Phospholipid based self-nanoemulsifying self-nanosuspension (p-SNESNS) as a dual solubilization approach for development of formulation with diminished food effect: Fast/fed in vivo pharmacokinetics study in human

Basalious, Emad B.; Ahmed, M.

doi:10.1016/j.ejps.2017.08.017

Cited by 14 publications

(3 citation statements)

References 32 publications

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“…Therefore, there is a great need to find more therapeutics with fewer side effects. SNESNS is a newly developed drug delivery system that has evolved as a modification of self-nanoemulsifying drug delivery systems to make them suitable to accommodate large drug doses and to enhance the solubility and efficacy of drugs depending on the synergism of two solubilization techniques which are self-nanoemulsification and in situ formation of nanosuspension [22,39,40]. The favorable advantages of SNESNS present it as a delivery system of choice for herbal extracts, which contain multiple components, including hydrophobic and hydrophilic materials, as the formed W/O nanoemulsion can load both materials.…”

Section: Discussionmentioning

confidence: 99%

Antidepressant and Cardioprotective Effects of Self-Nanoemulsifying Self-Nanosuspension Loaded with Hypericum perforatum on Post-Myocardial Infarction Depression in Rats

et al. 2022

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Hypericum perforatum (HP) is characterized by potent medicinal activity. However, the poor water solubility of many HP constituents limits their therapeutic effectiveness. Self-nanoemulsifying self-nanosuspension loaded with HP (HP.SNESNS) was formulated to improve the bioefficacy of HP. It was prepared using 10% triacetin, 57% Tween 20, and 33% PEG 400 and then incorporated with HP extract (100 mg/mL). HP.SNESNS demonstrated a bimodal size distribution (258.65 ± 29.35 and 9.08 ± 0.01 nm) corresponding to nanosuspension and nanoemulsion, respectively, a zeta potential of -8.03 mV, and an enhanced dissolution profile. Compared to the unformulated HP (100 mg/kg), HP.SNESNS significantly improved cardiac functions by decreasing the serum myocardial enzymes, nitric oxide (NO), and tumor necrosis factor- α (TNF-α) as well as restoring the heart tissue's normal architecture. Furthermore, it ameliorates anxiety, depressive-like behavior, and cognitive dysfunction by decreasing brain TNF-α, elevating neurotransmitters (norepinephrine and serotonin), and brain-derived neurotrophic factor (BDNF). In addition, HP.SNESNS augmented the immunohistochemical expression of cortical and hippocampal glial fibrillary acidic protein (GFAP) levels while downregulating the cortical Bcl-2-associated X protein (Bax) expression levels. Surprisingly, these protective activities were comparable to the HP (300 mg/kg). In conclusion, HP.SNESNS (100 mg/kg) exerted antidepressant and cardioprotective activities in the post-MI depression rat model. Graphical Abstract

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Section: Discussionmentioning

confidence: 99%

Antidepressant and Cardioprotective Effects of Self-Nanoemulsifying Self-Nanosuspension Loaded with Hypericum perforatum on Post-Myocardial Infarction Depression in Rats

et al. 2022

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“…Nanotechnology has, for example, been used to enhance the bioavailability of certain antibiotics [14] and has also been applied to produce different targeted drugs for the treatment of different diseases [15–17], and various nanosuspensions have been successfully applied [18, 19]. Nanoparticles can also be prepared using a variety of different processes, including reverse solvent, homogenization pressure, milling, and the production of self-nanoemulsifying self-nanosuspensions [20].…”

Section: Introductionmentioning

confidence: 99%

Design, Preparation, and Characterization of Dioscin Nanosuspensions and Evaluation of Their Protective Effect against Carbon Tetrachloride-Induced Acute Liver Injury in Mice

