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- Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats. [Journal Article]
- PPharmaceutics 2018 Nov 28; 10(4)
- The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phas...
The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats. The determined SSP (FL/Kollisolv MCT 70/TPGS = 10/10/80, weight %) in the pseudo-ternary phase diagram had the melting point of 32.37 °C and uniform mean particle size of below 30 nm without any precipitation of FL in the dispersion. In the dissolution test, the SSP exhibited 95.70 ± 3.40% of release at 15 min, whereas the raw FL showed poor dissolution (i.e., 6.75 ± 1.30%) at that time point. In addition, the SSP showed the enhanced oral absorption (i.e., 1.93-fold increase in AUCinfinite) as compared to the suspension group of raw FL. Therefore, the developed SSP would be a promising drug delivery system with excellent solubilization, dissolution, and bioavailability for FL.
- Predicting local drug availability of locally acting lozenges: From method design to a linear level A IVIVC. [Journal Article]
- EJEur J Pharm Biopharm 2018; 133:269-276
- Lozenges are commonly applied in the treatment of sore throat. They often contain drugs intended to exert their effect locally in the oral cavity and throat. In the recent past, an increasing interes...
Lozenges are commonly applied in the treatment of sore throat. They often contain drugs intended to exert their effect locally in the oral cavity and throat. In the recent past, an increasing interest in development of generic products for locally acting lozenges could be noted. However, it was not clear, if therapeutic equivalence of locally applied, locally acting lozenges can be predicted based on results from in vitro studies. The aim of the present study was to determine an in vitro model that enables the assessment of local availability and bioequivalence of locally acting lozenges. Two novel in vitro dissolution setups (prototypes I and II) developed for simulating parameters relevant to drug release in the oral cavity, were screened for their biopredictivity. In the first step of the respective study in vitro mass loss and drug release of two marketed flurbiprofen lozenge formulations was determined. Then, an in vivo sucking study was performed to determine in vivo mass loss of the lozenges in 12 healthy volunteers. In the final step in vivo mass loss was correlated with in vitro mass loss resulting in a point to point (level A) correlation both lozenge formulations when using in vitro data obtained in the prototype II-based in vitro setup indicating biopredictivity of this in vitro model.
- Study on the drug permeation mechanism from flurbiprofen-loaded glyceryl monooleyl ether-based lyotropic liquid crystalline nanoparticles across the skin: Synchrotron X-ray diffraction and confocal laser scanning microscopy study. [Journal Article]
- IJInt J Pharm 2018 Nov 14; 555:259-269
- The mechanism underlying the skin permeation of flurbiprofen (FLU)-loaded, glyceryl monooleyl ether-based liquid crystalline nanoparticles (LCNs) with a hexagonal structure was examined by synchrotro...
The mechanism underlying the skin permeation of flurbiprofen (FLU)-loaded, glyceryl monooleyl ether-based liquid crystalline nanoparticles (LCNs) with a hexagonal structure was examined by synchrotron X-ray diffraction and confocal laser scanning microscopy (CLSM). Fluorescent-labeled, FLU-loaded LCNs were prepared using coumarin 6 and rhodamine B 1,2-dihexadecanoyl-sn-glycero-3-phosphoethanolamine, triethylammonium salt (Rh-PE), which produce green and red fluorescence, respectively. Application of FLU-loaded LCNs to the hairless mouse stratum corneum (SC) induced expansion of the lattice spacing of the hexagonal structure with FLU release, as confirmed by the changes in the small-angle X-ray diffraction profiles. In addition, the FLU-loaded LCNs completely released FLU near the surface of the SC, which then penetrated the SC. Consequently, the repeat distance of the long periodicity phase was slightly modified. CLSM revealed green fluorescence in the epidermis and hair follicles and red fluorescence in the SC. In conclusion, LCNs adopt several permeation pathways: one is partly via the intercellular matrix and the other is the epidermis via hair follicles.
- Flurbiprofen-Associated Hemolytic Anemia. [Journal Article]
- AJAm J Ther 2018 Nov 01
- Docosahexaenoic acid-flurbiprofen combination ameliorates metaflammation in rats fed on high-carbohydrate high-fat diet. [Journal Article]
- BPBiomed Pharmacother 2018 Nov 02; 109:233-241
- CONCLUSIONS: Docosahexaenoic acid-flurbiprofen combination showed an ameliorative effect on obesity-associated metaflammation and its consequences in rats.
- Onset of analgesia by a topically administered flurbiprofen lozenge: a randomised controlled trial using the double stopwatch method. [Journal Article]
- BJBr J Pain 2018; 12(4):208-216
- CONCLUSIONS: These results indicate that the DSW method can be successfully applied to the evaluation of the onset of action of a locally administered analgesic in patients with acute sore throat, demonstrating that the onset of action (time to meaningful pain relief) of flurbiprofen lozenge was <45 minutes.
- Dendrimeric Poly(Epsilon-Lysine) Delivery Systems for the Enhanced Permeability of Flurbiprofen across the Blood-Brain Barrier in Alzheimer's Disease. [Journal Article]
- IJInt J Mol Sci 2018 Oct 18; 19(10)
- Alzheimer's disease (AD) is a progressive brain disorder and age-related disease characterised by abnormal accumulation of β-amyloid (Aβ). The development of drugs to combat AD is hampered by the lac...
