A novel solid-in-oil nanosuspension for transdermal delivery of diclofenac sodium.
OBJECTIVE
We formulated a solid-in-oil nanosuspension (SONS) as a novel transdermal delivery carrier for diclofenac sodium (DFNa). The basic transdermal characteristics of the SONS were evaluated using a Yucatan micropig (YMP) skin model.


METHODS
DFNa-sucrose erucate (i.e. surfactant) complexes were prepared via the formation of a water-in-oil emulsion. The complexes were suspended in isopropyl myristate (IPM) to form a SONS. The basic transdermal characteristics of the SONS were examined using full-thickness YMP dorsal skin in a Franz-type diffusion cell. DFNa powder suspended in IPM without complex formation was used as a control. The effect of the weight ratio of surfactant to DFNa on DFNa penetration of the skin was evaluated.


RESULTS
DFNa was successfully dispersed into IPM as a nanosized suspension via complex formation with sucrose erucate. The resultant SONS increased the permeability flux of DFNa across the YMP skin by up to 3.8-fold compared with the control. The size of the SONS depended on the weight ratio of the surfactant to DFNa. The optimal weight ratio for the highest DFNa permeation was 8.8, at which point the mean diameter of the SONS was 14.4 nm.


CONCLUSIONS
The SONS formulation can enhance the percutaneous absorption of DFNa.
Piao
Hongyu
H
Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, Fukuoka, 819-0395, Japan.
Kamiya
Noriho
N
Hirata
Akihiko
A
Fujii
Takeru
T
Goto
Masahiro
M
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D004008:Diclofenac / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers; D004339:Drug Compounding; D009226:Myristates / Q000737:chemistry*; D049329:Nanostructures; D010316:Particle Size; D010539:Permeability; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013395:Sucrose / Q000031:analogs & derivatives / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D013552:Swine; D013556:Swine, Miniature; D014783:Viscosity; D014867:Water / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D009226:Myristates; D013501:Surface-Active Agents; D014867:Water; C008205:isopropyl myristate; D004008:Diclofenac; D013395:Sucrose