Nasal Absorption of Propranolol in Rats

Hussain, Anwar; Hirai, Shinichiro; Bawarshi, Rima

doi:10.1002/jps.2600680942

Cited by 68 publications

(12 citation statements)

References 4 publications

(1 reference statement)

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“…For example, the blood concentration of propranolol following nasal application is similar to that after intravenous application. 27) Propranolol is a highly permeable drug. A small volume of the drug solution applied nasally can reach the surface of nasal epithelium, but without being dissolved, whereas powder formulations, when administered nasally, directly reach the surface of the nasal epithelium and are dissolved in the small fluid volume.…”

Section: Discussionmentioning

confidence: 99%

Nasal Drug Absorption from Powder Formulations: Effect of Fluid Volume Changes on the Mucosal Surface

Tanaka

Furubayashi

Enomura

et al. 2017

Biological & Pharmaceutical Bulletin

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The effect of changes in the mucosal fluid volume on the nasal drug absorption of powder formulations was evaluated using warfarin (WF), piroxicam (PXC), and norfloxacin (NFX) as model drugs. Lactose and sodium chloride (NaCl), which are water soluble and small-sized chemicals that increase osmotic pressure after dissolution, were used as excipients to change the mucosal fluid volume. The in vitro study using a Madin-Darby canine kidney (MDCK) cell monolayer indicated that lactose and NaCl, sprayed over the surface of air interface monolayers, increased the fluid volume on the monolayer surface and enhanced the transepithelial transport of the model drugs. The in vivo animal study indicated that the nasal absorption of PXC is enhanced by lactose and NaCl after nasal administration of the powder formulations. This is likely due to the enhanced dissolution of PXC on fluid-rich nasal mucosa and an increase in the effective surface area for drug permeation, which lead to better nasal absorption. However, both excipients failed to increase the nasal absorption of WF and NFX. To clarify the mechanism of the drug-dependent effect of lactose and NaCl, the nasal residence of the formulation was examined using FD70 as a non-absorbable marker. The nasal clearance of FD70 was enhanced by lactose and NaCl, leading to a decrease in the nasal drug absorption. Lactose and NaCl caused no damage to the nasal tissue. These results indicate that the addition of water-soluble excipients such as lactose to powder formulations can enhance the nasal absorption of highly permeable but poorly soluble drugs.Key words nasal drug absorption; powder formulation; lactose; osmotic pressure; nasal residence; mucociliary clearance Nasal drug application has gained a great deal of attention over the last few decades because of its great potential utility for systemic drug delivery. The range of drugs investigated for possible nasal application varies from lipophilic drugs to polar and hydrophilic molecules, including peptides and proteins.1-3) It offers an attractive alternative application for drugs that have limited oral bioavailability, are degradable by gastrointestinal fluid, or undergo high hepatic first-pass or gut-wall metabolism. In addition, nasal drug administration results in quick onset of action than oral and transdermal applications. 4,5) Because nasal administration is easier and less invasive than oral delivery, not only for the elderly but also for long-term-care patients with swallowing difficulties, it has considerable clinical potential for improving the QOL of both patients and care givers.

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Section: Discussionmentioning

confidence: 99%

Nasal Drug Absorption from Powder Formulations: Effect of Fluid Volume Changes on the Mucosal Surface

Tanaka

Furubayashi

Enomura

et al. 2017

Biological & Pharmaceutical Bulletin

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“…For example, propranolol, which is a highly permeable drug, shows a blood concentration profile following nasal application similar to that after intravenous administration [26]. In the case of nasal drug administration, a small volume of the drug solution (100 μL at most in humans) is applied.…”

Section: Discussionmentioning

confidence: 99%

Nasal Absorption of Macromolecules from Powder Formulations and Effects of Sodium Carboxymethyl Cellulose on Their Absorption

et al. 2016

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The nasal absorption of macromolecules from powder formulations and the effect of sodium carboxymethyl cellulose (CMC-Na) as a pharmaceutical excipient on their absorption were studied. Model macromolecules were fluorescein isothiocyanate-labeled dextran (average molecular weight of 4.4kDa, FD4) and insulin. The plasma concentration of FD4 after application of the powder containing 50% starch (control) was higher than that after application of the solution, and the absorption from 50% starch powder was enhanced by the substitution of starch with CMC-Na. The fractional absorption of FD4 after administration of the CMC-Na powder formulation was 30% and 40% higher than that after administration from the solution and the starch powder, respectively. The nasal absorption of insulin from the powder and the effect of CMC-Na were similar with those of FD4. The effective absorption of FD4 and insulin after application of powder with CMC-Na could be due to the increase in the nasal residence of FD4 and insulin. No damage in the nasal mucosa or dysfunction of the mucociliary clearance was observed after application of the drug powder and CMC-Na. The present findings indicate that nasal delivery of powder formulations with the addition of CMC-Na as an excipient is a promising approach for improving the nasal absorption of macromolecules.

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“…Recently, diseases like anthrax and influenza are treated by using the nasal vaccines prepared by using the recombinant Bacillus anthracis protective antigen (rPA) and chitosan respectively 28 . The common diseases like measles, pertussis, meningitis and influenza are caused by the pathogens that mainly enter into the body through the nasal mucosal surfaces and hence are good candidates for nasal vaccines.…”

Section:  Delivery Of Drugs To Brain Through Nasal Cavitymentioning

confidence: 99%

Untitled

2012

IJPSR

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The recent advancement of nasal drug delivery systems has increased enormously and is gaining significant importance. Intranasal therapy has been an accepted form of treatment in the Ayurvedic system of Indian Medicine. The non-invasive delivery of nasal drug delivery systems made to exploit for the development of successful treatment. The advantages, disadvantages, mechanism of action and application of nasal drug delivery system in local delivery, systematic delivery, nasal vaccines and CNS delivery are explained lucidly. The relevant aspects of biological, physicochemical and pharmaceutical factors of nasal cavity that must be considered during the process of discovery and development of new drugs for nasal delivery as well as in their incorporation into appropriate nasal pharmaceutical formulations are also discussed. Nasal route is more suitable for those drugs which cannot be administered orally due to gastric degradation or hepatic first pass metabolism of the drug. Intranasal drug delivery is found much promising route for administration of peptides and protein drugs. Much has been investigated and much more are to be investigated for the recent advancement of nasal drug delivery systems.

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Nasal Absorption of Propranolol in Rats

Cited by 68 publications

References 4 publications

Nasal Drug Absorption from Powder Formulations: Effect of Fluid Volume Changes on the Mucosal Surface

Nasal Drug Absorption from Powder Formulations: Effect of Fluid Volume Changes on the Mucosal Surface

Nasal Absorption of Macromolecules from Powder Formulations and Effects of Sodium Carboxymethyl Cellulose on Their Absorption

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