Chitosan in nasal delivery systems for therapeutic drugs

Casettari, Luca; Illum, Lisbeth

doi:10.1016/j.jconrel.2014.05.003

Cited by 366 publications

(229 citation statements)

References 108 publications

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“…In particular, this may provide a much higher residence time in the nasal cavity, pivotal to allow an enhancement of drug availability. 66 For the in vitro release studies, a simulated nasal electrolyte solution containing BSA was preferred to surfactant solutions 48 or mixtures with organic solvents miscible with water 67 , as a physiological dissolution medium. Generally, drug inclusion in nanoparticles is a strategy to prolong the release.…”

mentioning

confidence: 99%

The nasal delivery of nanoencapsulated statins – an approach for brain delivery

Clementino¹,

Batger²,

Garrastazu³

et al. 2016

IJN

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mentioning

confidence: 99%

The nasal delivery of nanoencapsulated statins – an approach for brain delivery

Clementino¹,

Batger²,

Garrastazu³

et al. 2016

IJN

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“…перспективностью как потенциальных моделей для совершенствования материалов и методов борьбы с опасными микроорганизмами. Альгинат натрия и хитозан с успехом используются для доставки лекарств через нос [7], слизистые мембраны глаз [9], а также ротовую полость [8].…”

Section: материалы и методы исследованияunclassified

Immobilization of Antimicrobial Bacterial Substances Onto Polymeric Matrices: Their Property Evaluation

Pokhilenko¹,

Dunaitsev²,

Perelygin³

et al. 2016

СПНО (MPSE)

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Отработаны условия получения альгинатных и хитозановых матриксов c антимикробными веществами (АМВ), выделенных из Bacillus lentus, Geobacillus thermoglucosidasius и Paenibacillus polymyxa. Исследованы зависимости формы матриксов от состава используемых ингредиентов и времени нахождения в жидкости. Показано влияние способа высушивания на целостность матрикса гранул и динамику потери их активности в отношении тест-штаммов. Установлено, что лиофилизация альгинатных гранул вызывала частичную деструкцию матриксов, сопровождаемую снижением антимикробного потенциала дозированной формы, что практически не наблюдалось после конвективного высушивания тех же образцов. При нахождении в воде в условиях комнатной температуры в течение месяца все варианты гранул не растворялись, но постепенно теряли активность. Более стабильные результаты по сохранению антимикробной активности показали варианты альгинатных гранул с хитозановым покрытием. Образцы чисто хитозановых микогранул были на порядок мельче альгинатных и хорошо сохраняли активность. Полученные данные по иммобилизации лабораторных образцов АМВ природного происхождения в альгинатные и хитозановые матриксы могут быть использованы при получении систем контролируемой доставки перспективных лекарственных средств. Ключевые слова: антимикробные вещества, бациллы, иммобилизация, альгинат, хитозан, гранулы. IMMOBILIZATION OF ANTIMICROBIAL BACTERIAL SUBSTANCES ONTO Conditions for producing alginate and chitosan matrices carrying antimicrobial substances (AMS) isolated fromBacillus lentus, Geobacillus thermoglucosidasius, and Paenibacillus polymyxa have been worked out. The dependence of the matrix shape on ingredients used and the residence time in the liquid has been studied. Influence of the drying procedure on the granule matrix intactness as well as on the dynamics of loosing activity toward test strains by them has been shown. Lyophilization of alginate granules was found to partially destruct the matrices along with decreasing in the antimicrobial potential of the dosage form while those were practically avoided during convective drying of the same specimens. While being kept in water at room temperature for a month, granules of all versions didn't dissolve but lost gradually their activity. More consistent results for chitosan-covered alginate granules have been obtained. Specimens of chitosan microgranules were smaller by order of magnitude compared to alginate ones, retaining successfully their activities. The laboratory data on immobilizing AMS specimens of the natural origin onto alginate and chitosan matrices can be used for designing systems for target delivery of promising therapeutics.

