Nasal drug delivery: An in vitro characterization of transepithelial electrical properties and fluxes in the presence or absence of enhancers

Wheatley, Margaret A.; Dent, John G.; Wheeldon, Eric B.; Smith, Philip L.

doi:10.1016/0168-3659(88)90043-0

Cited by 61 publications

(17 citation statements)

References 29 publications

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“…In this study, the experiment was carried out within 3 to 3.5 h since the obtaining of tissues, so the viability of the mucosa was maintained. 7,11) HPLC Method A HPLC system consisting of a pump (SPD-10A, SHI-MADZU, Japan) and ultroviolet detector (LC-10AT, SHIMADZU, Japan) was employed, the mobile phase consisted of methanol : 0.02 M KH 2 PO 4 : triethylamine (40 : 60 : 0.1, v/v/v) running at a flow rate of 1.0 ml/min. The detection wave length was 230 nm.…”

Section: Methodsmentioning

confidence: 99%

“…The excised tissue of animals such as sheep, [7][8][9] pig, 10,11) rabbit, 4,12,13) and ox 14,15) had been employed by researchers to study the drug delivery through nasal mucosa. Among these animals, the morphology of the ovine mucosa is more comparable to that of humans because of the presence of ciliated and non ciliated cells, basal cells, goblet cells and serous glands.…”

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confidence: 99%

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The Permeation of Nalmefene Hydrochloride across Different Regions of Ovine Nasal Mucosa

Yong-liang

Nie

et al. 2006

Chem. Pharm. Bull.

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Nasal drug delivery has been generating widespread interest in the drug delivery field because it could not only be used in local treatment but also in systemic administration. Various properties of nasal drug delivery made it an alternative route for intravenous and oral administration, such as bypassing of enzymatic or acidic degradation and exempting the first-pass hepatic metabolism; the relatively large epithelial surface, porous endothelial membranes and highly vascularized epithelium also maintained the rapid absorption of drugs.Various factors that might affect the permeability of drugs through the nasal mucosa could be broadly classified into three categories as follow: biological factors, formulation aspects and device-related factors. 1,2) The nasal structure feature was one of the main biological factors. The nasal cavity could be anatomically segregated into five different regions: nasal vestibule, atrium, respiratory area, olfactory region and nasopharnyx.2) The structure features of different regions were quite different which resulted in different blood supply, nasal secretion and mucociliary clearance among them, 3) and thus may influence the permeability of drug and presystemic degradation. Moreover, different devices and dosage forms may result in differences of the deposition place and residence time of drugs in the nasal cavity. Therefore, the research on the permeability of drug through mucosas of different regions of nasal cavity in vitro may help us to find out the main absorption region of drugs and understand the mechanism, rate and extent of drug absorption across the nasal mucosa. Furthermore, it may also be helpful for choosing dosage forms to deposit drugs on the main absorption region and prolong the residence time.However, there were few studies about the permeation of drugs through mucosas of different regions of the nasal cavity. In present study, the Valia-Chien chamber technique 4) and a hydrophilic model drug nalmefene hydrochloride [17-N-cyclopropylmethyl-3,14-b-dihydroxy-4,5-a-epoxy-6-methylene morphinan hydrochloride] 5) which was chosen for its possibility to be developed as a product for emergency medicine, 6) was used to study the permeability of the five different regions. The permeability coefficient and accumulative drug permeation was investigated. The permeation of NH through different pieces obtained from the same middle turbinate mucosa and the same septum mucosa was also investigated to evaluate the uniformity of such mucosa.The excised tissue of animals such as sheep, 7-9) pig, 10,11) rabbit, 4,12,13) and ox 14,15) had been employed by researchers to study the drug delivery through nasal mucosa. Among these animals, the morphology of the ovine mucosa is more comparable to that of humans because of the presence of ciliated and non ciliated cells, basal cells, goblet cells and serous glands. 16) In the present study, ovine nasal mucosa was employed. During the experimental process, it was easier to handle the tissue and keep the mucosa intact and unstrained. Ther...

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Section: Methodsmentioning

confidence: 99%

mentioning

confidence: 99%

The Permeation of Nalmefene Hydrochloride across Different Regions of Ovine Nasal Mucosa

Yong-liang

Nie

et al. 2006

Chem. Pharm. Bull.

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“…It is important to examine the pathway/mechanisms involved prior to addressing the possibilities to improve transnasal uptake by the brain [9,10]. The olfactory region is known to be the portal for a drug substance to enter from nose-to-brain following nasal absorption.…”

Section: Mechanism Of Nose To Brain Drug Transportmentioning

confidence: 99%

A Recent Review on Nasal Microemulsion for Treatment of CNS Disorder

Jaiswal

Darekar

Saudagar³

2017

Int J Curr Pharm Sci

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Nasal route is found to be valuable for targeting drugs to CNS via a different mechanism. The advantages, disadvantages, various aspects of nasal anatomy and physiology, mechanism of drug transport from nose brain, drug selection criteria to cross BBB/Blood-CSF barrier are discussed briefly. Nowadays many drugs have better systemic bioavailability through nasal route as compared to oral administration. In addition, intranasal drug delivery enables dose reduction, rapid attainment of therapeutic blood levels, quicker onset of pharmacological activity, and fewer side effects. There are various approaches in delivering a therapeutic substance to the target site. One such approach is using microemulsion as a carrier for the drug. The main purpose of this study is the use of microemulsion technology in drug targeting to the brain along with mechanism of the nose to brain transport, formulation and formation of the microemulsion and its characterization.

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“…94 Some hurdles need to be solved involving in vitro cell culture models these are: small amount of obtainable cells and differentiation issues with epithelial cells although advancement in cell culture techniques appear are promising.…”

Section: Fig 3: Various Models For Intra Nasal Drug Transport and Abmentioning

confidence: 99%

Untitled

2017

IJPSR

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Intra nasal drug delivery system (INDDS) has emerged as a noninvasive alternative for delivering peptides, proteins and other therapeutic agents, specifically to CNS (Central nervous system). This route is well suitable for systemic delivery because of high vasculature, permeability, elimination of hepatic first pass metabolism and low enzymatic environment of the nasal cavity. This route of delivery is especially suited to treat CNS disorders like -neurodegenerative diseases, mood disorders, cognitive dysfunctioning etc., due to drugs ability to directly reach the brain by passing blood brain barrier (BBB). It is also a well suited delivery route for the biotechnological products like DNA plasmids, hormone, proteins, peptides, DNA vaccines to give enhanced bioavailability. A wide variety of therapeutic compounds may be administered intra-nasally for topical, systemic and CNS disorders. In this review, we have focussed on the nasal passage anatomical pathway leading to CNS drug delivery, different factors affecting nasal absorption, bioavailability barriers, vaccines and other therapeutic, biologically active molecules delivered via intra nasal route and strategies to improve nasal absorption. We have also outlined various in vitro and in vivo cellular models for nasal drug absorption and permeability studies.

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Nasal drug delivery: An in vitro characterization of transepithelial electrical properties and fluxes in the presence or absence of enhancers

Cited by 61 publications

References 29 publications

The Permeation of Nalmefene Hydrochloride across Different Regions of Ovine Nasal Mucosa

The Permeation of Nalmefene Hydrochloride across Different Regions of Ovine Nasal Mucosa

A Recent Review on Nasal Microemulsion for Treatment of CNS Disorder

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