe, Ahmed, and Soliman, Gamal A.
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OLAPARIB ,PHARMACOKINETICS ,PANCREATIC enzymes ,ADP-ribosylation ,NANOPARTICLES ,ENZYME inhibitors ,OVARIAN cancer - Abstract
Olaparib (OLP) is an orally active poly (ADP-ribose) polymerase enzyme inhibitor, approved for treatment for the metastatic stage of prostate, pancreatic, breast and ovarian cancer. Due to its low bioavailability, an increase in dose and frequency is required to achieve therapeutic benefits, which also results in associated toxicity in patients. In the current study, OLP-loaded poly (d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) (OLP-PLGA NPs) and a coating of OLP-PLGA NPs with chitosan (CS) (OLP-CS-PLGA NPs) were prepared successfully in order to improve the dissolution rate and bioavailability. The developed OLP-PLGA NPs were evaluated for hydrodynamic particle size (392 ± 5.3 nm), PDI (0.360 ± 0.03), ZP (−26.9 ± 2.1 mV), EE (71.39 ± 5.5%) and DL (14.86 ± 1.4%), and OLP-CS-PLGA NPs, hydrodynamic particle size (622 ± 9.5 nm), PDI (0.321 ± 0.02), ZP (+36.0 ± 1.7 mV), EE (84.78 ± 6.3%) and DL (11.05 ± 2.6%). The in vitro release profile of both developed NPs showed a sustained release pattern. Moreover, the pharmacokinetics results exhibited a 2.0- and 4.75-fold increase in the bioavailability of OLP-PLGA NPs and OLP-CS-PLGA NPs, respectively, compared to normal OLP suspension. The results revealed that OLP-CS-PLGA NPs could be an effective approach to sustaining and improving the bioavailability of OLP. [ABSTRACT FROM AUTHOR]
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- 2022
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5. Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
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Anwer, Md Khalid, Mohammad, Muqtader, Ezzeldin, Essam, Fatima, Farhat, Alalaiwe, Ahmed, and Iqbal, Muzaffar
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Male ,Drug Carriers ,Calorimetry, Differential Scanning ,Static Electricity ,education ,apremilast ,Poly(D,L-lactide-coglycolide) ,Thalidomide ,Drug Liberation ,Kinetics ,Polylactic Acid-Polyglycolic Acid Copolymer ,X-Ray Diffraction ,International Journal of Nanomedicine ,Delayed-Action Preparations ,Spectroscopy, Fourier Transform Infrared ,Animals ,Nanoparticles ,sustained release ,Particle Size ,Rats, Wistar ,bioavailability ,Original Research - Abstract
Md Khalid Anwer,1 Muqtader Mohammad,1 Essam Ezzeldin,2,3 Farhat Fatima,1 Ahmed Alalaiwe,1 Muzaffar Iqbal2,3 1Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia; 2Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 3Bioavailability Laboratory, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia Background: Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods: In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results: The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of -43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion: Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment. Keywords: apremilast, Poly(D,L-lactide-coglycolide), nanoparticles, bioavailability, sustained release
- Published
- 2019
6. Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats.
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Ansari, Mohammad Javed, Anwer, Md. Khalid, Jamil, Shahid, Al-Shdefat, Ramadan, Ali, Bahaa E., Ahmad, Mohammad Muqtader, and Ansari, Mohammad Nazam
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RAT diseases , *TREATMENT of diabetes , *NANOPARTICLES analysis , *BIOAVAILABILITY ,INSULIN pharmacokinetics - Abstract
Objective: Insulin is a hormone used in the treatment of diabetes mellitus. Multiple injections of insulin every day may causes pain, allergic reactions at injection site, which lead to low patient compliance. The aim of this work was to develop and evaluate an efficient solid lipid nanoparticle (SLN) carrier for oral delivery of insulin. Methods: SLNs were prepared by double emulsion solvent evaporation (w/o/w) technique, employing glyceryltrimyristate (Dynasan 114) as lipid phase and soy lecithin and polyvinyl alcohol as primary and secondary emulsifier, respectively, and evaluatedin vitrofor particle size, polydispersity index (PDI) and drug entrapment. Results: Among the eight different developed formulae (F1–F8), F7 showed an average particle size (99 nm), PDI (0.021), high entrapment of drug (56.5%). The optimized formulation (F7) was further evaluated by FT-IR, DSC, XRD,in vitrorelease, permeation, stability, bioavailability and pharmacological studies. Insulin-loaded SLNs showed better protection from gastrointestinal environment as evident from the relative bioavailability, which was enhanced five times as compared to the insulin solution. A significant enhancement of relative bioavailability of insulin was observed, i.e. approximately five times of pure insulin solution when loaded in SLN (8.26% versus 1.7% only). [ABSTRACT FROM PUBLISHER]
- Published
- 2016
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7. Proniosomal transdermal therapeutic system of losartan potassium: development and pharmacokinetic evaluation.
