Absorption of drugs from the nasal mucosa of rat

Hirai, Shinichiro; Takatsuka, Yuichi; Matsuzawa, Tai; Mima, Hiroyuki

doi:10.1016/0378-5173(81)90058-2

Cited by 205 publications

(13 citation statements)

References 11 publications

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“…5,6) Cationic polymers, such as chitosan and PLA, enhance the in vivo nasal absorption of various water-soluble macromolecules without cytotoxicity to the nasal mucosa. [11][12][13][14][15]17) It has also been reported that these absorption-enhancing effects are dependent on the molecular weight and concentration. Thus, the molecular weight and concentration of polycationic compounds may be involved in their enhancing effect on the absorption of polar macromolecules.…”

Section: Fig 2 Simulated Absorption Profiles Of Fd-4 After In Co-mentioning

confidence: 97%

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Enhancement Effect of Poly-L-ornithine on the Nasal Absorption of Water-Soluble Macromolecules in Rats

Omori

Kamiya

Yamaki

et al. 2019

Biological & Pharmaceutical Bulletin

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The transnasal route for the delivery of water-soluble macromolecules, such as bioactive peptides and proteins, has attracted interest, although the use of permeation enhancers is required due to the poor permeabilities of these macromolecules across the nasal mucosa. With polycationic compounds, such as poly-L-arginine and chitosan, the nasal absorption of hydrophilic macromolecules is molecular weight-and concentration-dependently enhanced without causing cytotoxicity. In the present study, we evaluated the effect of various molecular weights and concentrations of poly-L-ornithine (PLO), a polycationic compound, on the nasal absorption and the damage to the nasal mucosa in vivo. PLO enhanced the nasal absorption of fluorescein isothiocyanate-dextran (FD-4), used as a model drug, and the bioavailability of FD-4 increased with the concentration of PLO. The enhancement effect was also dependent on the molecular weight. The administration of PLO at a concentration that sufficed for enhancing the nasal absorption had no effect on the activity of lactic dehydrogenase and the protein leakage in the nasal fluid, as indices of nasal mucosa damage. These findings suggest that a transnasal delivery system using PLO is a useful strategy for improving the nasal absorption of water-soluble macromolecules without toxicity to the nasal mucosa.

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Section: Fig 2 Simulated Absorption Profiles Of Fd-4 After In Co-mentioning

confidence: 97%

“…16) Of note, it has been reported that the enhancing effects of chitosan and PLA are dependent on the molecular weight and concentration applied. [11][12][13][14][15]17) This suggests that the enhancement effect of PLO may also be influenced by its molecular weight and concentration, but there were only few reports about its effect of PLO.…”

Section: Introductionmentioning

confidence: 99%

Enhancement Effect of Poly-L-ornithine on the Nasal Absorption of Water-Soluble Macromolecules in Rats

Omori

Kamiya

Yamaki

et al. 2019

Biological & Pharmaceutical Bulletin

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“…However, some nasal marketed products have reported an osmolality in the range 300-600 mOsmol/Kg. The formulation pH may interfere with the natural function of nasal lysozymes, which are defence enzymes active under acidic conditions36, (Shinichiro et al, 1981;Ellison and Giehl, Fig. 1.…”

Section: Liquid Formulationsmentioning

confidence: 99%

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

Salade

Wauthoz

Goole

et al. 2019

International Journal of Pharmaceutics

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Nasal delivery offers many benefits over other conventional routes of delivery (e.g. oral or intravenous administration). Benefits include, among others, a fast onset of action, non-invasiveness and direct access to the central nervous system. The nasal cavity is not only limited to local application (e.g. rhinosinusitis) but can also provide direct access to other sites in the body (e.g. the central nervous system or systemic circulation). However, both the anatomy and the physiology of the nose impose their own limitations, such as a small volume for delivery or rapid mucociliary clearance. To meet nasal-specific criteria, the formulator has to complete a plethora of tests, in vitro and ex vivo, to assess the efficacy and tolerance of a new drug-delivery system. Moreover, depending on the desired therapeutic effect, the delivery of the drug should target a specific pathway that could potentially be achieved through a modified release of this drug. Therefore, this review focuses on specific techniques that should be performed when a nasal formulation is developed. The review covers both the tests recommended by regulatory agencies (e.g. the Food and Drug Administration) and other complementary experiments frequently performed in the field.

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“…Number of errors (NE): = × (17) in vivo Studies Preparation of rats for drug administration: Animals were anaesthetized using a ketaminexylazine cocktail (70 mg/kg ketamine and 7 mg/kg xylazine). Then their trachea was intubated with feeding tube number 6 in order to enable animals to breathe (31).…”

Section: Sum Square Of Total Variation (Sst)mentioning

confidence: 99%

in vitro- and in vivo Evaluation of Methotrexate-Loaded Hydrogel Nanoparticles Intended to Treat Primary CNS Lymphoma via Intranasal Administration

et al. 2018

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The nano-formulation demonstrated an average particle size near 100 nm with a zeta potential of 18.65±1.77 mv. Loading efficiency and loading capacity were calculated to be 65.46±7.66 and 3.02±0.34 respectively. The Weibull model was found to be best describing the release phenomenon as a combination of swelling and Fickian diffusion. Moreover in in vivo studies, drug targeting efficiency and direct transport percentage for nanogel (test) and free drug solution (control) were 424.88% and 76.46% and 34842.15% and 99.71% respectively. Conclusion: According to in vivo studies, nanogel produced significantly higher concentration of MTX in the brain but not in the plasma when compared to the free drug solution. Besides, in comparison to intravenous administration of the same nanogel it was indicated that intranasal administration significantly increases the brain concentration of MTX.

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Absorption of drugs from the nasal mucosa of rat

Cited by 205 publications

References 11 publications

Enhancement Effect of Poly-L-ornithine on the Nasal Absorption of Water-Soluble Macromolecules in Rats

Enhancement Effect of Poly-L-ornithine on the Nasal Absorption of Water-Soluble Macromolecules in Rats

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

in vitro- and in vivo Evaluation of Methotrexate-Loaded Hydrogel Nanoparticles Intended to Treat Primary CNS Lymphoma via Intranasal Administration

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