Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system

Shakeel, Faiyaz; Iqbal, Muzaffar; Ezzeldin, Essam

doi:10.1111/jphp.12550

Cited by 59 publications

(19 citation statements)

References 30 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Malvern particle size analyzer (Holtsville, NY) was used to measure the particle size and PDI of the synthesized STM PLGA-NPs (F1 -F3) [16]. The NP dispersion was appropriately diluted (1:200), and sonicated for 10 min in order to get a clear dispersion.…”

Section: Particle Characterizationmentioning

confidence: 99%

Characteristics and anticancer properties of Sunitinib malate-loaded poly-lactic-co-glycolic acid nanoparticles against human colon cancer HT-29 cells lines

Alshetaili¹,

Anwer²,

Alshahrani³

et al. 2018

Trop. J. Pharm Res

View full text Add to dashboard Cite

Purpose: To develop poly-lactic-co-glycolic acid (PLGA)-based nanoparticles (NPs) for the delivery of sunitinib malate (STM) to colon cancer cells. Methods: Three different formulations (F1-F3) were developed by nano-precipitation technique using various concentrations of PLGA. The NPs were evaluated for particle size, polydispersity index, zeta potential, drug entrapment, and drug loading, using differential scanning calorimetry (DSC), Fouriertransform infrared spectroscopy (FTIR), x-ray diffraction (XRD), and scanning electron microscopy (SEM). Furthermore, in vitro drug release and anticancer studies were carried out on the formulations. Results: Among the three NPs, optimized NP (F3) of STM was chosen for in vitro anti-cancer study against H-29 human colon cancer cells lines based on its particle size (132.9 nm), PDI (0.115), zeta potential (-38.12 mV), entrapment efficiency (52.42 %), drug loading (5.24 %), and drug release (91.26 % in 48 h). A significant anti-cancer activity of the optimized NPs was observed, relative to free STM. Conclusion: These findings suggest that STM-loaded NPs possess significant anti-cancer activity against human colon cancer HT-29 cells lines.

show abstract

Section: Particle Characterizationmentioning

confidence: 99%

Characteristics and anticancer properties of Sunitinib malate-loaded poly-lactic-co-glycolic acid nanoparticles against human colon cancer HT-29 cells lines

Alshetaili¹,

Anwer²,

Alshahrani³

et al. 2018

Trop. J. Pharm Res

View full text Add to dashboard Cite

show abstract

“…The main objective of this work was to enhance solubility and bioavailability of ELUX and sustained the release in intestinal region for the effective treatment of IBS-D. Previously we have successfully improved the bioavailability of poorly bioavailable drug, ibrutinib (absolute bioavailability 2.9%) by self-nanoemulsifying drug delivery system ( Janssen Pharmaceutica NV, 2016 ; Shakeel et al, 2016 ). The alternative therapy available for IBS-D were limited due to its adverse effects mainly due to non-targeting of drugs.…”

Section: Discussionmentioning

confidence: 99%

Preparation, Evaluation and Bioavailability Studies of Eudragit Coated PLGA Nanoparticles for Sustained Release of Eluxadoline for the Treatment of Irritable Bowel Syndrome

et al. 2017

Self Cite

View full text Add to dashboard Cite

Eluxadoline is a newly approved orally administered drug used for the treatment of Irritable Bowel Syndrome with Diarrhea. It is reported as a poorly water-soluble drug due to which its dissolution rate and oral bioavailability are very poor. In this work, various plain PLGA nanoparticles (NPs) (F1–F4) were prepared and optimized based on particle size, PDI, zeta potential and percent drug entrapment efficiency (EE). The developed plain NPs (F1–F4) showed average particle size ranging from 260.19 to 279.76 nm with smooth surface and EE of 17.83–56.29%. The optimized plain NPs (F3) had particle size of 273.76 ± 7.25 nm with a low PDI value 0.327, zeta potential - 30.63 ± 2.47 mV and % EE of 56.29 ± 2.56%. The optimized F3 NPs was further submitted for enteric coating using Eudragit S100 polymer and evaluated in terms of particles characterization, in vitro release and pharmacokinetic studies in rats. The bioavailability of plain and coated nanaoparticles were enhanced by 6.8- and 18.5-fold, respectively, compared to normal suspension. These results revealed that the developed coated NPs could be used for its oral delivery for an effective treatment of Irritable Bowel Syndrome with Diarrhea.

show abstract

“…The most stable NEs were further subjected to freeze thaw cycles at 21 and 25 for one day and checked for physical change, separation, cracking and coalescence, and most stable formulation was further used for in vivo studies. The self-nanoemulsification test were performed to check any phase separation upon dilution with different diluents like water, 0.1 N HCl and phosphate buffer pH 6.8 13,28 . For this tests, 1ml of each NEs F1-F2 was diluted 1:500 with each diluents.…”

Section: Thermodynamic Stability and Emulsification Evaluationmentioning

confidence: 99%

“…termination of existence of zone of NE 6,7,28,29 . The oil phase, Isopropyl myristate, IPM was mixed with surfactant/co-surfactant Tween-80 / Labrasol, Smix in the mass ratios of 1:0, 1:1, 1:2 and 2:1, and mixture was titrated with double distilled water.…”

mentioning

confidence: 97%

Preparation, Characterization and <i>in vivo </i>Anti-inflammatory Studies of Ostrich Oil Based Nanoemulsion

Alshahrani

2019

J. Oleo Sci.

View full text Add to dashboard Cite

INTRODUCTION Nanoemulsions NEs are a transparent, clear and thermally stable emulsion of oil, surfactant and co-surfactant with size of globule 100 nm 1, 2. The NEs can be developed as oil-in-water o/w and water in-oil w/o forms, where the dispersed phase is either oil or water. NEs are developed using safe and non-toxic surfactants and co-surfactants for human use, which must be approved by FDA as Generally Recognized as Safe GRAS 3 5. NEs systems have been well recognized as novel nano-carrier to enhance solubility, absorption and bioavailability of many therapeutic active components present in food, drugs and pharmaceuticals 6 8. NEs can load enough hydrophobic drugs to shield the drug from hydrolysis, degradation and also used as an excellent vehicle for the parenteral drug delivery 9 16. Ostrich, emu and rhea are three major species of birds from the ratite family. Both the ostrich and emu are within the same family, called Struthionidae. These birds primarily used to produce meat, leather, and oil 17, 18. Several fatty acids have been identified in ostrich oil such as oleic acid, linoleic acid, palmitic acid, linolenicacidetc. Ostrich oil also contains flavones, polyphenols, tocopherols, which have antioxidant properties 19 21. Ostrich oil has ability to penetrate deeply into the tissues due presence of high content of oleic acid 22 .

show abstract

Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system

Abstract: These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy.

Cited by 59 publications

References 30 publications

Characteristics and anticancer properties of Sunitinib malate-loaded poly-lactic-co-glycolic acid nanoparticles against human colon cancer HT-29 cells lines

Characteristics and anticancer properties of Sunitinib malate-loaded poly-lactic-co-glycolic acid nanoparticles against human colon cancer HT-29 cells lines

Preparation, Evaluation and Bioavailability Studies of Eudragit Coated PLGA Nanoparticles for Sustained Release of Eluxadoline for the Treatment of Irritable Bowel Syndrome

Preparation, Characterization and <i>in vivo </i>Anti-inflammatory Studies of Ostrich Oil Based Nanoemulsion

Contact Info

Product

Resources

About