Zhao

et al. 2019

Evidence-Based Complementary and Alternative Medicine

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The purpose of this study was to prepare a dioscin nanosuspension (Dio-NS) that has a better distance and high solubility for oral administration and to evaluate its hepatoprotective effects. Optimal primary manufacture parameters, including shear time, shear speed, emulation temperature, pressure, and cycles of homogenization, were determined by single-factor experiments. The concentrations of dioscin, SDS, and soybean lecithin were optimized using the central composite design-response surface method, and their effects on the mean particle size (MPS) and particle size distribution of Dio-NS were investigated. Characterization of the Dio-NS formulations included examinations of the surface morphology and physical status of dioscin in Dio-NS, the stability of Dio-NS at different temperatures, in vitro solubility, and liver protective effect in vivo. Under optimal conditions, Dio-NS had an MPS of 106.72 nm, polydispersity index of 0.221, and zeta potential of −34.27 mV. Furthermore, the proportion of dioscin in Dio-NS was approximately 21.26%. The observation of particles with a spherical shape and the disappearance of crystalline peaks indicated that the physical and chemical properties of Dio-NS were altered. Furthermore, we observed that the dissolution of Dio-NS was superior to that of a physical mixture and Dio-GZF. Moreover, Dio-NS was demonstrated to have a protective effect against CCl4-induced acute liver damage in mice that was equivalent to that of silymarin (a positive control drug) at the same dose. The good hepatoprotective effect of our Dio-NS preparation can provide a theoretical basis for investigating its absorption mechanisms in the body.

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“…Therefore, the food effects to drug bioavailability should be investigated systematically in fed and fasted states to guide clinical rational use of drug especially for chronic administration, and to provide information on the control of the determination of drug dosage or the meal before and after drug administration 12 , 13 . The FDA has provided guidance on how to conduct a reasonable study according to the food effect on humans, which is treated with a randomized, balanced, single-dose, two-period, cross-over design for the food effect research on oral bioavailability under fasted and fed treatment 14 , 15 . In order to amplify the effect of food on oral bioavailability, a special test meal that contains high-fat, high-calorie and reasonable time of administration are always chosen in the fed group 16 .…”

Section: Introductionmentioning

confidence: 99%

Identification of beagle food taking patterns and protocol for food effects evaluation on bioavailability

Zhang

Wang

et al. 2018

Sci Rep

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Food is a known primary role to the exposure of the drugs orally administered. Since each animal may have unique food taking pattern and it is difficult to manipulate the food taking to animals, there lacks rationalized protocol for the food effects in pre-clinic study. The objective of this study was to identify the beagle food taking patterns and demonstrate their effects on bioavailability in valsartan. Herein, four types of food taking patterns of beagle were identified via inter-day and intra-day analysis, and named as Persisting, Pulsing, Postponing, Pushing (“4P Modes”), respectively, which were also validated by principal component analysis (PCA). Interestingly, food intake resulted in a reduced area under the concentration-time curve (AUC0–12h), maximum concentration (Cmax) and absorption rate, whilst the reduction varied in “4P Modes” of food taking. General considerations in the design of experiment for food effect to the bioavailability in beagles have been established as: to recognize the food taking patterns in each animal, to confirm the inter-day stability of the food taking behaviors, to trace the food taking patterns in parallel with plasma sampling. In conclusion, the right animals with proper food taking patterns should be assessed and selected for pre-clinic bioavailability evaluations.

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Phospholipid based self-nanoemulsifying self-nanosuspension (p-SNESNS) as a dual solubilization approach for development of formulation with diminished food effect: Fast/fed in vivo pharmacokinetics study in human

Cited by 14 publications

References 32 publications

Antidepressant and Cardioprotective Effects of Self-Nanoemulsifying Self-Nanosuspension Loaded with Hypericum perforatum on Post-Myocardial Infarction Depression in Rats

Antidepressant and Cardioprotective Effects of Self-Nanoemulsifying Self-Nanosuspension Loaded with Hypericum perforatum on Post-Myocardial Infarction Depression in Rats

Design, Preparation, and Characterization of Dioscin Nanosuspensions and Evaluation of Their Protective Effect against Carbon Tetrachloride-Induced Acute Liver Injury in Mice

Identification of beagle food taking patterns and protocol for food effects evaluation on bioavailability

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