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Thakur, Reena, Anwer, Md Khalid, Shams, Mohammad S., Ali, Asgar, Khar, Roop K., Shakeel, Faiyaz, and Taha, Ehab I.
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POTASSIUM , *TRANSDERMAL medication , *PHARMACOKINETICS , *BIOAVAILABILITY ,PERMEABILITY of solids - Abstract
The purpose of the current study was to investigate the feasibility of proniosomes as transdermal drug delivery system for losartan potassium. Different preparations of proniosomes were fabricated using different nonionic surfactants, such as Span 20, Span 40, Span 60, Span 80, Tween 20, Tween 40, and Tween 80. Different formulae were prepared and coded as PNG-1 (proniosomal gel-1) to PNG-7. The best in vitro skin permeation profile was obtained with proniosomal formulation PNG-2 in 24 h. The permeability parameters such as flux, permeability coefficient, and enhancement ratio were significant for PNG-2 compared with other formulations ( P < 0.05). This optimized PNG-2 was fabricated in the form of transdermal patch using HPMC gel as a suitable base. Proniosomal transdermal therapeutic system (PNP-H) was found to be the optimized one as it gave better release of drug and better permeation in a steady-state manner over a desired period of time, that is, 24 h through rat skin. In vivo pharmacokinetic study of PNP-H showed a significant increase in bioavailability (1.93 times) compared with oral formulation of losartan potassium. The formulation appeared to be stable when stored at room temperature (30 ± 2°C) and at refrigeration temperature (4 ± 2°C) for 45 days. [ABSTRACT FROM AUTHOR]
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- 2009
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8. Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability.
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Anwer, Md. Khalid, Ali, Essam A., Iqbal, Muzaffar, Ahmed, Mohammed Muqtader, Aldawsari, Mohammed F., Saqr, Ahmed Al, Ansari, Mohd Nazam, and Aboudzadeh, M. Ali
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BARICITINIB , *BIOAVAILABILITY , *COVID-19 treatment , *COVID-19 , *NANOPARTICLES , *LIPIDS - Abstract
Baricitinib (BTB) is an orally administered Janus kinase inhibitor, therapeutically used for the treatment of rheumatoid arthritis. Recently it has also been approved for the treatment of COVID-19 infection. In this study, four different BTB-loaded lipids (stearin)-polymer (Poly(d,l-lactide-co-glycolide)) hybrid nanoparticles (B-PLN1 to B-PLN4) were prepared by the single-step nanoprecipitation method. Next, they were characterised in terms of physicochemical properties such as particle size, zeta potential (ζP), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Based on preliminary evaluation, the B-PLN4 was regarded as the optimised formulation with particle size (272 ± 7.6 nm), PDI (0.225), ζP (−36.5 ± 3.1 mV), %EE (71.6 ± 1.5%) and %DL (2.87 ± 0.42%). This formulation (B-PLN4) was further assessed concerning morphology, in vitro release, and in vivo pharmacokinetic studies in rats. The in vitro release profile exhibited a sustained release pattern well-fitted by the Korsmeyer–Peppas kinetic model (R2 = 0.879). The in vivo pharmacokinetic data showed an enhancement (2.92 times more) in bioavailability in comparison to the normal suspension of pure BTB. These data concluded that the formulated lipid-polymer hybrid nanoparticles could be a promising drug delivery option to enhance the bioavailability of BTB. Overall, this study provides a scientific basis for future studies on the entrapment efficiency of lipid-polymer hybrid systems as promising carriers for overcoming pharmacokinetic limitations. [ABSTRACT FROM AUTHOR]
- Published
- 2022
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9. Improving the Solubilization and Bioavailability of Arbidol Hydrochloride by the Preparation of Binary and Ternary β-Cyclodextrin Complexes with Poloxamer 188.
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Anwer, Md. Khalid, Iqbal, Muzaffar, Ahmed, Mohammad Muqtader, Aldawsari, Mohammed F., Ansari, Mohd Nazam, Ezzeldin, Essam, Khalil, Nasr Y., Ali, Raisuddin, Catenacci, Laura, Sorrenti, Milena, and Bonferoni, Maria Cristina
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STABILITY constants , *BIOAVAILABILITY , *DRUG solubility , *SOLUBILITY , *ANTIVIRAL agents , *SOLUBILIZATION , *RATS , *STOICHIOMETRY - Abstract
In the current study, the effect of poloxamer 188 on the complexation efficiency and dissolution of arbidol hydrochloride (ADL), a broad-spectrum antiviral agent, with β-cyclodextrin (β-CD) was investigated. Phase solubility studies confirmed a stoichiometry of a 1:1 ratio for both ADL:β-CD and ADL/β-CD with a 1% poloxamer 188 system with an AL type of phase solubility curve. The stability constants (K1:1) calculated from the AL type diagram were 550 M-1 and 2134 M-1 for AD:β-CD and ADL/β-CD with 1% poloxamer 188, respectively. The binary ADL/β-CD and ternary ADL/β-CD with 1% poloxamer 188 complexes were prepared by kneading and a solvent evaporation method and were characterized by aqueous solubility, FTIR, PXRD, DSC and SEM in vitro studies. The solubility (13.1 fold) and release of ADL were markedly improved in kneaded ternary ADL/β-CD with 1% poloxamer 188 (KDB). The binding affinity of ADL and β-CD was confirmed by 1H NMR and 2D ROSEY studies. The ternary complex (KDB) was further subjected for in vivo pharmacokinetic studies in rats and a significant improvement in the bioavailability (2.17 fold) was observed in comparison with pure ADL. Therefore, it can be concluded that the solubilization and bioavailability of ADL can be remarkably increased by ADL/β-CD complexation in the presence of a third component, poloxamer 188. [ABSTRACT FROM AUTHOR]
- Published
- 2021
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10. Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin.
