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1

Gieszinger, Péter, Gábor Katona, Piroska Szabó-Révész, and Rita Ambrus. "Stability study of nasal powder formulation containing nanosized lamotrigine." Acta Pharmaceutica Hungarica 90, no. 1 (June 10, 2020): 27–31. http://dx.doi.org/10.33892/aph.2020.90.27-31.

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Drug administration through the nose offers great possibilities which have been discovered in the past few decades. Besides the most known local effect, systemic and central nervous system effect is also available, the administration is non-painful and the degradation effect of the gastrointestinal tract can be avoided. Amongst the nasal formulations, powders have become more popular as their stability is favorable compared to the liquid formulations and a higher dose can be administered in powder form. The quality insurance and stability of the products in the pharmaceutical field have gained considerable attention in the last decades. Due to this fact, the aim was to execute a long-term stability study of a previously developed, nanosized lamotrigine (LAM) containing nasal powder (NP) formulation. The results of the stability test showed that the NP formulation preserved its key properties (particle size, morphology, structure and in vitro drug release) after 6 months of storage.
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2

Ishikawa, Fusashi, Masaki Katsura, Ikumi Tamai, and Akira Tsuji. "Improved nasal bioavailability of elcatonin by insoluble powder formulation." International Journal of Pharmaceutics 224, no. 1-2 (August 2001): 105–14. http://dx.doi.org/10.1016/s0378-5173(01)00736-0.

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3

Garmise, Robert J., Kevin Mar, Timothy M. Crowder, C. Robin Hwang, Matthew Ferriter, Juan Huang, John A. Mikszta, Vincent J. Sullivan, and Anthony J. Hickey. "Formulation of a dry powder influenza vaccine for nasal delivery." AAPS PharmSciTech 7, no. 1 (March 2006): E131—E137. http://dx.doi.org/10.1208/pt070119.

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4

Wang, Sheena H., Shaun M. Kirwan, Soman N. Abraham, Herman F. Staats, and Anthony J. Hickey. "Stable Dry Powder Formulation for Nasal Delivery of Anthrax Vaccine." Journal of Pharmaceutical Sciences 101, no. 1 (January 2012): 31–47. http://dx.doi.org/10.1002/jps.22742.

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5

Gieszinger, Péter, Ildikó Csóka, Edina Pallagi, Gábor Katona, Orsolya Jójárt-Laczkovich, Piroska Szabó-Révész, and Rita Ambrus. "Preliminary study of nanonized lamotrigine containing products for nasal powder formulation." Drug Design, Development and Therapy Volume 11 (August 2017): 2453–66. http://dx.doi.org/10.2147/dddt.s138559.

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6

Pearson, Richard G., Tahir Masud, Elaine Blackshaw, Andrew Naylor, Michael Hinchcliffe, Kirk Jeffery, Faron Jordan, et al. "Nasal Administration and Plasma Pharmacokinetics of Parathyroid Hormone Peptide PTH 1-34 for the Treatment of Osteoporosis." Pharmaceutics 11, no. 6 (June 7, 2019): 265. http://dx.doi.org/10.3390/pharmaceutics11060265.

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Nasal delivery of large peptides such as parathyroid 1-34 (PTH 1-34) can benefit from a permeation enhancer to promote absorption across the nasal mucosa into the bloodstream. Previously, we have published an encouraging bioavailability (78%), relative to subcutaneous injection in a small animal preclinical model, for a liquid nasal spray formulation containing the permeation enhancer polyethylene glycol (15)-hydroxystearate (Solutol® HS15). We report here the plasma pharmacokinetics of PTH 1-34 in healthy human volunteers receiving the liquid nasal spray formulation containing Solutol® HS15. For comparison, data for a commercially manufactured teriparatide formulation delivered via subcutaneous injection pen are also presented. Tc-99m-DTPA gamma scintigraphy monitored the deposition of the nasal spray in the nasal cavity and clearance via the inferior meatus and nasopharynx. The 50% clearance time was 17.8 min (minimum 10.9, maximum 74.3 min). For PTH 1-34, mean plasma Cmax of 5 pg/mL and 253 pg/mL were obtained for the nasal spray and subcutaneous injection respectively; relative bioavailability of the nasal spray was ≤1%. Subsequently, we investigated the pharmacokinetics of the liquid nasal spray formulation as well as a dry powder nasal formulation also containing Solutol® HS15 in a crossover study in an established ovine model. In this preclinical model, the relative bioavailability of liquid and powder nasal formulations was 1.4% and 1.0% respectively. The absolute bioavailability of subcutaneously administered PTH 1-34 (mean 77%, range 55–108%) in sheep was in agreement with published human data for teriparatide (up to 95%). These findings have important implications in the search for alternative routes of administration of peptides for the treatment of osteoporosis, and in terms of improving translation from animal models to humans.
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7

