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1.
AAPS PharmSciTech ; 18(5): 1495-1506, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28078629

RESUMEN

The present study was aimed to investigate the effect of salient microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation of rizatriptan (RIZ). Studies were carried out using two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 0.9, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PMs) of 0.6 mm length. In the case of the PMs, arrays were applied three times at different places within a 1.77-cm2 skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Histological studies revealed that PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 4.9- and 4.2-fold increases in the RIZ steady-state flux values were observed with 1.5 mm ADM and PM-3 applications when compared to the passive studies. A good correlation between different dimensionless parameters like the amount of RIZ permeated (C t /C s), thickness (h/L) and surface area (S a/L 2) of the skin was observed with scaling analyses. Numerical simulations provided further information regarding the distribution of RIZ in MN-treated skin after application of different MNs. Overall, the study suggests that MN application enhances the RIZ transdermal permeation and the geometrical parameters of MNs play an important role in the degree enhancement.


Asunto(s)
Agujas/normas , Triazoles , Triptaminas , Administración Cutánea , Sistemas de Liberación de Medicamentos/instrumentación , Análisis Numérico Asistido por Computador , Agonistas de Receptores de Serotonina/química , Agonistas de Receptores de Serotonina/farmacocinética , Piel/patología , Absorción Cutánea , Triazoles/química , Triazoles/farmacocinética , Triptaminas/química , Triptaminas/farmacocinética
2.
Drug Deliv Transl Res ; 7(3): 383-394, 2017 06.
Artículo en Inglés | MEDLINE | ID: mdl-28160258

RESUMEN

The present study aimed to investigate the effect of microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation enhancement of amlodipine (AMLO). Two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PM) of 0.6 mm length were employed. In the case of PMs, arrays were applied thrice at different places within a 1.77-cm2 skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Scaling analyses were done using dimensionless parameters like concentration of AMLO (Ct/Cs), thickness (h/L) and surface area of the skin (Sa/L2). Microinjection moulding technique was employed to fabricate PM. Histological studies revealed that the PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 6.84- and 6.11-fold increase in the cumulative amount (48 h) of AMLO permeated was observed with 1.5 mm ADM and PM-3 treatments respectively, when compared to passive permeation amounts. Good correlations (R 2 > 0.89) were observed between different dimensionless parameters with scaling analyses. The enhancement in AMLO permeation was found to be in the order of 1.5 mm ADM ≥ PM-3 > 1.2 mm ADM > 0.6 mm ADM ≥PM-1 > passive. The study suggests that MN application enhances the AMLO transdermal permeation and the geometrical parameters of MNs play an important role in the degree of such enhancement.


Asunto(s)
Amlodipino/administración & dosificación , Antihipertensivos/administración & dosificación , Sistemas de Liberación de Medicamentos , Amlodipino/farmacocinética , Animales , Antihipertensivos/farmacocinética , Benzofenonas , Técnicas In Vitro , Cetonas , Microinyecciones , Agujas , Permeabilidad , Polietilenglicoles , Polímeros , Piel/metabolismo , Absorción Cutánea , Porcinos
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