Improved solubility and in vitro dissolution of Ibuprofen from poloxamer gel using eutectic mixture with menthol.
To improve the solubility and in vitro dissolution of poorly water-soluble ibuprofen with poloxamer and menthol, the effects of menthol and poloxamer 188 on the aqueous solubility of ibuprofen were investigated. The dissolution study of ibuprofen delivered by poloxamer gels composed of poloxamer 188 and menthol were performed. In the absence of poloxamer, the solubility of ibuprofen increased until the ratio of menthol to ibuprofen increased from 0:10 to 4:6, followed by an abrupt decrease in solubility above the ratio of 4:6, indicating that 4 parts of ibuprofen formed eutectic mixture with 6 parts of menthol. In the presence of poloxamer 188, the solutions with the same ratio of menthol to ibuprofen showed abrupt increase in the solubility of ibuprofen. Furthermore, the solution with ratio of 4:6 showed more than 2.5- and 6-fold increase in the solubility of ibuprofen compared with that without poloxamer and that without menthol, respectively. The poloxamer gel with menthol/ibuprofen ratio of 1:9 and higher than 15% poloxamer 188 showed the maximum solubility of ibuprofen, 1.2 mg/ml. Menthol improved the dissolution rates of ibuprofen from poloxamer gels. Dissolution mechanism showed that the dissolution rate of ibuprofen from the poloxamer gels without menthol was independent of the time, but the drug might be dissolved from the poloxamer gels with menthol by Fickian diffusion. Thus, the poloxamer gels developed using eutectic mixture with menthol, which gave the improved solubility and dissolution of drug, are potential candidates for ibuprofen-loaded transdermal and rectal delivery system.
Yong
Chul Soon
CS
College of Pharmacy, Yeungnam University, Gyongsan, South Korea.
Jung
Se Hyun
SH
Rhee
Jong-Dal
JD
Choi
Han-Gon
HG
Lee
Beom-Jin
BJ
Kim
Dong-Chool
DC
Choi
Young Wook
YW
Kim
Chong-Kook
CK
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D005782:Gels; D007052:Ibuprofen / Q000737:chemistry*; D008610:Menthol / Q000737:chemistry*; D020442:Poloxamer / Q000737:chemistry*; D012995:Solubility
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005782:Gels; D020442:Poloxamer; D008610:Menthol; D007052:Ibuprofen