Nasal administration of metoclopramide from different dosage forms: in vitro, ex vivo, and in vivo evaluation

Taş, Çetin; Özkan, Cansel Köse; Savaşer, Ayhan; Özkan, Yalçın; Taşdemir, Umut; Altunay, Hikmet

doi:10.1080/10717540902764172

Cited by 29 publications

(10 citation statements)

References 33 publications

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“…sCT also has a relatively short residence time in the nose, which limits its absorption. The lack of a suitable mucoadhesive polymer in commercial formulations is another possible reason for low bioavailability of sCT via the nasal route (Tas et al, 2009). …”

Section: Resultsmentioning

confidence: 99%

Delivery of salmon calcitonin using a microneedle patch

Taş

Mansoor

Kalluri

et al. 2012

International Journal of Pharmaceutics

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Peptides and polypeptides have important pharmacological properties but only a limited number have been exploited as therapeutics because of problems related to their delivery. Most of these drugs require a parenteral delivery system which introduces the problems of pain, possible infection, and expertise required to carry out an injection. The aim of this study was to develop a transdermal patch containing microneedles (MNs) coated with a peptide drug, salmon calcitonin (sCT), as an alternative to traditional subcutaneous and nasal delivery routes. Quantitative analysis of sCT after coating and drying onto microneedles was performed with a validated HPLC method. In vivo studies were carried out on hairless rats and serum levels of sCT were determined by ELISA. The AUC value of MNs coated with a trehalose-containing formulation (250 ± 83 ng/mL.min) was not significantly different as compared to subcutaneous injections (403 ± 253 ng/mL.min), but approximately 13 times higher than nasal administration (18.4 ± 14.5 ng/mL.min). Tmax (7.5 ± 5 min) values for MN mediated administration were 50% shorter than subcutaneous injections (15 min), possibly due to rapid sCT dissolution and absorption by dermal capillaries. These results suggest that with further optimization of coating formulations, microneedles may enable administration of sCT and other peptides without the need for hypodermic injections.

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Section: Resultsmentioning

confidence: 99%

Delivery of salmon calcitonin using a microneedle patch

Taş

Mansoor

Kalluri

et al. 2012

International Journal of Pharmaceutics

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“…Tas y colaboradores, evaluaron la permeabilidad de la metoclopramida contenida en diferentes formulaciones (solución, gel y polvo) y encontraron que el polímero y la conformación del mismo, tienen un efecto sobre el porcentaje de liberación del fármaco, es decir un alto contenido de polímero, conformado en micelas va a dar Vargas-Fresneda lugar a un sistema muy intrincado que dificulta la difusión del fármaco, porque reduce el área de difusión molecular efectiva, lo cual permite afirmar que una formulación de partículas puede ser superior en desempeño a los sistemas de gel o hidrogel. (Tas et al, 2009) Fig. 5.…”

Section: Ensayo De Liberación In Vitrounclassified

Formulación de metoclopramida en partículas poliméricas mucoadhesivas para administración intranasal

2020

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Se prepararon y liofilizaron partículas (Ps) poliméricas mucoadhesivas a base de Gantrez®, cargadas con fármaco, mediante el método de desplazamiento de disolvente modificado, para administración intranasal de metoclopramida HCl (MCP). Las Ps obtenidas se caracterizaron midiendo tamaño (368,0 ± 79,6), índice de polidispersión (0,294 ± 0,014) y potencial Z (-47,3 ± 4,4) (Nanosizer, Malvern, ZS90). La carga de fármaco (%CF= 12,86 ± 0,7) y la eficiencia de encapsulamiento (%EE= 77,14 ± 3,9) se determinaron por un método espectrofotométrico UV, previamente validado. Se hizo un estudio de liberación in vitro, bajo condiciones sink, usando membranas de diálisis y un agitador orbital. Las partículas obtenidas poseen características tecnológicas adecuadas en cuanto a tamaño, contenido de fármaco y perfil de liberación, por lo que se consideran potencialmente adecuadas para la administración nasal de metoclopramida.

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“…The mucosa must be oriented with the mucosal side facing the donor chamber. The thickness of the tissue (usually 200 µm) should be measured and mentioned as it is directly linked to the diffusion rate (Tas et al, 2009;Shah et al, 2015;Acharya et al, 2013). The influence of the thickness was investigated in a study that compared the permeation of both hydrophilic (i.e.…”

Section: Ex-vivo Modelsmentioning

confidence: 99%

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

Salade

Wauthoz

Goole

et al. 2019

International Journal of Pharmaceutics

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Nasal delivery offers many benefits over other conventional routes of delivery (e.g. oral or intravenous administration). Benefits include, among others, a fast onset of action, non-invasiveness and direct access to the central nervous system. The nasal cavity is not only limited to local application (e.g. rhinosinusitis) but can also provide direct access to other sites in the body (e.g. the central nervous system or systemic circulation). However, both the anatomy and the physiology of the nose impose their own limitations, such as a small volume for delivery or rapid mucociliary clearance. To meet nasal-specific criteria, the formulator has to complete a plethora of tests, in vitro and ex vivo, to assess the efficacy and tolerance of a new drug-delivery system. Moreover, depending on the desired therapeutic effect, the delivery of the drug should target a specific pathway that could potentially be achieved through a modified release of this drug. Therefore, this review focuses on specific techniques that should be performed when a nasal formulation is developed. The review covers both the tests recommended by regulatory agencies (e.g. the Food and Drug Administration) and other complementary experiments frequently performed in the field.

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Nasal administration of metoclopramide from different dosage forms: in vitro, ex vivo, and in vivo evaluation

Cited by 29 publications

References 33 publications

Delivery of salmon calcitonin using a microneedle patch

Delivery of salmon calcitonin using a microneedle patch

Formulación de metoclopramida en partículas poliméricas mucoadhesivas para administración intranasal

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

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