Effect of enhancers on the in vitro percutaneous absorption of piroxicam from compounding formulations

Abstract

The piroxicam permeation through porcine ear skin, in a Franz Cell was evaluated, comparing with a commercial product. The permeate was analyzed by high performance liquid chromatography (HPLC) using a 5 mm C 18 column with mobile phase methanol:phosphate buffer (60:40), at 354 nm and the run time of 10 min. This method was validated and the limit of quantification was 0.138 μg/mL, with linearity over 0.02-5 μg/mL, without endogenous skin interference. The order of piroxicam permeation after 24 h was: LE > L> Feldene® > N > LP > NP > NE. The L based formulations showed greater piroxicam permeation compared with N based formulations, particularly up to 10 h of experiment. The ethanol enhancer provided the highest piroxicam permeation. The commercial product shows a different behavior, providing piroxicam permeation almost after 10 h. These results show the development of effective, simple and economic percutaneous formulations of piroxicam allowing the choice of formulations for higher or lower piroxicam permeation.

Transdermal behaviour of the N-alkylamide spilanthol (affinin) from Spilanthes acmella (Compositae) extracts

“…To check the influence of operational manipulations, the commercial extract was included as control sample. As the organic solvents used may have permeation modifying properties (Bortolon et al, 2008;Vavrova et al, 2005;Williams and Barry, 2004), a 100% aqueous percutaneous delivery in a solvent independent way needs to be examined. As spilanthol is a lipophilic compound (log P ow = 3.4), its aqueous solubility is considered to be insufficient to perform this experiment with a purely aqueous dose solution.…”

Development and Validation of a Liquid Chromatography-Mass Spectrometry Assay for Determination of Cromolyn Sodium in Skin Permeation Studies

“…These conditions worked well with aqueous samples, but significant ion suppression using our instrumentation was noted with samples in PBS or methanolic skin extracts. Furthermore, these conditions promoted the intermittent formation of sodium adducts, as noted by Lin et al [ 10 ]. Previously published LC-MS assays for CS quantification relied on ionization by positive ESI [ 11 – 13 ], but the structure of this drug does not lend to easy ionization in positive mode.…”

“…In vitro permeation studies are uniquely subjected to such requirement as direct analysis of drug diffusion through skin and do not implement extensive drug extraction techniques usually used for analysis of compounds in urine or serum [ 8 ]. As a result, analytical methods employed for such studies need to be able to selectively quantify target drug from skin components, like epidermal ceramides, that leach into permeation samples [ 9 , 10 ].…”

Skin Delivery of Glucosamine and Chondroitin Sulphates—A Perspective on the Conservative Treatment for Osteoarthritis of the Knee

“…The topical route prevents the first-pass effect from occurring [7]. Furthermore, a number of undesirable side effects may be noticed when orally administering drugs, such as nausea, dyspepsia, diarrhea, constipation, ulcer, and mucosal bleeding-which does not occur when applying the topical route [8] [9]. It is important to add that the topical route holds advantage over both the intravenous and intramuscular routes as it is a painless and noninvasive route of administration, enhancing patients' adherence to recommended therapy [10] [11] [12].…”