Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement

He, Jiali; Han, Yue; Xu, Gujun; Yin, Lifang; Neubi, M. Ngandeu; Zhou, Jianping; Ding, Yang

doi:10.1039/c6ra28676c

Cited by 47 publications

(27 citation statements)

References 53 publications

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“…However, for long-term stability, maintenance of the original crystal structure is beneficial due to its lower state of energy. Moreover, the same induced properties and results were confirmed by previously reported studies [36] .…”

Section: : Photomicrographs Of Sem and Inverted Phase Microscopic Imasupporting

confidence: 90%

“…1B). The zeta potential of reconstituted EENS was -19.3±6.73 mV indicating good physical stability of the optimized NS [36] .…”

Section: Resultsmentioning

confidence: 94%

“…1A), which was easily re-dispersed upon gentle shaking. It was reported that narrow and uniform particle size distribution favours dissolution enhancement, boosts intestinal absorption and improves oral bioavailability [36] . Optimized EENS showed PDI value equal to 0.22±0.15 indicating narrow distribution of particles and thus better stability of NS.…”

Section: Resultsmentioning

confidence: 99%

“…Deproteinization was done by adding 100 μl acetonitrile to 50 μl plasma sample and 300 μl acetonitrile to 200 μl of clear tissue homogenates followed by centrifugation at 6000 rpm for 15 min at 4º. Transparent supernatant obtained was filtered using a 0.20 μm syringe filter and injected into the HPLC system for determining EE content in plasma and tissue samples [34,36] .…”

Section: Pharmacokinetic and Biodistribution Study In Sprague Dawley mentioning

confidence: 99%

“…As the particle size of EENS was smaller than that of EE, these possessed much larger surface area and hence a faster dissolution rate. Besides particle size, particle shape also affects the dissolution of drugs [36] . Particles that are irregular, flaky and long exhibit a higher hydrodynamic thickness at the boundary layer.…”

Section: : Photomicrographs Of Sem and Inverted Phase Microscopic Imamentioning

confidence: 99%

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Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Powar¹,

Hajare²

2020

ijps

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The present investigation was aimed to fabricate lyophilized nanosuspension of poorly soluble ethinylestradiol in order to enhance oral bioavailability and stability. The top-down high-pressure homogenization technique was used to formulate the desired dosage form. The formulations were characterized and optimized for compatibility, crystallographic investigation, surface topography, drug release, in vitro apoptosis and cytotoxicity and in vivo pharmacokinetic investigations. The mean particle size and zeta potential of the optimized lyophilized ethinylestradiol nanosuspension were 220±0.37 nm and -19.3±6.73 mV, respectively. The surface topographical studies showed needle-shaped particles from bar shape upon nanonization by high-pressure homogenization technique. Differential scanning calorimetry and X-ray powder diffraction studies confirmed the crystalline nature of ethynylestradiol after nanonization. The dissolution rate of ethinylestradiol nanosuspension was improved as compared to ethinylestradiol powder. In vitro cytotoxicity of ethinylestradiol nanosuspension on MCF-7 cell line showed more than 80 % inhibition of viability of cells relative to that produced by ethinylestradiol aqueous dispersion. Noteworthy, apoptotic cells treated with ethinylestradiol nanosuspension showed shrinkage, followed by fragmentation and cell death. Significantly, ethinylestradiol nanosuspension enhanced C max and AUC 0-t by 1.5-fold and 1.7-fold compared to that of the aqueous solution. The relative bioavailability of ethinylestradiol was enhanced 2-fold and high concentrations were found to be distributed to liver, spleen and stomach. Thus lyophilized nanosuspension could be a better approach to enhance solubility, oral bioavailability and stability of ethinylestradiol in pharmaceutical formulations.

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Section: : Photomicrographs Of Sem and Inverted Phase Microscopic Imasupporting

confidence: 90%

“…1B). The zeta potential of reconstituted EENS was -19.3±6.73 mV indicating good physical stability of the optimized NS [36] .…”

Section: Resultsmentioning

confidence: 94%

Section: Resultsmentioning

confidence: 99%

Section: Pharmacokinetic and Biodistribution Study In Sprague Dawley mentioning

confidence: 99%

Section: : Photomicrographs Of Sem and Inverted Phase Microscopic Imamentioning

confidence: 99%

See 3 more Smart Citations

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Powar¹,

Hajare²

2020

ijps

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Advancement of nanomedicines in chronic inflammatory disorders

et al. 2022

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Chronic diseases, as stated by the WHO, are a threat to human health which kill 3 out of every 5 people worldwide. Therapeutics for such illnesses can be developed using traditional medicine. However, it is not an easy path from natural products to Western pharmacological and pharmaceutical methods. For several decades, chronic inflammatory disorders, especially in Westernized countries, have increased incidence and prevalence. Several NSAIDs are used to decrease inflammation and pain; however, there are numerous negative consequences of these anti-inflammatory medications, whereas plant-based natural products have anti-inflammatory therapeutic benefits that have little or no adverse effects. Nanoparticles are a new type of drug delivery device that may be designed to provide excellent target selectivity for certain cells and tissues while also having a high drug loading capacity, resulting in better pharmacokinetics, pharmacodynamics (PKPD), and therapeutic bioavailability. The size and polarity of phytochemical compounds make it hard to pass the blood–brain barrier (BBB), blood-vessel endothelial lining, gastrointestinal tract and mucosa. In addition, the gastrointestinal system is enzymatically destroyed. Therefore, nanoparticles or nanocrystals might also be used for encapsulation or conjugation of these chemicals as a method to improve their organic effectiveness through their gastrointestinal stability, absorption rate and dispersion. The therapy of numerous inflammatory illnesses, including arthritis, gastritis, Nephritis, Hepatitis (Type A, B &C), ulcerative colitis, Alzheimer's disease, atherosclerosis, allergic responses (asthma, eczema) or autoimmune disorders, is characterised by nanoparticles. This review paper provides information on the numerous nanosystem described with their probable mechanism to treat chronic inflammatory diseases.

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Particle Size Reduction Techniques of Pharmaceutical Compounds for the Enhancement of Their Dissolution Rate and Bioavailability

et al. 2021

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Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement

Abstract: We prepare celecoxib nanosuspensions using TPGS as stabilizer via high speed shear as a pre-treatment step, followed by HPH method; and the solidification of fresh nanosuspension was carried out by freeze-drying.

Cited by 47 publications

References 53 publications

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Advancement of nanomedicines in chronic inflammatory disorders

Particle Size Reduction Techniques of Pharmaceutical Compounds for the Enhancement of Their Dissolution Rate and Bioavailability

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