Nižić Nodilo, Laura, Ivo Ugrina, Drago Špoljarić, Daniela Amidžić Klarić, Cvijeta Jakobušić Brala, Mirna Perkušić, Ivan Pepić, et al. "A Dry Powder Platform for Nose-to-Brain Delivery of Dexamethasone: Formulation Development and Nasal Deposition Studies." Pharmaceutics 13, no. 6 (May 26, 2021): 795. http://dx.doi.org/10.3390/pharmaceutics13060795.

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Nasal route of administration offers a unique opportunity of brain targeted drug delivery via olfactory and trigeminal pathway, providing effective CNS concentrations at lower doses and lower risk for adverse reactions compared to systemic drug administration. Therefore, it has been recently proposed as a route of choice for glucocorticoids to control neuroinflammation processes in patients with severe Covid-19. However, appropriate delivery systems tailored to enhance their efficacy yet need to emerge. In this work we present the development of sprayable brain targeting powder delivery platform of dexamethasone sodium phosphate (DSP). DSP-loaded microspheres, optimised employing Quality-by-Design approach, were blended with soluble inert carriers (mannitol or lactose monohydrate). Powder blends were characterized in terms of homogeneity, flow properties, sprayability, in vitro biocompatibility, permeability and mucoadhesion. Nasal deposition studies were performed using 3D printed nasal cavity model. Mannitol provided better powder blend flow properties compared to lactose. Microspheres blended with mannitol retained or enlarged their mucoadhesive properties and enhanced DSP permeability across epithelial model barrier. DSP dose fraction deposited in the olfactory region reached 17.0% revealing the potential of developed powder platform for targeted olfactory delivery. The observed impact of nasal cavity asymmetry highlighted the importance of individual approach when aiming olfactory region.
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Tos, Mirko, Frank Svendstrup, Helge Arndal, Steffen Ørntoft, John Jakobsen, Peter Borum, Camilla Schrewelius, et al. "Efficacy of an Aqueous and a Powder Formulation of Nasal Budesonide Compared in Patients with Nasal Polyps." American Journal of Rhinology 12, no. 3 (May 1998): 183–90. http://dx.doi.org/10.2500/105065898781390217.

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Nasal polyps are commonly treated surgically. Intranasal administration of topical corticosteroids has gained increased acceptance as a treatment alternative. The aim of our study was to compare the efficacy of treatment of two formulations of budesonide with placebo on nasal polyps. At four Danish clinics 138 patients suffering from moderate or severe nasal polyps were randomized to a twice daily treatment with Rhinocort® Aqua 128 μg, Rhinocort Turbuhaler® 140 μg or placebo (Astra Draco, Sweden) for 6 weeks. Polyp size (primary efficacy variable), nasal symptoms, sense of smell, and patients’ overall evaluation of treatment of efficacy were assessed by scores. Polyp size was reduced significantly in both budesonide treated groups compared with placebo, but there was no statistical difference between the two actively treated groups. Patients’ nasal symptom scores was significantly more reduced in the Aqua compared to the Turbuhaler treated group, and both reduced symptom scores were significantly better compared to placebo. Sense of smell was significantly improved in the actively treated groups compared to placebo. The proportion of patients rating substantial or total control over symptoms after 6 weeks treatment was 60.9% and 48.2% in the Aqua and Turbuhaler-treated groups, respectively, which was significantly better compared with 29.8% in the placebo-treated group. Rhinocort Aqua and Rhinocort Turbuhaler were equally well tolerated.
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9

Dai, Jiajia, Benfang Ruan, Ying Zhu, Xianrui Liang, Feng Su, and Weike Su. "Preparation of nanosized Fluticasone Propionate nasal spray with improved stability and uniformity." Chemical Industry and Chemical Engineering Quarterly 21, no. 3 (2015): 457–64. http://dx.doi.org/10.2298/ciceq140609001d.

