Cremophor RH40-PEG 400 microemulsions as transdermal drug delivery carrier for ketoprofen.
The aim of this study was to prepare novel microemulsion for transdermal drug delivery of ketoprofen (KP). The microemulsion composed of ketoprofen as model drug, isopropyl myristate (IPM) as oil phase, surfactant mixture consisting of polyoxyl 40 hydrogenated castor oil (Cremophor RH40) as surfactant and polyethylene glycol 400 (PEG400) as co-surfactant at the ratio 1:1, and water were prepared. The viscosity, droplet size, pH, conductivity of microemulsions, and skin permeation of KP through shed snake skin were evaluated. The particle size, pH, viscosity and conductivity of microemulsions were in the range of 114-210 nm, 6.3-6.8, 124-799 cPs and 1-45 µS/cm, respectively. The ratio of IPM, and surfactant mixture played the important role in the skin permeation of KP microemulsions. As the amount of surfactant mixture and IPM increased, the skin permeation of KP decreased. The formulation composed of 30% IPM, 45% surfactant mixture and 25% water showed the highest skin permeation flux. The incorporation of terpenes in the 2.5% KP microemulsions resulted in significant enhancement in skin permeation of KP. The rank order of enhancement ratio for skin permeation enhancement of terpenes was α-pinene > limonene > menthone. The results suggested that the novel microemulsion system containing IPM, water, Cremophor RH40:PEG400 and terpenes can be applied for using as a transdermal drug delivery carrier.
Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand. tanasait@ su.ac.th
Tanasait
T
Ngawhirunpat
Narumon
N
Worachun
Praneet
P
Opanasopit
Theerasak
T
Rojanarata
Suwannee
S
Panomsuk
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D017815:Elapidae; D004655:Emulsions; D005079:Excipients / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D007660:Ketoprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008863:Microspheres; D009226:Myristates / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013501:Surface-Active Agents / Q000737:chemistry; D013729:Terpenes / Q000737:chemistry; D014783:Viscosity; D014867:Water / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D009226:Myristates; D013501:Surface-Active Agents; D013729:Terpenes; D014867:Water; C008205:isopropyl myristate; C022131:cremophor; D011092:Polyethylene Glycols; D007660:Ketoprofen