Alzheimer's disease (AD) is a progressive brain disorder and age-related disease characterised by abnormal accumulation of β-amyloid (Aβ). The development of drugs to combat AD is hampered by the lack of therapeutically-active molecules able to cross the blood-brain barrier (BBB). It is agreed that specifically-designed carriers, such as dendrimers, could support the drug penetration across the BBB. The aim of this study was to design biocompatible and biodegradable dendrimeric delivery systems able to carry Flurbiprofen (FP), as drug for AD treatment, across the BBB and liberate it at the target tissue. These dendrons were synthesised using solid-phase peptide synthesis method and characterised by mass spectrometry and fourier-transform infrared spectroscopy (FTIR). The results revealed successful synthesis of dendrons having FP been integrated during the synthesis at their branching ends. Cytotoxicity assays demonstrated the biocompatibility of the delivery systems, whereas HPLC analysis showed high percentages of permeability across an in vitro BBB model for FP-integrated dendrons. Results also revealed the efficiency of drug conjugates on the γ-secretase enzyme in target cells with evidence of eventual drug release by hydrolysis of the carrier. This study demonstrates that the coupling of FP to dendrimeric delivery systems can successfully be achieved during the synthesis of the poly(epsilon-lysine) macromolecules to improve the transport of the active drug across the BBB.
- Carbonic anhydrase inhibitory potential of 1,2,4-triazole-3-thione derivatives of flurbiprofen, ibuprofen and 4-tert-butylbenzoic hydrazide : Design, synthesis, characterization, biochemical evaluation, molecular docking and dynamic simulation studies. [Journal Article]
- MCMed Chem 2018 Oct 12
- CONCLUSIONS: The proposed synthetic approach provides a suitable platform for the generation of a new library of compounds which could potentially be employed in the future testing and optimization of inhibitor potencies.
- Prediction of Skin Permeation of Flurbiprofen from Neat Ester Oils and Their O/W Emulsions. [Journal Article]
- CPChem Pharm Bull (Tokyo) 2018; 66(10):959-966
- Although many in silico models were reported to predict the skin permeation of drugs from aqueous solutions, few studies were founded on the in silico estimation models for the skin permeation of dru...
Although many in silico models were reported to predict the skin permeation of drugs from aqueous solutions, few studies were founded on the in silico estimation models for the skin permeation of drugs from neat oil formulations and o/w emulsions. In the present study, the cumulative amount of a model lipophilic drug, flurbiprofen (FP), that permeated through skin was determined from 12 different kinds of ester oils (Qoil) and an in silico model was developed for predicting the skin permeation of FP from these ester oils. Thus, the obtained Qoil values were well predicted with the FP solubility in the oils (Soil), the amount of FP uptake into the stratum corneum (SCoil) and molecular descriptors of dipolarity/polarizability (π2H) and molecular density. This model suggests that the thermodynamic activities of FP both in the formulations and skin are the key factors for predicting the skin permeation of FP from the ester oils. In addition, a high linear relationship was observed in the double-logarithm plots between the Qoil and the cumulative amount of FP permeated through skin from 20% ester oil in water emulsion (Qemul20%). Furthermore, the skin permeations of FP from 5 and 10% ester oil in water emulsions, Qemul5% and Qemul10%, respectively, were also predicted by the horizontal translation of the y-axis intercept of the liner equation for the relation between the Qoil and Qemul20%. These prediction methods must be helpful for designing topical oily and/or o/w emulsion formulations having suitable and high skin permeation rate of lipophilic drugs.
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- Zr-based metal-organic framework-modified cotton for solid phase micro-extraction of non-steroidal anti-inflammatory drugs. [Journal Article]
- JCJ Chromatogr A 2018 Nov 16; 1576:19-25
- A novel metal-organic framework UiO-66-modified cotton was prepared and applied to solid phase microextraction of non-steroidal anti-inflammatory drugs, namely ketoprofen, naproxen and flurbiprofen. ...
A novel metal-organic framework UiO-66-modified cotton was prepared and applied to solid phase microextraction of non-steroidal anti-inflammatory drugs, namely ketoprofen, naproxen and flurbiprofen. UiO-66 was immobilized onto the surface of cotton by a polydopamine functionalized method. The resultant cotton@PDA@UiO-66 was characterized by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy. The solid phase microextraction conditions were optimized, including sampling flow rate, formic acid content of the eluent, pH value of sample solution, NaCl content and sample volume. By combining with HPLC, this method showed high extraction efficiency (the enrichment factors of ketoprofen, naproxen and flurbiprofen were 44, 49 and 45, respectively), wide linear range (0.1-500 ng/mL), good linearity with R ≥ 0.9996 and satisfactory sensitivity (LODs ≤ 0.03 ng/mL, LOQs ≤ 0.1 ng/mL), as well as good reproducibility (RSD ≤ 4.51%). This method was also successfully applied to extraction of NSAIDs in swine muscle sample. Good recoveries were obtained, ranging from 88.54% to 95.7% with relative standard deviations less than 3.77%.