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Transmucosal nasal delivery has been recognized as up-and-coming option for delivery of therapeutic compounds. However, the short residence time of the formulation within the nasal cavity coupled to its low permeability is regarded as the barrier to good bioavailability. To overcome those limitations, we developed a new formulation - nanosized Fluticasone Propionate (FP) nasal spray. High pressure homogenization (HPH) was employed to achieve effective particle size reduction. Latin square experimental design (LSED) was implemented for high pressure homogenization process. With optimized process conditions, the resulting particles were less than 250 nm in size. The aging effect in FP nanosuspensions after 30-day refrigerated storage was not considerable. However, for long-term storage, a combination of homogenization and lyophilization (HL) was required to acquire stable FP nanocystals. The crystallinity of FP was examined by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), and no alternation was observed before or after homogenization and lyophilization process. The finished nasal spray offered a more uniform drug content compared to marketed formulation, which ensure the consistency and reproducibility of dose delivery. The study confirmed the effectiveness of homogenization, the usefulness of Latin square design and the feasibility of nano nasal spray.
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10

Trows, Sabrina, and Regina Scherließ. "Carrier-based dry powder formulation for nasal delivery of vaccines utilizing BSA as model drug." Powder Technology 292 (May 2016): 223–31. http://dx.doi.org/10.1016/j.powtec.2016.01.042.

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11

Martignoni, Isabella, Valentina Trotta, Wing-Hin Lee, Ching-Yee Loo, Michele Pozzoli, Paul M. Young, Santo Scalia, and Daniela Traini. "Resveratrol solid lipid microparticles as dry powder formulation for nasal delivery, characterization andin vitrodeposition study." Journal of Microencapsulation 33, no. 8 (November 16, 2016): 735–42. http://dx.doi.org/10.1080/02652048.2016.1260659.

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12

Bartos, Csilla, Edina Pallagi, Piroska Szabó-Révész, Rita Ambrus, Gábor Katona, Tamás Kiss, Mernaz Rahimi, and Ildikó Csóka. "Formulation of levodopa containing dry powder for nasal delivery applying the quality-by-design approach." European Journal of Pharmaceutical Sciences 123 (October 2018): 475–83. http://dx.doi.org/10.1016/j.ejps.2018.07.061.

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13

Imran, Syed Ali, Obinna Esomchukwu, and Remigius Agu. "Development of Intranasal Levothyroxine Powder Delivery for Hypothyroidism." Journal of the Endocrine Society 5, Supplement_1 (May 1, 2021): A828—A829. http://dx.doi.org/10.1210/jendso/bvab048.1689.

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Abstract Background: Hypothyroidism affects 3-5% of the general population with oral levothyroxine (LT4) being the predominant replacement therapy. However, significant proportion of hypothyroid patients are unable to absorb oral replacement leading to therapeutic failure and may require injectable thyroxine. Objectives: To develop non-invasive, less costly, and patient-friendly LT4 nasal delivery alternative using mucoadhesive polymers: chitosan and hydroxypropylmethylcellulose (HPMC). Methods: Six nasal LT4 formulations were developed with either chitosan or hydroxypropyl methylcellulose as mucoadhesive. The formulations were prepared through freeze-drying by varying the drug to polymer ratio (1:1, 1:3, and 1:5). The percentage drug yield was calculated by analyzing the weight of the formulation pre- and post-freeze drying. HPLC analysis was conducted to determine the amount of LT4 loaded in each formulation. Furthermore, the surface morphology, particle size, zeta potential, differential scanning calorimetry, X-ray diffraction as well as the in vitro release were assessed to determine the physicochemical properties and release characteristics of the formulations, respectively. Results: Both percentage drug loading and yield were > 70% for all the formulations. The freeze-dried formulations displayed a compact needle-like surface morphology. LT4-chitosan formulations, 1:1, 1:3, and 1:5 had mean particle size of 2.45 ± 0.88 µm, 2.76 ± 1.38 µm, and 1.59 ± 0.27 µm, respectively. Mean particle sizes for 1:1, 1:3, and 1:5 LT4-HPMC formulations were 0.56 ± 0.02 µm, 0.22 ± 0.06 µm, and 0.46 ± 0.04 µm. Zeta potential for LT4-chitosan formulation 1:1, 1:3, and 1:5 were -18.7 ± 1.00 mV, -16.2 ± 0.79 mV, and -19.17 ± 1.01 mV, respectively. LT4-HPMC 1:1, 1:3, and 1:5 formulations had zeta charges of -11.66 ± 3.16 mV, -6.06 ± 3.92 mV, and -9.53 ± 1.68 mV, respectively. Differential calorimetric analysis confirmed drug-polymer integration in all formulations, and X-ray powder diffraction showed both chitosan and HPMC formulations as crystalline configuration. The formulations with the highest in vitro release were LT4-HPMC 1:3 and LT4-chitosan 1:5. Conclusions: Results of this study suggest that both chitosan and HPMC can be used as sustained release polymers for the intranasal delivery of LT4.
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14

Engio, Lisa, and Remigius U. Agu. "Systemic Delivery of Peptide Hormones Using Nasal Powders: Strategies and Future Perspectives." Drug Delivery Letters 9, no. 4 (October 31, 2019): 286–98. http://dx.doi.org/10.2174/2210303109666190617170026.

