Nasal <i>in-situ</i> gels for delivery of rasagiline mesylate: improvement in bioavailability and brain localization

Ravi, Punna Rao; Aditya, N.P.; Patil, Sanjay B.; Cherian, Lata

doi:10.3109/10717544.2013.860501

Cited by 77 publications

(46 citation statements)

References 42 publications

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“…Further biological studies in Wistar rats indicated that the intranasal gels were not toxic and non-irritant to the rat nasal mucosa. The RM concentration in the rat brain tissue was significant, indicating an enhanced uptake of RM from the formulation when compared to the drug solution [97]. The administration of the drug intranasally overcomes the extensive first pass metabolism, a mechanism that is responsible for poor drug bioavailability of therapeutics administered orally.…”

Section: In Situ Gelmentioning

confidence: 99%

“…The administration of the drug intranasally overcomes the extensive first pass metabolism, a mechanism that is responsible for poor drug bioavailability of therapeutics administered orally. The extended residence time and intimate contact with nasal epithelium resulting from the mucoadhesive behavior of the gels improved the drug uptake from the nasal cavity [97].…”

Section: In Situ Gelmentioning

confidence: 99%

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Chitosan-Based Nanocarriers for Nose to Brain Delivery

Aderibigbe

Naki

2019

Applied Sciences

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In the treatment of brain diseases, most potent drugs that have been developed exhibit poor therapeutic outcomes resulting from the inability of a therapeutic amount of the drug to reach the brain. These drugs do not exhibit targeted drug delivery mechanisms, resulting in a high concentration of the drugs in vital organs leading to drug toxicity. Chitosan (CS) is a natural-based polymer. It has unique properties such as good biodegradability, biocompatibility, mucoadhesive properties, and it has been approved for biomedical applications. It has been used to develop nanocarriers for brain targeting via intranasal administration. Nanocarriers such as nanoparticles, in situ gels, nanoemulsions, and liposomes have been developed. In vitro and in vivo studies revealed that these nanocarriers exhibited enhanced drug uptake to the brain with reduced side effects resulting from the prolonged contact time of the nanocarriers with the nasal mucosa, the surface charge of the nanocarriers, the nano size of the nanocarriers, and their capability to stretch the tight junctions within the nasal mucosa. The aforementioned unique properties make chitosan a potential material for the development of nanocarriers for targeted drug delivery to the brain. This review will focus on chitosan-based carriers for brain targeting.

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Section: In Situ Gelmentioning

confidence: 99%

Section: In Situ Gelmentioning

confidence: 99%

Chitosan-Based Nanocarriers for Nose to Brain Delivery

Aderibigbe

Naki

2019

Applied Sciences

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“…Hematoxylin-Eosin (HE) stained paraffin sections (7 mm) were examined under light microscope. Untreated nasal mucosa was used as a control [33].…”

Section: Histological Studiesmentioning

confidence: 99%

Development of Nasal Mucoadhesive Microspheres of Granisetron: A Potential Drug

Pandey¹,

Shankar²,

Kumar

et al. 2020

Drug Res (Stuttg)

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Background Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. Objectives In this research mucoadhesive microspheres were developed in order to carry out the absorption of drug through nasal mucosa with the aim to improve therapeutic efficacy, avoid hepatic first pass metabolism and increase residence time. Material and Methods Mucoadhesive microspheres of Granisetron using chitosan as polymer were prepared by emulsification cross-linking method to increase the residence time on the mucosa. The surface of prepared microspheres was characterized by SEM (Scanning electron microscopy) and evaluated for particle size, encapsulation efficiency, production yield, swelling ability, in-vitro mucoadhesion, in-vitro drug release and stability study. Result Among all the formulations F6 with drug/polymer ratio of 1:3 displayed the best result. On drug release kinetic model study, all the formulations follow Zero order. Stability studies revealed that the microspheres kept at 25±2°C and 60±5% RH showed the maximum stability. Conclusion After all the evaluation parameters and result obtained it can be said that these results confirmed the suitability of Granisetron mucoadhesive chitosan microspheres for nasal delivery system.

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“…The temperature of the medium was maintained at 37±0.5 ° C. Five ml aliquots outgoing for suitable time periods and immediately making the replacement with fresh dissolution medium. The drug content in the withdrawn sample was determined spectrophotometrically by using a UV-Vis spectrophotometer at the selected λ max 285 [14].…”

Section: In Vitro Releasementioning

confidence: 99%

Optimization and in Vitro Evaluation of the Release of Class Ii Drug From Its Nanocubosomal Dispersion

Al-Sakini

Maraie

2019

Int J App Pharm

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Objective: This work involves investigation and evaluation of the factors that affect the preparation and the release of the model class II drug (erythromycin) to optimize the efficiency of its prepared nanocubosomal dispersion to give very fast initial burst effect within the first hour that can continue for further two hours. Methods:The work involved preparation of ten formulas of cubosomal dispersion by emulsifying different concentrations of glyceryl monooleate (GMO) (lipid content)/surfactant mixtures which were nano-sized and characterized morphologically by Transmission electronic microscopic (TEM), zeta potential, particle size, polydispersity index (pdI), pH, entrapment efficiency, conductivity test, dilution test and in vitro drug release. Results:The selected nanocubosomal formula (F1) showed pH (7.41), particle size (315.05 nm), pdI (0.194), zeta potential (-30.852), entrapment efficiency (91%) and gave a 70% drug release within the first hour of the in vitro test and continued until it gave 96.3% drug release with further 2 h.Conclusion: this work succeeded in preparing optimized cubosomal dispersion for erythromycin using different GMO/poloxamer 407 percent. The optimum formula gave an immediate release of the model drug (erythromycin) and it was ready to be incorporated in any suitable dosage form to give fast onset of action.

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Nasal in-situ gels for delivery of rasagiline mesylate: improvement in bioavailability and brain localization

Cited by 77 publications

References 42 publications

Chitosan-Based Nanocarriers for Nose to Brain Delivery

Chitosan-Based Nanocarriers for Nose to Brain Delivery

Development of Nasal Mucoadhesive Microspheres of Granisetron: A Potential Drug

Optimization and in Vitro Evaluation of the Release of Class Ii Drug From Its Nanocubosomal Dispersion

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