Comparison of Modern In Vitro Permeability Methods with the Aim of Investigation Nasal Dosage Forms

Bartos, Csilla; Szabó‐Révész, Piroska; Horváth, Tamás; Varga, Patrícia; Ambrus, Rita

doi:10.3390/pharmaceutics13060846

Cited by 20 publications

(14 citation statements)

References 33 publications

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“…Overall, the PDA1-5 nanoparticle flux diffusions were in the range of picograms per m 2 per second, which indicates that they could not penetrate through the membrane or might penetrate but at a very slow rate. In general, chemicals or drugs that can penetrate the skin should have a transdermal flux within milli-to micrograms per unit area per unit time, such as nitroglycerin, transcutrol, ibuprofen, and ketoprofen. − …”

Section: Resultsmentioning

confidence: 99%

Polydopamine-Based Nanoparticles for Safe Sunscreen Protection Factor Products with Enhanced Performance

Supanakorn

Thiramanas

Mahatnirunkul

et al. 2022

ACS Appl. Nano Mater.

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Excessive exposure to ultraviolet light (UV) can damage skin cells and cause skin cancer. Applying sunscreen that blocks both UVA and UVB is recommended before going outside. An ideal sunscreen should not come off, penetrate the bloodstream, or cause health risks, while also remaining effective at blocking UV rays. Herein, we focused on sunscreen applications based on polydopamine (PDA) nanoparticles, an artificial melanin material. Various sizes of nanoparticles were fabricated using a spontaneous oxidation reaction with the dopamine monomer to sodium hydroxide (DA/NaOH) molar ratios of 1:0.2 to 1:1. The monodisperse and spherical PDA nanoparticles with sizes ranging from 59.5 to 659.1 nm showed monotonic broadband UV−vis absorption. PDA2 (molar ratio of DA/ NaOH 1:0.8) presented the highest UVB absorption (290−320 nm) and a sun protection factor boosted by approximately 50% compared to that of the original base formulation. When the particle size was larger than 150 nm, the results from X-ray photoelectron spectroscopy and confocal spectroscopy showed that the surface functionality of the synthesized PDA nanoparticles that was dominated with hydroxyl groups induced their adherence to the stratum corneum after 24 h of incubation. The nanoparticles were biocompatible with human keratinocytes (HaCaT), that is, direct interactions between the PDA particles and HaCaT cells did not cause any cell damage. Results from in vitro photoprotection ability suggested that PDA nanoparticles could protect the cells from UVA irradiation in terms of membrane protection, reactive oxygen species reduction, and cell viability recovery. Interestingly, the results obtained from the bacterial reverse mutation and in vitro skin irritation tests indicated that the nanoparticles did not induce mutagenicity or irritate skin cells. Our findings provide a promising approach for the synthesis of PDA nanoparticles as a safe sunscreen component.

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Section: Resultsmentioning

confidence: 99%

Polydopamine-Based Nanoparticles for Safe Sunscreen Protection Factor Products with Enhanced Performance

Supanakorn

Thiramanas

Mahatnirunkul

et al. 2022

ACS Appl. Nano Mater.

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“…The medium in the acceptor chamber is constantly agitated by a magnetic stirring bar (Mattiasson, 2020). Bartos et al (2021) compared the suitability of a vertical diffusion cell apparatus (Franz diffusion cell device) to a horizontal diffusion apparatus (side-by-side type diffusion device) for different formulations (including a spray, gel, and powder). The study found that spray and powder formulations could be investigated by horizontal diffusion devices; however, the investigation of gel formulations is not desirable in this type of diffusion device.…”

Section: Diffusion Chamber Devices For Ex Vivo Permeation Studiesmentioning

confidence: 99%

In vitro and ex vivo experimental models for evaluation of intranasal systemic drug delivery as well as direct nose‐to‐brain drug delivery