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Background: Peptide Hormones (PH) are mainly administered as parenteral injections due to their peculiar physicochemical properties, and susceptibility to enzymatic degradation after oral administration. With invasive routes, however, patient safety, acceptability, and compliance become a concern, especially when a patient has a chronic condition that requires repeated injections. The delivery of peptide hormones via the nasal route has gained momentum over the last few decades as a noninvasive alternative to parenteral injections and commercially available nasal liquid products. Objective: The aim of this paper was to review: (1) The benefits and limitations of nasal powder products, (2) Formulation strategies to enhance nasal delivery of peptide hormone drugs, (3) Nasal powder devices, and (4) Future perspectives of therapeutic nasal powders. The drugs examined specifically include calcitonin, desmopressin, ghrelin, glucagon, human growth hormone, insulin, octreotide, and oxytocin. Methods:: Nasal delivery of peptide hormones using powders was reviewed with the following databases: EBSCO, PUBMED, Web of Science, ClinicalTrials.gov, and EU Clinical Trials Register. Results: Nasal powders are a promising drug delivery system that may be safer and more effective than traditional injections and presently marketed nasal liquids for peptide hormone drugs. Conclusion: With sustained interest and growing body of supporting evidence, a range of nasal powders for systemic delivery of these drugs and delivery devices can be expected to enter the market in the future and offer more options to patients
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15

Trenkel, Marie, and Regina Scherließ. "Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects." Pharmaceutics 13, no. 3 (March 13, 2021): 385. http://dx.doi.org/10.3390/pharmaceutics13030385.

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Nasal drug delivery is still primarily associated with locally-effective drugs, but next-generation products utilising the benefits of nasal administration—such as easy access to a relatively permeable mucosa, the presence of immunocompetent cells, and a direct route to the brain—are under investigation. Nasal powders offer the potential to improve the drugs’ effects by providing higher resistance against the mucociliary clearance, and thus prolonging the contact time of the drug with its target site. However, suitable and easy-to-use in-vitro setups tailored to the characterisation of this effect are missing. In this study, a selection of excipients for powder formulations were used to evaluate the applicability of different methods which investigate the influence on the contact time. The combination of the assessment of rheological properties, dynamic vapour sorption, and adhesiveness on agar–mucin plates was found to be a valuable predictive tool. For the additional assessment of the sensations associated with the close contact of powders and the mucosa, a slug mucosal irritation assay was conducted and adapted to powders. These methods are regarded as being especially useful for comparative screenings in early formulation development.
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16

Derakhshan, Alireza, Mahmood Khodadoost, Mostafa Ghanei, Latif Gachkar, Homa Hajimahdipour, Ali Taghipour, Jaleh Yousefi, Maryam Khoshkhui, and Farahzad J. Azad. "Effects of a Novel Barley-Based Formulation on Allergic Rhinitis: A Randomized Controlled Trial." Endocrine, Metabolic & Immune Disorders - Drug Targets 19, no. 8 (November 11, 2019): 1224–31. http://dx.doi.org/10.2174/1871530319666190306100611.

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Objective: Current treatment options for Allergic Rhinitis (AR) may have their own limitations and side effects. This study aimed to investigate the effects of Ma-al-Shaeer (MS), a novel natural formulation based on Hordeum vulgare, in the treatment of AR compared with Fexofenadine (FX). Methods: A total of 77 patients with AR were divided into two groups: MS group (n=38) and FX group (n=39). The first group received 15 g of dried MS powder, and the second group received 60 mg of FX twice daily for 14 days. At baseline (week zero) and after the 14-day treatment period (week two), both groups were evaluated for sneezing, rhinorrhea, nasal congestion, nasal itching, post nasal drip, eye, throat, or ear symptoms, headache, cough, mental function, quality of life scores, blood eosinophil count and total IgE levels. Rhinitis control assessment tests were conducted at week zero and again at one week after cessation of treatment (week three) in both groups. Results: All symptoms of AR except cough were significantly reduced in both groups; for nasal congestion, post nasal drip, and headache, the MS treatment was found to be superior. Rhinitis control was significantly increased after treatment in both groups (p value < 0.001). Both drugs significantly reduced total IgE levels. There was no significant change in eosinophil count in either group. Conclusion: MS formulation based on H. vulgare may be an effective treatment for AR. Further studies are needed to confirm the effect of MS as an alternative treatment in AR.
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Yang, William H., Jerry Dolovich, Michel A. Drouin, Paul Keith, Jennifer Haddon, Barbara Jennings, and the Rhinocort Study Group. "Comparison of Budesonide Turbuhaler with Budesonide Aqua in the Treatment of Seasonal Allergic Rhinitis." Canadian Respiratory Journal 5, no. 6 (1998): 455–60. http://dx.doi.org/10.1155/1998/639710.

