4.6 Article

Effect of microneedles on transdermal permeation enhancement of amlodipine

期刊

DRUG DELIVERY AND TRANSLATIONAL RESEARCH
卷 7, 期 3, 页码 383-394

出版社

SPRINGER HEIDELBERG
DOI: 10.1007/s13346-017-0361-z

关键词

Amlodipine; Histological examination; Microneedle geometry; Scaling analyses; Transdermal permeation

资金

  1. Department of Science and Technology (DST), Ministry of Science and Technology, Govt. of India
  2. British Council, London, UK, under DSTUKIERI scheme [DST/INT/UK/P-60/2014]

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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 (R) 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, arrayswere applied thrice at different places within a 1.77-cm(2) 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 (C-t/C-s), thickness (h/L) and surface area of the skin (Sa/L-2). 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.

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