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This article evaluated the influence of vehicle compositions on topical drug availability. In vitro drug release and in vivo experiments were performed in case of the hydrophilic ketamine hydrochloride and the lipophilic piroxicam. Ketamine hydrochloride is a NMDA receptor antagonist that has been useful for anesthesia and analgesia. The study of transdermal ketamine delivery is a novelty, because nobody has investigated the hypnotic effects of ketamine after this administration route. In vitro measurements gave a good basis for screening among the developed products. The physiological changes after ketamine administration showed, that there were significant differences among the parameters tested (breathing rate, duration of sleep) from the developed products (hydrogel, lyotropic liquid crystal and o/w cream) compared to the reference product (Carbopol gel). The in vivo feedback for piroxicam was the measurement of the anti-inflammatory activity by edema inhibition percentage. Significant differences were measured in case of the developed systems compared to the reference.

The aim of the present study was to determine the rate of transport and long-term effect of a drug applied to the oral mucosa in different ointments. Three ointments with bioadhesive properties: Orabase, Carbopol 935P, and polymethyl methacrylate (PMM) and the ointment Miglyol without such properties were used. Benzyl nicotinate (BN) was used as an active ingredient that causes hyperemia. The kinetics of drug action was measured by electron paramagnetic resonance (EPR) oximetry in vivo using the paramagnetic probe (Lithium phthalocyanine) implanted beneath the epithelium of the buccal mucosa in rats. EPR spectra line-width was proportional to local changes of partial pressure of oxygen (pO(2)) in tissue and was monitored for 90 min after the application of ointments mixed with BN. The greatest increase in pO(2) and the highest efficiency of drug action was observed after the application of 2% BN in PMM (P<0.01). Additionally in PMM the drug effect increased linearly with BN concentration up to 3%, at higher concentrations (3.5 and 4% BN) no further effect was observed. The results demonstrated that the greatest and the longest effect caused by a hyperemic drug in PMM. By increasing the concentration of the drug in PMM higher pO(2) in the oral mucosa can be established but only until the saturation is reached.