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Evaluation of poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (PEO-PPO-PEO) gels as a release vehicle for percutaneous fentanyl.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Liaw, Jiahorng Lin, Yu-Hsin |
| Copyright Year | 2000 |
| Abstract | The primary objective of this study was to investigate the feasibility of PEO-PPO-PEO copolymer gel as a release vehicle for percutaneous administration of fentanyl in vitro and in vivo. A cellulose membrane and nude mouse skin with series concentrations of PEO-PPO-PEO block copolymers were used to examine the sustained-release pattern and permeation of fentanyl. The in vivo percutaneous absorption was examined using rabbits to evaluate the preliminary pharmacokinetics of fentanyl with 46% PEO-PPO-PEO copolymer formulation patches. The micelle formation ability of this block copolymer and the penetration ability of PEO-PPO-PEO copolymer over time were also studied by pyrene fluorescence probe methods and the dynamic light scattering test. At a concentration of 46% at 37 degrees C, PEO-PPO-PEO copolymers formed a gel and showed a pseudo-zero-order sustained-release profile. With increasing concentration of copolymer in the cellulose membrane transport, the apparent release flux of fentanyl (200 microgram/ml) decreased to 1. 09+/-0.19 microgram cm(-2) h(-1). Assessment of the effect of the copolymer on nude mouse skin also showed a decrease in the apparent permeability coefficient [(P(H(2)O))=2.24+/-0.47x10(-6) cm s(-1) vs. (P(46% block copolymer))=0.93+/-0.23x10(-7) cm s(-1)]. The preliminary pharmacokinetics of the fentanyl patch was shown to be in steady state within 24 h, and this was maintained for at least 72 h with an elimination half-life (t(1/2)) of 10.5+/-3.4 h. A fluorescence experiment showed polymeric micelle formation of PEO-PPO-PEO copolymers at 0.1% (w/w) within 50 nm micelle size and the PEO-PPO-PEO copolymers were able to penetrate nude mouse skin within 24 h. Thus, it appears that fentanyl preparations based on PEO-PPO-PEO copolymer gel might be practical for percutaneous delivery. |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/S0168-3659(00)00268-6 |
| PubMed reference number | 10925135 |
| Journal | Medline |
| Volume Number | 68 |
| Issue Number | 2 |
| Alternate Webpage(s) | http://libir.tmu.edu.tw/bitstream/987654321/41960/1/64++Evaluation+of+poly(ethylene+oxide)-poly(propylene+oxide)-poly(ethylene+oxide)+(PEO-PPO-PEO)+gels+as+a+release+vehicle+for+percutaneous+fentanyl..pdf |
| Alternate Webpage(s) | https://doi.org/10.1016/S0168-3659%2800%2900268-6 |
| Journal | Journal of controlled release : official journal of the Controlled Release Society |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
