Intestinal permeability determinants of norfloxacin in Ussing chamber model

Mendes, Cassiana; Meirelles, Gabriela de Carvalho; Silva, Marcos A. S.; Ponchel, Gilles

doi:10.1016/j.ejps.2018.05.030

Cited by 21 publications

(10 citation statements)

References 43 publications

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“…The Ussing chamber assay is a conventional system to evaluate the cross‐mucosa permeation of drugs through the calculation of the apparent permeability coefficient (PAPP) ( Figure a) . Here, we used the Ussing chamber assay for the evaluation of the transmucosal penetration capacity of free CAT‐Ce6 and CAT‐Ce6‐loaded NPs with various CAT‐Ce6: F‐PEI (or PEI) weight ratios of 4:1–1:4 according to the standard procedure . As shown in Figure b, CAT‐Ce6/F‐PEI NPs showed much higher mucous permeation than that of CAT‐Ce6/PEI NPs, although the latter showed improved transmucosal penetration compared with free CAT‐Ce6.…”

Section: Resultsmentioning

confidence: 80%

“…Since the bladder mucosa is the primary physiological barrier for the intravesical drugs, we first evaluated the transmucosal absorption efficiency of CAT‐Ce6/F‐PEI NPs. The Ussing chamber assay is a conventional system to evaluate the cross‐mucosa permeation of drugs through the calculation of the apparent permeability coefficient (PAPP) ( Figure a) . Here, we used the Ussing chamber assay for the evaluation of the transmucosal penetration capacity of free CAT‐Ce6 and CAT‐Ce6‐loaded NPs with various CAT‐Ce6: F‐PEI (or PEI) weight ratios of 4:1–1:4 according to the standard procedure .…”

Section: Resultsmentioning

confidence: 99%

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Fluorinated Polyethylenimine to Enable Transmucosal Delivery of Photosensitizer‐Conjugated Catalase for Photodynamic Therapy of Orthotopic Bladder Tumors Postintravesical Instillation

Yuan

Deng

et al. 2019

Adv Funct Materials

115

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Photodynamic therapy (PDT) by insertion of an optical fiber into the bladder cavity has been applied in the clinic for noninvasive treatment of bladder tumors. To avoid systemic phototoxicity, bladder intravesical instillation of a photosensitizer may be an ideal approach for PDT treatment of bladder cancer, in comparison to conventional intravenous injection. However, the instillationbased PDT for bladder cancer treatment remains to be less effective due to the poor urothelial uptake of photosensitizer, as well as the tumor hypoxiaassociated PDT resistance. Herein, it is uncovered that fluorinated polyethylenimine (F-PEI) achieved by mixing with Chorin-e6-conjugated catalase (CAT-Ce6) is able to form self-assembled CAT-Ce6/F-PEI nanoparticles, which show greatly improved cross-membrane, transmucosal, and intratumoral penetration capacities compared with CAT-Ce6 alone or nonfluorinated CAT-Ce6/PEI nanoparticles. Owing to the decomposition of tumor endogenous H 2 O 2 by CAT-Ce6/F-PEI nanoparticles penetrating into bladder tumors, the tumor hypoxia would be effectively relieved to further favor PDT. Therefore, bladder intravesical instillation with CAT-Ce6/F-PEI nanoparticles could offer remarkably improved photodynamic therapeutic effect to destruct orthotopic bladder tumors with reduced systemic toxicity compared to hematoporphyrin, the first-line photosensitizer used for bladder cancer PDT in clinic. This work presents a unique photosensitizer nanomedicine formulation, promising for clinical translation in instillation-based PDT to treat bladder tumors.

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Section: Resultsmentioning

confidence: 80%

Section: Resultsmentioning

confidence: 99%

Fluorinated Polyethylenimine to Enable Transmucosal Delivery of Photosensitizer‐Conjugated Catalase for Photodynamic Therapy of Orthotopic Bladder Tumors Postintravesical Instillation

Yuan

Deng

et al. 2019

Adv Funct Materials

115

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“…Having established the relationship between drug–polymer miscibility, intermolecular interaction, and physical stability of ASDs, we investigated the dissolution behaviors of three drug/polymer systems in simulated gastric media (pH 1.5) in an attempt to explore the possible correlations between molecular characteristic of NFX/polymer blends and the dissolution of ASDs. NFX is highly soluble at pH 1.5 wherein the equilibrium solubility was measured to be 17–18 mg/mL ( T = 37 °C) in this study, while the usual dose for NFX is 400 mg, well below the amount of soluble solute in 500 mL of simulated gastric medium. Therefore, it is unnecessary to test the dissolution rate according to the concentration of saturated NFX solution.…”

Section: Resultsmentioning

confidence: 72%

Investigation of Drug–Polymer Miscibility, Molecular Interaction, and Their Effects on the Physical Stabilities and Dissolution Behaviors of Norfloxacin Amorphous Solid Dispersions

Liu

Jia

et al. 2020

Crystal Growth & Design

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This study investigated the drug–polymer miscibility, intermolecular interaction, physical stability, and dissolution performance of amorphous solid dispersions (ASDs) of norfloxacin (NFX) with polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl methylcellulose phthalate (HPMCP). The NFX–polymer miscibility was evaluated based on the Hansen solubility parameter and Flory–Huggins interaction parameter. The results are in broad agreement with an order of NFX–HPMCP > NFX–HPMC > NFX–PVP. The NFX–polymer molecular interaction in the solution state was determined by nuclear magnetic resonance (NMR) spectroscopic studies. The strength of interaction was rank ordered as HPMC > HPMCP > PVP, which was different from the solid state. Powder X-ray diffraction (PXRD) detected the stability of ASDs, and the result indicates that the high drug–polymer miscibility and strong interactions could translate to high resistance to drug crystallization. Dissolution studies of ASDs were carried out across the gastrointestinal pH range. Interestingly, there was no significant dissolution enhancement, and a polymer-dependent drug release profile was observed. On the basis of the drug–polymer miscibility and hydrophilicity of polymers, a nonclassical drug release mechanism was revealed. Furthermore, it has been speculated that the effectiveness of a polymer in maintaining supersaturation of drug in solution can be more dependent on the specific drug–polymer interaction mode than on the strength.

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“…Norfloxacin is the quinolone that has been mostly used because of its low solubility, low permeability, and therefore low bioavailability, characteristics that theoretically allow it to selectively decontaminate the bowel. However, it was withdrawn from the US market as of April 2014 (not because of safety concerns).…”

Section: Do Prophylactic Antibiotics Prevent Infections and The Downsmentioning

confidence: 99%

Prophylactic Antibiotics in Cirrhosis: Are They Promoting or Preventing Infections?

García–Tsao

2019

Clinical Liver Disease

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Intestinal permeability determinants of norfloxacin in Ussing chamber model

Cited by 21 publications

References 43 publications

Fluorinated Polyethylenimine to Enable Transmucosal Delivery of Photosensitizer‐Conjugated Catalase for Photodynamic Therapy of Orthotopic Bladder Tumors Postintravesical Instillation

Fluorinated Polyethylenimine to Enable Transmucosal Delivery of Photosensitizer‐Conjugated Catalase for Photodynamic Therapy of Orthotopic Bladder Tumors Postintravesical Instillation

Investigation of Drug–Polymer Miscibility, Molecular Interaction, and Their Effects on the Physical Stabilities and Dissolution Behaviors of Norfloxacin Amorphous Solid Dispersions

Prophylactic Antibiotics in Cirrhosis: Are They Promoting or Preventing Infections?

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