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OBJECTIVE: To compare the effect of budesonide Turbuhaler 400 µg/day with budesonide aqua 256 µg/day in the treatment of seasonal allergic rhinitis (SAR). Secondarily to ascertain patients' preferences for the two nasal devices and to assess quality of life.DESIGN: Randomized, multicentre, double-blind, double- dummy, parallel groups study.SETTING: Private practices and hospital clinics in Ontario, Quebec and Manitoba.POPULATION: Two hundred and eighty-four out-patients with SAR, who were symptomatic during the ragweed season, volunteered for enrolment (243 randomized).RESULTS: Mean daily nasal symptom scores were significantly reduced with treatment. There were no statistically significant changes from baseline for eye symptoms. Most patients (more than 80%) achieved substantial control of their symptoms with budesonide. The most common nasal and non-nasal adverse events for both groups were epistaxis and headache. Turbuhaler was easier to use and more convenient to carry, had less of an unpleasant taste, and caused less nasal irritation than the aqua spray. More than twice as many patients preferred Turbuhaler to the aqua spray (69% versus 31%). Improvement in quality of life from baseline to clinic visits was statistically significant in both groups.CONCLUSION: Once daily use of 256 mg of budesonide aqua and 400 mg of budesonide Turbuhaler are equally safe and efficacious in the treatment of SAR. Patients preferred the budesonide powder formulation delivered via Turbuhaler two to one over the aqua formulation.
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18

Gieszinger, Péter, Tamás Kiss, Piroska Szabó-Révész, and Rita Ambrus. "The Development of an In Vitro Horizontal Diffusion Cell to Monitor Nasal Powder Penetration Inline." Pharmaceutics 13, no. 6 (May 28, 2021): 809. http://dx.doi.org/10.3390/pharmaceutics13060809.

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The development of in vitro investigation models could be important using sensitive and fast methods during formulation. Intranasal applied drugs (meloxicam, lamotrigine, and levodopa) avoid the gastrointestinal tract and can achieve higher bioavailability, therefore a penetration extent is a key property. In this study, the in vitro adaptability of a modified horizontal diffusion cell was tested by using these model active pharmaceutical ingredients (APIs). The special factors consisted of the volume of the chambers, the arrangement of the stirrers, the design of probe input for real-time analysis and decreased membrane area. Membranes were impregnated by isopropyl myristate and by using phosphate buffer to evaluate the effect of API hydrophilicity on the diffusion properties. The lipophilicity of the API was proportional to the penetration extent through isopropyl myristate-impregnated membranes compared with buffer-soaked membranes. After evaluating the arithmetic mean of standard relative deviations and the penetrated extent of APIs at 15 min, Metricel® could be suggested for levodopa and meloxicam, and Whatman™ for lamotrigine. The modified model is suitable for inline, real-time detection, at nasal conditions, using small volumes of phases, impregnated membrane, to monitor the diffusion of the drug and to determine its concentration in the acceptor and donor phases.
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19

Rossi, Irene, Francesca Buttini, Fabio Sonvico, Filippo Affaticati, Francesco Martinelli, Giannamaria Annunziato, Diana Machado, Miguel Viveiros, Marco Pieroni, and Ruggero Bettini. "Sodium Hyaluronate Nanocomposite Respirable Microparticles to Tackle Antibiotic Resistance with Potential Application in Treatment of Mycobacterial Pulmonary Infections." Pharmaceutics 11, no. 5 (May 1, 2019): 203. http://dx.doi.org/10.3390/pharmaceutics11050203.

