Novel microemulsion enhancer formulation for simultaneous transdermal delivery of hydrophilic and hydrophobic drugs
Lee, PJ; Langer, R; Shastri, VP
| HERO ID | 3539879 |
|---|---|
| In Press | No |
| Year | 2003 |
| Title | Novel microemulsion enhancer formulation for simultaneous transdermal delivery of hydrophilic and hydrophobic drugs |
| Authors | Lee, PJ; Langer, R; Shastri, VP |
| Journal | Pharmaceutical Research |
| Volume | 20 |
| Issue | 2 |
| Page Numbers | 264-269 |
| Abstract | <strong>PURPOSE: </strong>Microemulsion (ME) systems allow for the microscopic co-incorporation of aqueous and organic phase liquids. In this study, the phase diagrams of four novel ME systems were characterized.<br /><br /><strong>METHODS: </strong>Water and IPM composed the aqueous and organic phases respectively, whereas Tween 80 served as a nonionic surfactant. Transdermal enhancers such as n-methyl pyrrolidone (NMP) and oleyl alcohol were incorporated into all systems without disruption of the stable emulsion.<br /><br /><strong>RESULTS: </strong>A comparison of a W/O ME with an O/W ME of the same system for lidocaine delivery indicated that the O/W ME provides significantly greater flux (p < 0.025). The water phase was found to be a crucial component for flux of hydrophobic drugs (lidocaine free base, estradiol) as well as hydrophilic drugs (lidocaine HCl, diltiazem HCl). Furthermore, the simultaneous delivery of both a hydrophilic drug and a hydrophobic drug from the ME system is indistinguishable from either drug alone. Enhancement of drug permeability from the O/W ME system was 17-fold for lidocaine free base, 30-fold for lidocaine HCl, 58-fold for estradiol, and 520-fold for diltiazem HCl.<br /><br /><strong>CONCLUSIONS: </strong>The novel microemulsion systems in this study potentially offers many beneficial characteristics for transdermal drug delivery. |
| Doi | 10.1023/A:1022283423116 |
| Pmid | 12636166 |
| Wosid | WOS:000180830200017 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |
| Keyword | microemulsion; transdermal drug delivery; chemical enhancers; n-methyl pyrrolidone |