Publications by authors named "Mahmoud A Shaker"

3 Publications

  • Page 1 of 1

Enhancement of atorvastatin oral bioavailability via encapsulation in polymeric nanoparticles.

Int J Pharm 2021 Jan 24;592:120077. Epub 2020 Nov 24.

Department of Pharmaceutics, Faculty of Pharmacy, King Khalid University, Abha, Saudi Arabia.

Despite the fact that atrovastatin (At) is being one of the bestselling statins used to prevent complicated cardiovascular diseases, its low oral bioavailability decreases its clinical relevance. Herein, incorporation of At into ethylcellulose nanoparticles (At-NPs) was executed to test if it would enhance its oral bioavailability. The emulsification-evaporation method was used to prepare the At-NPs. The prepared nanoparticles were characterized by measuring the particle size, zeta potential as well as using FTIR, DSC, and XRD examination. The entrapment efficiency, drug content, and the in vitro release behavior of At-NPs were also examined. The in vivo oral bioavailability of the selected At-NPs formula was tested after being given orally to New Zealand rabbits. The nanoparticles obtained had a high drug content and a distinct spherical shape but with varying sizes. No physical or chemical interactions were detected between At and the nanoparticles as confirmed by FTIR, DSC, and XRD. The in vitro release study of At from the prepared At-NPs has shown nanoparticles size-dependent release behavior. The in vivo oral absorption testing confirmed the bioavailability of the prepared At-NPs to be as follows: (C = 940 ng/ml and AUC = 8759 ng.h/ml) > Lipitor® (C = 635 ng/ml and AUC = 4367 ng.h/ml) > At (C = 515 ng/ml and AUC = 2517 ng.h/ml). These results revealed that the oral formula of At-NPs increases the bioavailability of At 3.87 times. This makes ethylcellulose nanoparticles an esteemed candidate nano-vehicle for At, increasing its bioavailability and thus improving its clinical relevance.
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http://dx.doi.org/10.1016/j.ijpharm.2020.120077DOI Listing
January 2021

Improved solubility, dissolution, and oral bioavailability for atorvastatin-Pluronic® solid dispersions.

Int J Pharm 2020 Jan 28;574:118891. Epub 2019 Nov 28.

Department of Pharmaceutics, Faculty of Pharmacy, King Khalid University, Abha, Saudi Arabia.

Despite the status of atorvastatin (AT) as one of the top selling statins for prophylaxis against primary and secondary cardiovascular diseases, its limited oral absorption limits its full therapeutic benefits. Herein, formulations of AT with amphiphilic carriers (Pluronic F127® and Pluronic F68®) were developed in the form of hard capsules to improve in vitro solubility and dissolution, as well as in vivo oral bioavailability. Prepared formulas were characterized by assessing solubility improvements in the carrier solution and examining the FTIR, DSC, and X-RPD profiles for each formula. The dissolution rate and absorption were also examined after oral administration to New Zealand rabbits. The solubility of AT was improved by the incorporation of either Pluronic F127® or Pluronic F68®. No chemical changes or interactions were detected using X-RPD, DSC, and FTIR characterization. Dissolution profiles revealed an increase in the rate and maximum amount of dissolved AT and showed that up to 93% of the AT content was dissolved within 30 min. In vivo absorption of the tested formula (C = 1146 ng/ml and AUC0-12 to 9,993.4 ng.h/ml) was greater than Lipitor® (C = 642.3 ng/ml and AUC0-12 = 4427.4 ng.h/ml) and AT (C = 517.6 ng/ml and AUC0- 12 = 2,473.7 ng.h/ml). In conclusion, the formulation of AT with Pluronics® profoundly augments the dissolution behavior and absorption of AT and may serve as a useful approach for improving AT therapeutic and clinical efficacy.
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http://dx.doi.org/10.1016/j.ijpharm.2019.118891DOI Listing
January 2020

Recent expansions of novel strategies towards the drug targeting into the brain.

Int J Nanomedicine 2019 30;14:5895-5909. Epub 2019 Jul 30.

Pharmaceutics Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt.

The treatment of central nervous system (CNS) disorders always remains a challenge for the researchers. The presence of various physiological barriers, primarily the blood-brain barrier (BBB) limits the accessibility of the brain and hinders the efficacy of various drug therapies. Hence, drug targeting to the brain, particularly to the diseased cells by circumventing the physiological barriers is essential to develop a promising therapy for the treatment of brain disorders. Presently, the investigations emphasize the role of different nanocarrier systems or surface modified target specific novel carrier system to improve the efficiency and reduce the side effects of the brain therapeutics. Such approaches supposed to circumvent the BBB or have the ability to cross the barrier function and thus increases the drug concentration in the brain. Although the efficacy of novel carrier system depends upon various physiological factors like active efflux transport, protein corona of the brain, stability, and toxicity of the nanocarrier, physicochemical properties, patient-related factors and many more. Hence, to develop a promising carrier system, it is essential to understand the physiology of the brain and BBB and also the other associated factors. Along with this, some alternative route like direct nose-to-brain drug delivery can also offer a better means to access the brain without exposure of the BBB. In this review, we have discussed the role of various physiological barriers including the BBB and blood-cerebrospinal fluid barrier (BCSFB) on the drug therapy and the mechanism of drug transport across the BBB. Further, we discussed different novel strategies for brain targeting of drug including, polymeric nanoparticles, lipidic nanoparticles, inorganic nanoparticles, liposomes, nanogels, nanoemulsions, dendrimers, quantum dots, etc. along with the intranasal drug delivery to the brain. We have also illustrated various factors affecting the drug targeting efficiency of the developed novel carrier system.
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http://dx.doi.org/10.2147/IJN.S210876DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6679699PMC
November 2019