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Tuberculosis resistant cases have been estimated to grow every year. Besides Mycobacterium tuberculosis, other mycobacterial species are responsible for an increasing number of difficult-to-treat infections. To increase efficacy of pulmonary treatment of mycobacterial infections an inhalable antibiotic powder targeting infected alveolar macrophages (AMs) and including an efflux pump inhibitor was developed. Low molecular weight sodium hyaluronate sub-micron particles were efficiently loaded with rifampicin, isoniazid and verapamil, and transformed in highly respirable microparticles (mean volume diameter: 1 μm) by spray drying. These particles were able to regenerate their original size upon contact with aqueous environment with mechanical stirring or sonication. The in vitro drugs release profile from the powder was characterized by a slow release rate, favorable to maintain a high drug level inside AMs. In vitro antimicrobial activity and ex vivo macrophage infection assays employing susceptible and drug resistant strains were carried out. No significant differences were observed when the powder, which did not compromise the AMs viability after a five-day exposure, was compared to the same formulation without verapamil. However, both preparations achieved more than 80% reduction in bacterial viability irrespective of the drug resistance profile. This approach can be considered appropriate to treat mycobacterial respiratory infections, regardless the level of drug resistance.
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Pozzoli, Michele, Philippe Rogueda, Bing Zhu, Timothy Smith, Paul M. Young, Daniela Traini, and Fabio Sonvico. "Dry powder nasal drug delivery: challenges, opportunities and a study of the commercial Teijin Puvlizer Rhinocort device and formulation." Drug Development and Industrial Pharmacy 42, no. 10 (March 22, 2016): 1660–68. http://dx.doi.org/10.3109/03639045.2016.1160110.

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21

Brunaugh, Ashlee D., Hyojong Seo, Zachary Warnken, Li Ding, Sang Heui Seo, and Hugh D. C. Smyth. "Development and evaluation of inhalable composite niclosamide-lysozyme particles: A broad-spectrum, patient-adaptable treatment for coronavirus infections and sequalae." PLOS ONE 16, no. 2 (February 11, 2021): e0246803. http://dx.doi.org/10.1371/journal.pone.0246803.

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Niclosamide (NIC) has demonstrated promising in vitro antiviral efficacy against SARS-CoV-2, the causative agent of the COVID-19 pandemic. Though NIC is already FDA-approved, administration of the currently available oral formulation results in systemic drug levels that are too low for the inhibition of SARS-CoV-2. We hypothesized that the co-formulation of NIC with an endogenous protein, human lysozyme (hLYS), could enable the direct aerosol delivery of the drug to the respiratory tract as an alternative to oral delivery, thereby effectively treating COVID-19 by targeting the primary site of SARS-CoV-2 acquisition and spread. To test this hypothesis, we engineered and optimized composite particles containing NIC and hLYS suitable for delivery to the upper and lower airways via dry powder inhaler, nebulizer, and nasal spray. The novel formulation demonstrates potent in vitro and in vivo activity against two coronavirus strains, MERS-CoV and SARS-CoV-2, and may offer protection against methicillin-resistance staphylococcus aureus pneumonia and inflammatory lung damage occurring secondary to SARS-CoV-2 infections. The suitability of the formulation for all stages of the disease and low-cost development approach will ensure rapid clinical development and wide-spread utilization.
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Vakhitov, T. R., V. E. Katnov, P. V. Grishin, S. N. Stepin, and D. O. Grigoriev. "Biofriendly nanocomposite containers with inhibition properties for the protection of metallic surfaces." Proceedings of the Royal Society A: Mathematical, Physical and Engineering Sciences 473, no. 2199 (March 2017): 20160827. http://dx.doi.org/10.1098/rspa.2016.0827.

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An attempt to combine two ‘green’ compounds in nanocomposite microcontainers in order to increase protection properties of waterborne acryl-styrene copolymer (ASC) coatings has been made. N -lauroylsarcosine (NLS) served as a corrosion inhibitor, and linseed oil (LO) as a carrier-forming component. LO is compatible with this copolymer and can impart to the coating self-healing properties. For the evaluation of the protective performance, three types of coatings were compared. In the first two, NLS was introduced in the coating formulation in the forms of free powder and micro-containers filled with LO, correspondingly. The last one was a standard ASC coating without inhibitor at all. Low-carbon steel substrates were coated by these formulations by spraying and subjected subsequently to the neutral salt spray test according to DIN ISO 9227. Results of these tests as well as the data obtained by electrochemical study suggest that such containers can be used for the improvement of adhesion of ASC-based coatings to the substrate and for the enhancement of their protective performance upon integrity damage, whereas the barrier properties of intact coatings were decreased.
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Fransén, N., U. Espefält Westin, C. Nyström, and E. Björk. "The in vitro transport of dihydroergotamine across porcine nasal respiratory and olfactory mucosa and the effect of a novel powder formulation." Journal of Drug Delivery Science and Technology 17, no. 4 (2007): 267–71. http://dx.doi.org/10.1016/s1773-2247(07)50094-8.

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Fallacara, Arianna, Laura Busato, Michele Pozzoli, Maliheh Ghadiri, Hui Xin Ong, Paul M. Young, Stefano Manfredini, and Daniela Traini. "In vitro characterization of physico-chemical properties, cytotoxicity, bioactivity of urea-crosslinked hyaluronic acid and sodium ascorbyl phosphate nasal powder formulation." International Journal of Pharmaceutics 558 (March 2019): 341–50. http://dx.doi.org/10.1016/j.ijpharm.2019.01.012.

