Formulation optimization of an indomethacin-containing photocrosslinked polyacrylic acid hydrogel as an anti-inflammatory patch.
Photocrosslinked polyacrylic acid hydrogel, made from polyacrylic acid (PAA) modified with 2-hydroxyethyl methacrylate (HEMA), is a promising candidate adhesive for dermatological patches. In this study, we investigated the further availability of hydrogel as an adhesive for dermatological patches using a hydrogel containing indomethacin (IDM) as a model anti-inflammatory patch. From an orthogonal experimental study, we clarified the relationships between formulation factors and characteristics of model formulation. Formulations with a lower degree of swelling were prepared by increasing the degree of HEMA modification and the addition of Tween 80. Apparent permeation rate was increased by addition of L-menthol and Tween 80. A tendency for higher HEMA modification to be accompanied by the prolongation of the lag time of IDM was observed. To obtain an applicable anti-inflammatory patch, we conducted a formulation optimization study using a novel optimization method, a response-surface method incorporating multivariate spline interpolation (RSM-S). Consequently, a highly functional anti-inflammatory patch in terms of its adhesive properties and bioavailability was successfully obtained. Since a wide range of functions can be fully controlled by manipulating the formulation factors, photocrosslinked polyacrylic acid hydrogel is an attractive candidate adhesive for dermatological patches.
Nishikawa
Masato
M
Department of Pharmaceutics, Hoshi University, Ebara 2-4-41, Shinagawa, Tokyo, 142-8501, Japan.
Onuki
Yoshinori
Y
Isowa
Koichi
K
Takayama
Kozo
K
D000180:Acrylic Resins / Q000008:administration & dosage* / Q000737:chemistry / Q000528:radiation effects; D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000528:radiation effects; D002626:Chemistry, Pharmaceutical; D003432:Cross-Linking Reagents / Q000008:administration & dosage* / Q000737:chemistry / Q000528:radiation effects; D020100:Hydrogels / Q000008:administration & dosage* / Q000737:chemistry / Q000528:radiation effects; D007213:Indomethacin / Q000008:administration & dosage* / Q000737:chemistry / Q000528:radiation effects; D008297:Male; D010777:Photochemistry; D051381:Rats; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D014466:Ultraviolet Rays
D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003432:Cross-Linking Reagents; D020100:Hydrogels; C006903:carbopol 940; D007213:Indomethacin
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