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“…17 Application of chitosan microspheres for nasal delivery for drug molecules such as morphine, 19 zolmitriptan, 20 verapamil, 21 metoclopramide, 22 insulin, [23][24][25] goserelin 26 and human growth hormone 13 using different production methods i.e., spray drying 20 and emulsification techniques 24 have already been studied. They showed that chitosan in solution enables the transport of even macro drug molecules across the nasal membrane.…”

Section: Introductionmentioning

confidence: 99%

“…[10][11][12][13][14][15][16] Of special interest has been the use of chitosan as an absorption enhancer and a bioadhesive materials acting by opening the tight junctions of nasal mucosa to overcome the high degree effect of the mucociliary clearance by increasing the residence time of the formulation in the nasal cavity. 17 Chitosan, a natural linear polycationic, biocompatible, biodegradable and mucoadhesive polymer derives from alkaline deacetylation of chitin of several Mw (10kDa-2000kDa) with varying degrees of deacetylation (40-98%). The inherent characteristics of the chitosan determines physicochemical properties of the polymer which are key for its effectiveness as an absorption enhancer as well as being a mucoadhesive material.…”

mentioning

confidence: 99%

Mucoadhesive Microspheres of Chitosan and Polyvinyl Alcohol as A Carrier for Intranasal Delivery of Insulin: In Vitro and In Vivo Studies

Darbandi¹

2017

MOJBB

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The aim of this study was to investigate the capabilities of chitosan microspheres as drug carrier system in co-formulation with polyvinyl alcohol (PVA), to improve the systemic absorption of intranasal insulin delivery.Insulin loaded microspheres was developed from varying ratio of chitosan solutions along with polyvinyl alcohol (PVA) as additive polymer using spray drying method. Different formulations were developed and morphological studies of the optimized formulas showed that the size range of spherical shaped particulate matters existed from 200 nm to 2 μm. It was clearly observed that physicochemical properties of the microspheres were extensively affected by changing the concentration ratio of the two polymeric materials. In vitro studies of insulin release pattern was performed in various time intervals up to 24 h. It was evident that microspheres made up of chitosan showed initial burst release but slower release as the experiment continued. Microspheres made up of combination of the aforementioned two polymers had instant, sharp and burst drug release. Surprisingly there was no absorption after intranasal delivery of chitosan-PVA microspheres in groups of rats comparing to formulated chitosan microspheres having profound absorption due to their smaller particle size, slower drug release rate and better mucoadhesive properties. Therefore, significant reduction in the plasma blood glucose level for chitosan based optimized formulation was seen right after 4.5 hours compared with control group. The aim of the present study was to fabricate an appropriate application of polymeric microspheres for intranasal delivery of insulin using a novel optimized formulation based on industrial level spray drying technique and to realize the possible barriers in scale up process of its large scale production, considering the effectiveness of polyvinyl alcohol (PVA) and chitosan to increase mucoadhesivness, gelling ability and ultimately effective release behavior pattern of insulin. According to this study, the combination of the polymers used and the mean particle size of formulated microspheres were found to be key factors in insulin drug release resulting for further enhancement of insulin absorption via intranasal route of delivery. Furthermore, avoidance of hepatic first pass metabolism makes it a preferred route for the delivery of small drug molecules but not basically the macromolecules as the permeability and degradability are rate-limiting steps in their systemic absorptions. KeywordsFeasibility of intranasal route for delivery of peptides and proteins has already been evaluated as mentioned before, due to the perceived less demanding barriers to peptides and proteins transport across the nasal epithelium as compared to the oral mucosa and nasal cavity comprising lower enzymatic content, higher leakiness of the membrane and high vascularity and no hepatic first pass metabolism But still there are few nasal peptide based products which have appeared on the market e.g. calcitonin (Miacalcin These prod...

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Chitosan in nasal delivery systems for therapeutic drugs

Cited by 366 publications

References 108 publications

The nasal delivery of nanoencapsulated statins – an approach for brain delivery

The nasal delivery of nanoencapsulated statins – an approach for brain delivery

Immobilization of Antimicrobial Bacterial Substances Onto Polymeric Matrices: Their Property Evaluation

Mucoadhesive Microspheres of Chitosan and Polyvinyl Alcohol as A Carrier for Intranasal Delivery of Insulin: In Vitro and In Vivo Studies

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Chitosan in nasal delivery systems for therapeutic drugs

Cited by 366 publications

References 108 publications

The nasal delivery of nanoencapsulated statins &ndash; an approach for brain delivery

The nasal delivery of nanoencapsulated statins &ndash; an approach for brain delivery

Immobilization of Antimicrobial Bacterial Substances Onto Polymeric Matrices: Their Property Evaluation

Mucoadhesive Microspheres of Chitosan and Polyvinyl Alcohol as A Carrier for Intranasal Delivery of Insulin: In Vitro and In Vivo Studies

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The nasal delivery of nanoencapsulated statins – an approach for brain delivery

The nasal delivery of nanoencapsulated statins – an approach for brain delivery