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Salatin, Sara, Jaleh Barar, Mohammad Barzegar-Jalali, Khosro Adibkia, Mitra Alami-Milani, and Mitra Jelvehgari. "Formulation and Evaluation of Eudragit RL-100 Nanoparticles Loaded In-Situ Forming Gel for Intranasal Delivery of Rivastigmine." Advanced Pharmaceutical Bulletin 10, no. 1 (December 11, 2019): 20–29. http://dx.doi.org/10.15171/apb.2020.003.

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Purpose: Rivastigmine hydrogen tartrate (RHT) is commonly used for the treatment of mild to moderate Alzheimer’s disease (AD). The aim of this work was to formulate in-situ pluronic F-127 (PF-127) hydrogels containing Eudragit RL-100 (EU-RL) nanoparticles (NPs) in order to improve the therapeutic efficacy of RHT through the nasal route. Methods: The NPs were prepared using different polymer to drug ratios and evaluated for their physicochemical characteristics, cellular uptake and in vitro cytotoxicity against lung adenocarcinoma cells (A459). PF-127 nanoformulations were prepared via cold method and analyzed in terms of physicochemical properties and drug release profiles. The nanoformulations and plain drug gel were then assessed by ex vivo permeation studies across the sheep nasal mucosa. Results: The EU-RL NPs exhibited a particle size within the range of 118 to 154 nm and positive zeta potential values of 22.5 to 30 mV with an approximately spherical shape. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD) suggested no drug to polymer interaction through the preparation of nanoformulations. The RHT-loaded NPs exhibited an acceptable cytocompatibility with a time- and dose-dependent cellular internalization. Conclusion: Our results clearly indicated the potential of nanoformulations as controlled release systems to improve the therapeutic efficacy of RHT through the intranasal administration
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Jadam, Monica Limau, Zaemah Jubri, and Siti Halimah Sarijo. "Synthesis of Calcium/Aluminium-Ciprofloxacin-Layered Double Hydroxide for a New Antibacterial Drug Formulation." Solid State Phenomena 317 (May 2021): 233–38. http://dx.doi.org/10.4028/www.scientific.net/ssp.317.233.

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An antibacterial drug, ciprofloxacin (Cipro) was successfully encapsulated into Ca/Al-layered double hydroxide (CLDH) with molar ratio Ca/Al = 3:1 (R3) by anion exchange method at optimum concentration of 0.2 M Cipro. The successful intercalation was confirmed by patterns analysis of powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), elemental analysis (CHNS) and accelerated surface area and porosity (ASAP) analysis. Basal spacing of CLDH synthesized in this study is 8.7 Å. Due to the inclusion of Cipro into the layered CLDH, basal spacing expanded to 16.2 Å in Ca/Al-Cipro-LDH (CCLDH) compare to in CLDH. The FTIR spectra of the hybrid nanocomposite show resemblance peaks of the layered double hydroxide (LDH) and Cipro, indicating the inclusion of the drug anion into the LDH interlamellae. The percentage loading of Cipro calculated from the data obtained from CHNS is 75.9% (w/w). This shows that Ca/Al-layered double hydroxide, CLDH has prospective application as the host for ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid), an antibacterial drug for a novel drug delivery formulation.
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Dehghan, Solmaz, Masoumeh Tavassoti Kheiri, Khalil Abnous, Maryam Eskandari, and Mohsen Tafaghodi. "Preparation, characterization and immunological evaluation of alginate nanoparticles loaded with whole inactivated influenza virus: Dry powder formulation for nasal immunization in rabbits." Microbial Pathogenesis 115 (February 2018): 74–85. http://dx.doi.org/10.1016/j.micpath.2017.12.011.

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Strege, Mark A., Siyuan Huang, and Donald S. Risley. "Quantitative determination of beta-cyclodextrin in a powder insulin formulation for nasal delivery using hydrophilic interaction chromatography with evaporative light scattering detection." Journal of Liquid Chromatography & Related Technologies 42, no. 3-4 (February 25, 2019): 74–78. http://dx.doi.org/10.1080/10826076.2019.1571508.

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Jermy, B. Rabindran, Vijaya Ravinayagam, Widyan A. Alamoudi, Dana Almohazey, Hatim Dafalla, Lina Hussain Allehaibi, Abdulhadi Baykal, Muhammet S. Toprak, and Thirunavukkarasu Somanathan. "Targeted therapeutic effect against the breast cancer cell line MCF-7 with a CuFe2O4/silica/cisplatin nanocomposite formulation." Beilstein Journal of Nanotechnology 10 (November 12, 2019): 2217–28. http://dx.doi.org/10.3762/bjnano.10.214.