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Anwer, Md. Khalid, Iqbal, Muzaffar, Muharram, Magdy M., Mohammad, Muqtader, Ezzeldin, Essam, Aldawsari, Mohammed F., Alalaiwe, Ahmed, and Imam, Faisal
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BIOAVAILABILITY , *ANAEROBIC bacteria , *AEROBIC bacteria , *NANOPARTICLES , *STEARIC acid - Abstract
Delafloxacin (DFL) is a novel potent and broad-spectrum fluoroquinolone group of antibiotics effective against both Gram-positive and negative aerobic and anaerobic bacteria. In this study, DFL-loaded stearic acid (lipid) chitosan (polymer) hybrid nanoparticles (L-P-NPs) have been developed by single-emulsion-solvent evaporation technique. The mean particle size and polydispersity index (PDI) of optimized DFL-loaded L-P-NPs (F1-F3) were measured in the range of 299–368 nm and 0.215–0.269, respectively. The drug encapsulation efficiency (EE%) and loading capacity (LC%) of DFL-loaded L-P-NPs (F1-F3) were measured in the range of 64.9–80.4% and 1.7–3.8%, respectively. A sustained release of DFL was observed from optimized DFL-loaded L-P-NPs (F3). Minimum inhibitory concentration (MIC) values of the DFL-loaded L-P-NPs (F3) appeared typically to be four-fold lower than those of delafloxacin in the case of Gram-positive strains and was 2-4-fold more potent than those of delafloxacin against Gram-negative strains. The pharmacokinetic study in rats confirmed that the bioavailability (both rate and extent of absorption) of DFL-loaded L-P-NPs was significantly higher (2.3-fold) than the delafloxacin normal suspension. These results concluded that the newly optimized DFL-loaded L-P-NPs were more potent against both Gram-positive and negative strains of bacteria and highly bioavailable in comparison to delafloxacin normal suspension. [ABSTRACT FROM AUTHOR]
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- 2020
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11. High throughput μ-SPE based elution coupled with UPLC–MS/MS for determination of eluxadoline in plasma sample: Application in pharmacokinetic characterization of PLGA nanoparticle formulations in rats.
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Iqbal, Muzaffar, Ezzeldin, Essam, Al-Rashood, Khalid A., Al-Shdefat, Ramadan, and Anwer, Md. Khalid
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HIGH throughput screening (Drug development) , *SOLID phase extraction , *ELUTION (Chromatography) , *HIGH performance liquid chromatography , *MASS spectrometry , *PHARMACOKINETICS - Abstract
Eluxadoline is a novel μ- and κ-opioid receptor (OR) agonist and δ-OR antagonist, recently approved as a first line therapy for the treatment of irritable bowel syndrome. Due to abuse potential, poor bioavailability and high intersubject variability, a sensitive and reliable assay is prerequisite for its determination in biological samples. This work first time report the development and validation of UPLC–MS/MS assay for determination of eluxadoline in rat plasma sample using risperidone as an internal standard (IS). A high-throughput 96-well plate format μ-SPE technique was used for plasma sample extraction. The extracted samples were separated on Acquity BEH™ C 18 column (100 × 2.1 mm, 1.7 μm) using mobile phase elution of acetonitrile: 20 mM ammonium acetate (80:20, v/v) at a flow rate of 0.3 mL min −1 . The precursor to product ion transition of m / z 570.16 → 118.12 (qualifier), 570.16 → 171.08 (quantifier) for eluxadoline, and m / z 411.18 → 191.07 for IS were used for MRM monitoring. The calibration curves were linear in concentration range of 0.15–50 ngmL −1 with LOD and LOQ of 0.07 and 0.15 ngmL −1 , respectively. The validation results satisfied the criteria of USFDA and SWGTOX guidelines and were within the acceptable limit. Finally, the method was successfully applied in bioavailability enhancement study of the newly developed PLGA nanoparticles and Eudragit coated PLGA nanoparticles of eluxadoline in rats. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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