Aim: The main purpose for this study was to develop and evaluate amphiphilogels loaded
with meloxicam-submicron particles considering the benefits of the transdermal route of
administration of anti-inflammatory drugs (nonsteroidal). Materials and Methods: Glyceryl
monostearate (7%, 9% and 11% w/w) and sorbiton monostearate (span 60; 21%, 23%
and 25% w/w) amphiphilogels containing meloxicam-submicron particles equivalent to
0.5% w/w drug were formulated. Then these were evaluated through rheological,
in-vitro
permeation,
in-vitro release, pharmacokinetics, pharmacodynamics and skin irritation
studies. The rodents were chosen as subjects to conduct the pharmacokinetics study of
meloxicam via oral administration and transdermally as solutions and gels, respectively.
Results: It was observed that the Cmax value of drug obtained from meloxicam solution
and a marketable piroxicam gel formulation were radically lower than that obtained
from an amphiphilogel (FM4, containing 7% w/w glyceryl monostearate). It was also
observed that when applied transdermally, the bioavailability of meloxicam from FM4
was higher (
n = 3,
p< 0.001) than 2.5 times the bioavailability of meloxicam from a
solution which was orally administered. The anti-inflammatory property of FM4 was
comparatively much greater than the commercially available formulations in carrageenan-
induced edema in rat’s paw. Conclusion: It can be concluded that the amphiphilogels
loaded with meloxicam-submicron particles was found to be a safe and efficient drug
delivery system for enhanced transdermal delivery of meloxicam.