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The combination of magnetic nanoparticles with a porous silica is a composite that has attracted significant attention for potential multifunctional theranostic applications. In this study, 30 wt % CuFe2O4 was impregnated into a matrix of monodispersed spherical hydrophilic silica (HYPS) nanoparticles through a simple dry impregnation technique. The chemotherapy drug cisplatin was loaded through electrostatic equilibrium adsorption over 24 h in normal saline solution. The presence of cubic spinel CuFe2O4 on HYPS was confirmed through powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and diffuse reflectance UV–vis spectroscopy (DR UV–vis) analysis. The HYPS particles showed a surface area of 170 m2/g, pore size of 8.3 nm and pore volume of 0.35 cm3/g. The cisplatin/CuFe2O4/HYPS nanoformulation showed the accumulation of copper ferrite nanoparticles on the surface and in the pores of HYPS with a surface area of 45 m2/g, pore size of 16 nm and pore volume of 0.18 cm3/g. Transmission electron microscopy (TEM) and energy dispersive X-ray (EDX) mapping analysis showed the presence of homogeneous silica particles with nanoclusters of copper ferrite distributed on the HYPS support. Vibrating sample magnetometry (VSM) analysis of CuFe2O4/HYPS showed paramagnetic behavior with a saturated magnetization value of 7.65 emu/g. DRS UV–vis analysis revealed the functionalization of cisplatin in tetrahedral and octahedral coordination in the CuFe2O4/HYPS composite. Compared to other supports such as mesocellular foam and silicalite, the release of cisplatin using the dialysis membrane technique was found to be superior when CuFe2O4/HYPS was applied as the support. An in vitro experiment was conducted to determine the potential of CuFe2O4/HYPS as an anticancer agent against the human breast cancer cell line MCF-7. The results show that the nanoparticle formulation can effectively target cancerous cells and could be an effective tumor imaging guide and drug delivery system.
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Pesic, Marija, Frank Schippers, Rob Saunders, Lyn Webster, Martin Donsbach, and Thomas Stoehr. "Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial." European Journal of Clinical Pharmacology 76, no. 11 (September 4, 2020): 1505–16. http://dx.doi.org/10.1007/s00228-020-02984-z.

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Abstract Purpose Remimazolam is a novel and ultra-short-acting sedative currently developed for intravenous use in procedural sedation, general anesthesia, and ICU sedation. However, intravenous administration is not always appropriate, depending on the patient or setting. This study evaluated intranasal administration as a potential alternative route. Methods The study used a randomized, double-blind, 9 period cross-over design to compare the pharmacokinetics, pharmacodynamics, and safety of single intranasal doses of 10, 20, and 40 mg remimazolam (as powder or solution) with intranasal placebo and 4 mg intravenous remimazolam. Results Intranasal remimazolam powder had a consistent absolute bioavailability of approximately 50%; Tmax was 10 min; AUC and Cmax were dose-proportional. The higher doses of intranasal solution, however, resulted in decreasing bioavailability and loss of dose-proportionality in AUC and Cmax despite complete drug absorption due to partial swallowing of dose and the resulting first-pass effect. Pharmacodynamics were generally consistent with PK. Peak effects (drowsiness, relaxation, any, memory, response time) were in similar ranges after intranasal (10 to 40 mg) as intravenous (4 mg) dosing and were partially, but not consistently, dose-related. Safety results were generally consistent with other benzodiazepines; however, intranasal remimazolam (but not placebo) caused nasal discomfort/pain, in some cases even severe. Conclusions Intranasal administration of remimazolam was safe and caused sedative effects. However, the severe pain and discomfort caused by intranasal remimazolam prohibit its use by this route of administration, at least with the currently available intravenous formulation.
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Reno, Frederick E., Patrick Normand, Kevin McInally, Sherwin Silo, Patricia Stotland, Myriam Triest, Dolores Carballo, and Claude Piché. "A novel nasal powder formulation of glucagon: toxicology studies in animal models." BMC Pharmacology and Toxicology 16, no. 1 (October 26, 2015). http://dx.doi.org/10.1186/s40360-015-0026-9.

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Gomes dos Reis, Larissa, Maliheh Ghadiri, Paul Young, and Daniela Traini. "Nasal Powder Formulation of Tranexamic Acid and Hyaluronic Acid for the Treatment of Epistaxis." Pharmaceutical Research 37, no. 10 (September 4, 2020). http://dx.doi.org/10.1007/s11095-020-02913-w.

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