Intranasal Drug Administration — An Attractive Delivery Route for Some Drugs

Marx, Degenhard; Williams, Gerallt; Birkhoff, Matthias

doi:10.5772/59468

Cited by 36 publications

(21 citation statements)

References 14 publications

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“…A limitation of the current trial design was the use of non-optimized IV formulation, resulting in the need to apply large volumes of either solution or powder in order to achieve clinical effects. These volumes were in both cases beyond what has been reported as optimal for nasal delivery [16,17], which could have resulted in lower absorption and bioavailability even at low doses. Therefore, while this trial clearly shows a low potential of the current formulation to be abused via the intranasal route, it offers no more than a proof of concept on the potential clinical use of the intranasal route for therapeutic purposes.…”

Section: Discussionmentioning

confidence: 76%

Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial

Pesic

Schippers

Saunders

et al. 2020

Eur J Clin Pharmacol

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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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Section: Discussionmentioning

confidence: 76%

Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial

Pesic

Schippers

Saunders

et al. 2020

Eur J Clin Pharmacol

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“…In addition, the nanocapsulated formulation has fewer adverse effects and is delivered in a controlled manner. The effectiveness of therapy is influenced by the size of nanoparticles, encapsulation efficiency, degree of drug release and surface charge of the drug on a nanometric support [33]. Currently, carriers are used to treat chronic diseases such as pulmonary tuberculosis, diabetes, cancer, atherosclerosis, Parkinson's disease, asthma and Alzheimer's disease [34].…”

Section: Drug Carriersmentioning

confidence: 99%

Analysis of the Exposure of Organisms to the Action of Nanomaterials

et al. 2020

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The rapid development of the production of materials containing metal nanoparticles and metal oxides is a potential risk to the environment. The degree of exposure of organisms to nanoparticles increases from year to year, and its effects are not fully known. This is due to the fact that the range of nanoparticle interactions on cells, tissues and the environment requires careful analysis. It is necessary to develop methods for testing the properties of nanomaterials and the mechanisms of their impact on individual cells as well as on entire organisms. The particular need to raise public awareness of the main sources of exposure to nanoparticles should also be highlighted. This paper presents the main sources and possible routes of exposure to metal nanoparticles and metal oxides. Key elements of research on the impact of nanoparticles on organisms, that is, in vitro tests, in vivo tests and methods of detection of nanoparticles in organisms, are presented.

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“…2 Examples of commercially available nasally administrated drugs in the form of gels, spray are decongestants for cold symptoms, antihistamines and corticosteroids for rhino sinusitis. 3 But, muco ciliary clearance, a major disadvantage associated with nasal route can be overcome by increasing the residence time in the nasal cavity through formulation of muco-adhesive in situ gel. 4,5 In situ hydrogels or prepared hydrogel-based formulations allow intimate contact with the mucosal surface, prolong the residence time and improve drug bioavailability over liquid preparations.…”

Section: Introductionmentioning

confidence: 99%

Sweet Basil Seed Mucilage as a Gelling agent in Nasal Drug Delivery

Avlani¹,

Ash²,

Majee³

et al. 2019

IJPTR

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Intranasal gel formulation with mucilage of natural origin has been potentially explored as an alternative dosage form of drug administration. The purpose of present investigation was to develop paracetamol loaded nasal gel with sweet basil seed mucilage (BSM) as a gelling agent obtained by thermal-hydration process and to characterise both mucilage as well as the gel formulations. Phytochemical screening of BSM reveals it to be rich in carbohydrates. The FT-IR spectrum of the mucilage exhibits the presence of O-H, C-H, and-COO −. The mucilage showed high swelling index of 462% and relative viscosity of BSM dispersion (0.25% w/v) in nasal medium was found to be 2.94 at 25⁰ C. Nasal gel formulations demonstrated satisfactory pH, spreadability, extrudibility and drug content. The in vitro release profile of G1 (6%w/w BSM) demonstrated almost 95% release with Korsmeyer-Peppas kinetics with highest values of permeability coefficient and steady-state flux. Other formulations with 8-10%w/w BSM exhibited 70-80% release within 2.5 hours. G2 and G3 followed zero order kinetics with quasi-Fickian diffusion. The study indicates that G1 (6 %w/w BSM) can be selected for nasal gel formulation which may be used for in vivo studies in future.

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Intranasal Drug Administration — An Attractive Delivery Route for Some Drugs

Cited by 36 publications

References 14 publications

Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial

Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial

Analysis of the Exposure of Organisms to the Action of Nanomaterials

Sweet Basil Seed Mucilage as a Gelling agent in Nasal Drug Delivery

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