In Vitro Skin Permeation Enhancement of Sumatriptan by Microneedle Application.
Different dimensions of commercially available microneedle devices, namely, Admin- Patch(®) microneedle arrays (MN) (0.6, 0.9, 1.2 and 1.5 mm lengths) and Dermaroller(®) microneedle rollers (DR) (0.5 and 1mm lengths) were evaluated for their relative efficiency in enhancement of transdermal permeation of Sumatriptan (SMT). Solubility assessment of SMT was carried out using propylene glycol (PG), polyethylene glycol (PEG) in combination with saline (S) at different ratios and the order of solubility was found to be 70:30 > 80:20 > 90:10 %v/v in both PG:S and PEG:S. In vitro skin permeation studies were performed using PG:S (70:30 %v/v) as donor vehicle. A significant increase in cumulative amount of SMT permeated, steady state flux, permeability coefficient and diffusion coefficient values were observed after microneedle treatment, and the values were in the order of 1.5mm MN >1.2mm MN >0.9mm MN >1mm DR >0.6mm MN >0.5mm DR > passive permeation. Lag times were significantly shorter after longer microneedle application (0.24h for 1.5mm MN). Arrays were found to be superior to rollers with similar microneedle lengths in enhancing SMT permeation and may be attributed to higher density of microneedles and force of application onto skin. The in vitro flux values revealed that 2.5cm(2) area patch is sufficient for effective therapy after treatment of skin with 1.5mm MN. It may be inferred that microneedle application significantly enhances the transdermal penetration of SMT and that it may be feasible to deliver clinically relevant therapeutic levels of SMT using microneedle assisted transdermal delivery systems.
Department of Pharmaceutics, KVSR Siddhartha College of Pharmaceutical Sciences, Vijayawada-520010, AP, India. buchinalluri@yahoo.com.
Buchi N
BN
Nalluri
Sai Sri V
SS
Anusha
Sri R
SR
Bramhini
J
J
Amulya
Ashraf S K
AS
Sultana
Chandra U
CU
Teja
Diganta B
DB
Das
D000279:Administration, Cutaneous; D000818:Animals; D016503:Drug Delivery Systems; D009339:Needles; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D058825:Serotonin 5-HT1 Receptor Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D018170:Sumatriptan / Q000008:administration & dosage* / Q000493:pharmacokinetics; D013552:Swine
D058825:Serotonin 5-HT1 Receptor Agonists; D011092:Polyethylene Glycols; D018170:Sumatriptan