Effect of microneedles on transdermal permeation enhancement of amlodipine.
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-cm2skin 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 (R2> 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.
Department of Pharmaceutics, KVSR Siddhartha College of Pharmaceutical Sciences, Vijayawada, 520010 AP, India. buchinalluri@yahoo.com.
Buchi N
BN
Nalluri
Department of Pharmaceutics, KVSR Siddhartha College of Pharmaceutical Sciences, Vijayawada, 520010 AP, India.
Chandrateja
C
Uppuluri
Department of Pharmaceutics, KVSR Siddhartha College of Pharmaceutical Sciences, Vijayawada, 520010 AP, India.
Jyothirmayee
J
Devineni
Department of Chemical engineering, Loughborough University, Loughborough, LE11 3TU, UK.
Atul
A
Nayak
Department of Engineering and Informatics, University of Bradford, Bradford, BD7 1DP, UK.
Karthik J
KJ
Nair
Department of Engineering and Informatics, University of Bradford, Bradford, BD7 1DP, UK.
Benjamin R
BR
Whiteside
Department of Chemical engineering, Loughborough University, Loughborough, LE11 3TU, UK.
Diganta B
DB
Das
D017311:Amlodipine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001577:Benzophenones; D016503:Drug Delivery Systems; D066298:In Vitro Techniques; D007659:Ketones; D008845:Microinjections; D009339:Needles; D010539:Permeability; D011092:Polyethylene Glycols; D011108:Polymers; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013552:Swine
D000959:Antihypertensive Agents; D001577:Benzophenones; D007659:Ketones; D011108:Polymers; D017311:Amlodipine; C063834:polyetheretherketone; D011092:Polyethylene Glycols
Amlodipine; Histological examination; Microneedle geometry; Scaling analyses; Transdermal permeation