PubMed · 10223869
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M Maegele. 1999. [Allergic rhinitis. Topical steroids without systemic effect].. https://pubmed.ncbi.nlm.nih.gov/10223869/
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The aim of this study was to provide evidence for the peripheral effect of opioids in oromaxillary procedures and to investigate whether postoperative morphine sulfate plus lidocaine administered as a local spray achieve better analgesic efficacy than lidocaine applied alone. The double-blind randomized study included 60 patients. The patients exhibited neither preoperative pain nor inflammation (tooth extractions) and when pain occurred received as alternative medication diclofenac retard 50 mg or tramadol. Side effects were documented. No differences between the two groups were observed in the demographic data, visual and numeric analog scale in the first 24 h, or in the consumption of analgesics. Since the patients presented in a pain-free state at the time of surgery, apparently no activation of the peripheral opioid receptors occurs. Thus, a peripheral effect of opioids could not be demonstrated in this model.
Highly deformable hydrophilic lipid vesicles have been studied for transdermal delivery of therapeutically active small molecules and proteins. Here, we report the effects of edge activators on the formation of ultradeformable liposomes (UL) and transdermal gene delivery. Sodium cholate, sodium deoxycholate, and Tween 80 were tested as edge activators. Of the edge activators, sodium cholate and sodium deoxycholate resulted in the smaller sizes of UL and more positive zeta potentials than did Tween 80. Moreover, sodium deoxycholate-based UL showed the highest positive zeta potentials, which might lead to the firmer binding with negatively charged DNA. Following topical application onto mice, DNA complexed with UL containing either sodium cholate or sodium deoxycholate showed substantial transdermal absorption. In contrast, DNA complexed with Tween 80-based UL did not show in vivo transdermal absorption. These data suggest that UL might be of use as a transdermal delivery system of plasmid DNA, and that the choice of edge activators may play an important role in the transdermal delivery of plasmid DNA via UL.
A novel series of 15-fluoro prostaglandins with phenoxy termination of the omega-chain was synthesized and evaluated for binding and functional activation of the prostaglandin FP receptor in vitro and for side effect potential and topical ocular hypotensive efficacy in vivo. Compounds with the 15alpha-fluoride relative stereochemistry displayed EC50 values of <or=20 nM, comparable to the value for the endogenous ligand PGF2alpha. Evaluation of selected ester prodrugs of these 15-fluoro prostaglandins in vivo highlighted their generally low propensity to elicit hyperemia or ocular irritation in rabbits and efficacious intraocular pressure-lowering property in monkeys. In particular 13,14-dihydro-15-deoxy-15alpha-fluoro-16-aryloxy-omega-tetranor-cis-Delta4-PGF2alpha isopropyl ester (24) caused relatively little ocular irritation in rabbits while lowering intraocular pressure in conscious ocular hypertensive monkeys by 39% following a topical ocular dose of 3 microg.