Intranasal Drug Delivery: How, Why and What for?

Pires, A. S.; Fortuna, Ana; Alves, Gilberto

doi:10.18433/j3nc79

Cited by 471 publications

(399 citation statements)

References 160 publications

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“…The mechanism of gelation involves the formation of double-helical junction zones followed by aggregation of the double-helical segments to form a 3-D network by complexation with cations and hydrogen bonding with water. Because human nasal mucosa is covered with approximately 0.1 ml mucus, which consists of sodium, potassium and calcium ions, a solution-gel phase transition can be expected (Bajaj et al, 2007;Pires et al, 2009;Dhuria et al, 2010;Morris et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Development ofin situgel for nasal delivery: design, optimization,in vitroandin vivoevaluation

2013

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Context: The mucoadhesive gel formulations are helpful to prolong the residence time at the nasal absorption site and thereby facilitate the uptake of drug. Sumatriptan succinate has oral bioavailability of 15% and undergoes hepatic metabolism, hence it is suitable for nasal administration.Objective: The objective of the investigation was to develop a mucoadhesive in situ gel to improve the bioavailability of the sumatriptan succinate. Materials and methods: Deacetylated gellan gum was used as gelling agent. In situ gel was formulated by ion activation mechanism in simulated nasal fluid. A 3 2 factorial design was found suitable to optimize batch. In vivo study was carried out in Spraugue-Dawley rats, and drug was estimated in plasma by UPLC-MS. Result: The optimized batch showed drug release of 98.57% within 5 h followed by Peppas model of drug release. Ex vivo studies on sheep nasal mucosa showed 93.33% within 5 h. In histopathological study, optimized batch was found to be safe and stable in accelerated stability study for three months. Optimized formulation, F7 has shown absolute bioavailability, which was found to be 164.70%. Drug targeting index for brain tissues was found to be 1.866. Discussion: Concentration of the gelling polymer was compromised for satisfactory gel strength and an acceptable viscosity. The release depended on viscosity of formulation. Drug targeting index indicates sumatriptan can reach to brain via olfactory pathway. Conclusion: In situ gel proved to be suitable for administration of sumatriptan succinate through nasal route. The ease of administration coupled with less frequent administration enhances patient compliance.

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Section: Introductionmentioning

confidence: 99%

Development ofin situgel for nasal delivery: design, optimization,in vitroandin vivoevaluation

2013

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“…Studies in animals concluded that lectins have minimal acute irritancy and can be thus be used for further in vivo studies [ 19 ]. However, many lectins are toxic or immunogenic especially those obtained from Ricinus communis, Phaseolus vulgaris and Lycopersicon esculentum and Canavalia ensiformis [5] .There is a probability that lectins promote the production of antibodies which could lead to the blockage of lectin-based delivery vehicles. These antibodies may also expose patients to the risk of systemic anaphylaxis on successive exposure.…”

Section: Lectinsmentioning

confidence: 99%

“…Furthermore, drugs that have low oral bioavailability have been shown to be successfully delivered systemically using the nasal route; studies have suggested that the nasal route is a great alternative to parenteral route for delivery of protein and peptide drugs [4]. Also due to direct delivery of drugs to the systemic circulation, the onset of pharmacological action is rapid [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Novel Mucoadhesive Polymers for Nasal Drug Delivery

Anand¹,

Feridooni²,

Agu³

2012

Recent Advances in Novel Drug Carrier Systems

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“…The nasal cavity can provide larger surface area for rapid systemic absorption due to its highly vascularised surface 8 . This non-invasive route not only provides rapid onset of action, but often increased bioavailability in low doses as it bypasses the first pass metabolism 9 .…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

Lungare

Bowen

Badhan

2016

Journal of Pharmaceutical Sciences

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The aim of this study was to develop and characterise an intranasal delivery system for amantadine (AMT). Optimal formulations (F) consisted of a thermosensitive polymer Pluronic ® 127 (P127) and either carboxy methyl cellulose (CMC) or chitosan (CS) which demonstrated gel-transition at nasal cavity temperatures (34 °C ± 1 °C). Rheologically, the loss tangent (Tan δ) confirmed a three-stage gelation phenomena at 34 °C ± 1 °C and nonNewtonian behaviour. Storage of FCMC and FCS at 4 °C for 8 weeks resulted in repeatable release profiles at 34 °C when sampled, with a Fickian mechanism earlier on but moving towards anomalous transport by week 8. Polymers (P127, CMC and CS) demonstrated no significant cellular toxicity to human nasal epithelial cells up to 4 mg/mL and up to 1 mM for AMT (IC50: 4.5 mM ± 0.05 mM). FCMC and FCS demonstrated slower release across an in-vitro human nasal airway model (43-44 % vs 79 % ± 4.58 % for AMT). Using a human nasal cast model, deposition into the olfactory regions (potential nose-to-brain) was demonstrated upon nozzle insertion (5 mm) whereas tilting of the head forward (15°) resulted in greater deposition in the bulk of the nasal cavity. KEYWORDSParkinson's disease; rheology; nasal; RPMI 2650; nose to brain; thermoresponsive; 3 INTRODUCTION Parkinson's disease (PD) is an ageing associated progressive neurological disorder and affects 1.5 % of the population over 65-years of age 1 , with age-adjusted prevalence rates thought to be around 150 per 100,000 with a suggested mean onset in the 70's 1 . Ageing is the largest single risk factor for the development of PD and the pathogenesis of PD is composed of a range of events leading towards neuronal apoptosis, primarily of degradation of dopamine neurones in the sustantia nigra. The mainstay of clinical drug therapy focuses on increases the levels of dopamine (DA) in the brain, with oral dosing of levodopa being the most commonly used to pharmacological intervention treatment to reverse the symptoms of PD. It is also common to use adjunct therapies in conjunction with levodopa, such as the weak NMDA-type receptor antagonist amantadine, which can aid in blocking dopamine reuptake.

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Intranasal Drug Delivery: How, Why and What for?

Cited by 471 publications

References 160 publications

Development ofin situgel for nasal delivery: design, optimization,in vitroandin vivoevaluation

Development ofin situgel for nasal delivery: design, optimization,in vitroandin vivoevaluation

Novel Mucoadhesive Polymers for Nasal Drug Delivery

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

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