Generation, inhalation delivery and anti-hypertensive effect of nisoldipine nanoaerosol

Onischuk, A. A.; Толстикова, Т. Г.; Baklanov, A.; Хвостов, Михаил В.; Сорокина, И. В.; Жукова, Н. А.; An’kov, Sergey V.; Borovkova, Olga V.; Dultseva, G.G.; Болдырев, В. В.; Фомин, В. М.; Huang, G. S.

doi:10.1016/j.jaerosci.2014.08.004

Cited by 18 publications

(10 citation statements)

References 25 publications

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“…In our previous works we have studied the pulmonary delivery of aerosolized non-steroid anti-inflammatory, 19 , 20 , 21 hypotensive, 22 anti-tuberculous drugs. 23 The dependence of lung deposition efficiency and delivered dose on particle size was investigated.…”

Section: Introductionmentioning

confidence: 99%

Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections

Valiulin

Onischuk

Dubtsov

et al. 2021

Journal of Pharmaceutical Sciences

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Under pandemic-caused emergency, evaluation of the potential of existing antiviral drugs for the treatment of COVID-19 is relevant. Triazavirin, an antiviral drug developed in Russia for per-oral administration, is involved in clinical trials against SARS-CoV-2 coronavirus. This virus has affinity to epithelial cells in respiratory tract, so drug delivery directly in lungs may enhance therapeutic effect and reduce side effects for stomach, liver, kidneys. We elaborated ultrasonic method of triazavirin aerosol generation and investigated the inhalation delivery of this drug in mice. Mean particle size and number concentration of aerosol used in inhalation experiments are 560 nm and 4 × 10 5 cm −3 , respectively. Aerosol mass concentration is 1.6 × 10 −4 mg/cm 3 . Inhalation for 20 min in a nose-only chamber resulted in 2 mg/kg body delivered dose and 2.6 μg/mL triazavirin concentration in blood plasma. Elimination rate constant determined in aerosol administration experiments was k e = 0.077 min −1 , which agrees with the value measured after intravenous delivery, but per-oral administration resulted in considerably lower apparent elimination rate constant of pseudo-first order, probably due to non-linear dependence of absorption rate on triazavirin concentration in gastrointestinal tract. The bioavailability of triazavirin aerosol is found to be 85%, which is about four times higher than for per-oral administration.

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Section: Introductionmentioning

confidence: 99%

Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections

Valiulin

Onischuk

Dubtsov

et al. 2021

Journal of Pharmaceutical Sciences

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“…The particle size of molecules is essential in order to deliver the drug to the targeted cells. The particles between 10 and 20 nm in size deposited to the alveolar region are about four times more efficient than those several microns in diameter 15. The smaller the particles are, the more efficient the delivery, It could be however depending on the delivery system used.…”

Section: Introductionmentioning

confidence: 99%

<p>Optimization of nanoemulsion containing gemcitabine and evaluation of its cytotoxicity towards human fetal lung fibroblast (MRC5) and human lung carcinoma (A549) cells</p>

Wahgiman

Salim

Rahman

et al. 2019

IJN

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BackgroundGemcitabine (GEM) is a chemotherapeutic agent, which is known to battle cancer but challenging due to its hydrophilic nature. Nanoemulsion is water-in-oil (W/O) nanoemulsion shows potential as a carrier system in delivering gemcitabine to the cancer cell.MethodsThe behaviour of GEM in MCT/surfactants/NaCl systems was studied in the ternary system at different ratios of Tween 80 and Span 80. The system with surfactant ratio 3:7 of Tween 80 and Span 80 was chosen for further study on the preparation of nanoemulsion formulation due to the highest isotropic region. Based on the selected ternary phase diagram, a composition of F1 was chosen and used for optimization by using the D-optimal mixture design. The interaction variables between medium chain triglyceride (MCT), surfactant mixture Tween 80: Span 80 (ratio 3:7), 0.9 % sodium chloride solution and gemcitabine were evaluated towards particle size as a response.ResultsThe results showed that NaCl solution and GEM gave more effects on particle size, polydispersity index and zeta potential of 141.57±0.05 nm, 0.168 and −37.10 mV, respectively. The optimized nanoemulsion showed good stability (no phase separation) against centrifugation test and storage at three different temperatures. The in vitro release of gemcitabine at different pH buffer solution was evaluated. The results showed the release of GEM in buffer pH 6.5 (45.19%) was higher than GEM in buffer pH 7.4 (13.62%). The cytotoxicity study showed that the optimized nanoemulsion containing GEM induced cytotoxicity towards A549 cell and at the same time reduced cytotoxicity towards MRC5 when compared to the control (GEM solution).

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“…During the past few decades, the need to measure aerosol properties has increased tremendously , therefore, refined techniques are necessary to control the dynamics of aerosol pollution from industrial activity, volcanic eruptions, cigarette smoke, motor vehicle emissions, and resuspended soil (Harrison 1986;Chow 1995;Colbeck 1995;Giechaskiel et al 2014;Amaral et al 2015). On the contrary, new technologies for "desirable" aerosol production are developed by material scientists and engineers to produce nanopowders and pigments (Guo et al 2010;Gevorkyan et al 2017), nanoaerosol drugs (Onischuk et al 2014(Onischuk et al , 2016, and flowing precursors for chemical reactors (Powell et al 2017). Aerosol measurements are of immense importance in these applications.…”

Section: Introductionmentioning

confidence: 99%

Determination of the aerosol particle size distribution by means of the diffusion battery: Analytical inversion

Onischuk

Valiulin

Baklanov

et al. 2018

Aerosol Science and Technology

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The algorithm of the analytical inversion of aerosol size distribution is proposed in this work. As the diffusion battery separates particles into several fractions according to their diffusivity, the total spectrum can be represented as the sum of spectra of fractions. Analytical formulas are derived to calculate mean diameters for particles in different fractions using diffusion battery penetrations as input parameters. The spectra of fractions are approximated by lognormal functions. Two analytical solutions for the aerosol size distribution inversion problem are discussed. The sizing accuracy of analytical solutions is investigated, comparing them with the measurements through transmission electron microscopy using the laboratory-generated NaCl aerosol. The agreement is demonstrated to be within 10% accuracy. It is shown that in case of two-mode size distribution, the spectrum components are well resolved for rather distant peaks (modal diameters of 10 and 300 nm) and poorly resolved for nearby modes (50 and 300 nm). To improve the peak resolution, the procedure of spectrum correction is applied demonstrating an excellent peak separation. Finally, the peak resolution is experimentally verified for the laboratory-generated two-mode spectra of tungsten oxide-NaCl aerosol with the modal diameters of 10 and 60 nm, respectively. Both analytical solutions demonstrated good peak resolution.

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Generation, inhalation delivery and anti-hypertensive effect of nisoldipine nanoaerosol

Cited by 18 publications

References 25 publications

Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections

Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections

<p>Optimization of nanoemulsion containing gemcitabine and evaluation of its cytotoxicity towards human fetal lung fibroblast (MRC5) and human lung carcinoma (A549) cells</p>

Determination of the aerosol particle size distribution by means of the diffusion battery: Analytical inversion

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