Haasbroek‐Pheiffer

Niekerk

Kooy

et al. 2023

Biopharm & Drug Disp

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The intranasal route of administration provides a noninvasive method to deliver drugs into the systemic circulation and/or directly into the brain. Direct nose‐to‐brain drug delivery offers the possibility to treat central nervous system diseases more effectively, as it can evade the blood–brain barrier. In vitro and ex vivo intranasal models provide a means to investigate physiological and pharmaceutical factors that could play a role in drug delivery across the nasal epithelium as well as to determine the mechanisms involved in drug absorption from the nose. The development and implementation of cost‐effective pharmacokinetic models for intranasal drug delivery with good in vitro‐in vivo correlation can accelerate pharmaceutical drug product development and improve economic and ecological aspects by reducing the time and costs spent on animal studies. Special considerations should be made with regard to the purpose of the in vitro/ex vivo study, namely, whether it is intended to predict systemic or brain delivery, source and site of tissue or cell sampling, viability window of selected model, and the experimental setup of diffusion chambers. The type of model implemented should suit the relevant needs and requirements of the project, researcher, and interlaboratory. This review aims to provide an overview of in vitro and ex vivo models that have been developed to study intranasal and direct nose‐to‐brain drug delivery.

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“…The steady-state flux (Jss, mg/cm 2 /h) was computed from the quantity of EH, which permeated through the nasal mucosa (Q) divided by the membrane surface and the time duration. The permeability coefficient (Kp, cm/h) was calculated from Jss and the initial drug concentration (C 0 ) as given below [29].…”

Section: Apparatus Assemblymentioning

confidence: 99%

Assessment of Nasal-Brain-Targeting Efficiency of New Developed Mucoadhesive Emulsomes Encapsulating an Anti-Migraine Drug for Effective Treatment of One of the Major Psychiatric Disorders Symptoms

et al. 2022

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Migraine is one of the major symptoms of many psychiatric and mental disorders like depression and anxiety. Eletriptan Hydrobromide (EH) is a well-tolerated drug in migraine treatment, but suffers from low oral bioavailability and low brain targeting after oral delivery. New nasal mucoadhesive EH-emulsomes development could be a new means to direct the drug from the nose-to-brain to achieve rapid onset of action and high drug concentration in the brain for acute migraine treatment. Eletriptan mucoadhesive emulsomes formulations were prepared using thin-film hydration method and 23 full factorial design was adopted to study different formulation factors’ effect on the emulsomes characters. The emulsomes were characterized for entrapment efficiency (EE%), zeta potential (ZP), particle size (PS), morphology, and ex-vivo permeation through the nasal mucosa. The selected formula was evaluated in mice for its in-vivo bio-distribution in comparison with EH intranasal and intravenous solutions. Drug targeting efficacy (DTE%) and nose-to-brain direct transport percentage (DTP%) were calculated. The optimization formulation showed a nanoparticle size of 177.01 nm, EE 79.44%, and ZP = 32.12 ± 3.28 mV. In addition, in-vitro permeability studies revealed enhanced drug permeability with suitable mean residence time up to 120 ± 13 min. EH-emulsomes were stable under different storage conditions for three months. In vivo examination and pharmacokinetic drug targeting parameters revealed EH transport to the CNS after EH nanoparticle nasal administration. Histopathology study showed no ciliotoxic effect on the nasal mucosa. From the results, it can be confirmed that the emulsomes formulation of EH proved safe direct nose-to-brain transport of EH after nasal administration of EH emulsomes.

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Comparison of Modern In Vitro Permeability Methods with the Aim of Investigation Nasal Dosage Forms

Cited by 20 publications

References 33 publications

Polydopamine-Based Nanoparticles for Safe Sunscreen Protection Factor Products with Enhanced Performance

Polydopamine-Based Nanoparticles for Safe Sunscreen Protection Factor Products with Enhanced Performance

In vitro and ex vivo experimental models for evaluation of intranasal systemic drug delivery as well as direct nose‐to‐brain drug delivery

Assessment of Nasal-Brain-Targeting Efficiency of New Developed Mucoadhesive Emulsomes Encapsulating an Anti-Migraine Drug for Effective Treatment of One of the Major Psychiatric Disorders Symptoms

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