PubMed · 3684795
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E Lopez, V Dvonch. 1987. Consultation corner. Discitis.. https://doi.org/10.3928/0147-7447-19871001-20
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The chemistry of organic polycyclic cage compounds has intrigued medicinal chemists for over 50 years, yet little is published about their pharmacological profiles. Polycyclic cage compounds have important pharmaceutical applications, ranging from the symptomatic and proposed curative treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's disease (e.g., amantadine and memantine), to use as anti-viral agents against influenza and the immunodeficiency virus (HIV). The polycyclic cage appears to be a useful scaffold to yield drugs with a wide scope of applications, and can be used also to modify and improve the pharmacokinetic and pharmacodynamic properties of drugs in current use. This review attempts to summarize the pharmacological profiles of polycyclic cage compounds with an emphasis on the lesser known pentacycloundecanes, homocubanes, and trishomocubanes.
The site-specific expression of selectins (P- and E-selectin) on endothelial cells of blood vessels during inflammation provides an opportunity for the targeted delivery of anti-inflammatory drugs to sites of chronic inflammation. It is well documented that the selectins mediate the initial interaction (rolling) of leukocytes in an inflamed vessel by binding to carbohydrate-presenting counter-receptors displayed on leukocytes. Previous work in our laboratory has shown that artificial capsules with the adhesive properties of leukocytes can be made by attaching leukocyte adhesive ligands to polymer microspheres (Biomaterials 23(10) (2002) 2167). Specifically, we showed that drug-loaded poly (lactic-co-glycolic-acid) (PLGA) microspheres coated with biotinylated-Sialyl LewisX (sLeX), a carbohydrate that serves as a ligand to selectins, mimic the adhesive behavior of leukocytes on selectins in flow chambers, displaying slow rolling under flow, suggesting that these drug-loaded particles can potentially target inflammatory sites in vivo. Since the effectiveness of this delivery system might depend on the degradation of polymer microspheres as well as the degradation of sLeX molecules, we measured the effect of polymer and ligand degradation on the adhesiveness of microspheres over time. We show that degrading sLeX microspheres maintain the ability to recognize selectin surfaces under flow for at least 2 weeks and that the ability to sustain recognition depends upon the extent at which microspheres are loaded. We also show that microsphere rolling velocity increases as microsphere degrade and that this increase is due to a combination of increase in average microsphere size and loss of sLeX molecules on microsphere surface--a result of microsphere degradation confirmed by flow cytometry. Control experiments show that microsphere, not sLeX, degradation limits the lifetime of our targeted delivery system; therefore, factors affecting degradation such as type of polymer, type of drug, extent of drug loading and microsphere size, provide an opportunity for engineering the time-scale of activity for the delivery system.
PURPOSE: To report the use of commercially available preservative-free intravitreal triamcinolone acetonide for the treatment of macular oedema due to retinal vascular diseases. DESIGN: Retrospective interventional case series. METHODS: Charts of eyes that received 4 mg preservative-free intravitreal triamcinolone acetonide for the treatment of persistent macular oedema due to retinal vascular diseases were reviewed. Patients were included if they had a follow-up of at least 3 months. Visual acuity, intraocular pressure, presence of an anterior chamber reaction, and mean macular thickness on optical coherence tomography (OCT) were recorded. RESULTS: A total of 10 eyes of 10 patients were identified. Visual acuity improved by a mean of 1.1 Snellen lines at 1 month and 1.3 lines at 3 months. Macular thickness on OCT decreased by a mean of 183.5 microm at 1 month (P<0.0001). Intraocular pressure increased from a mean of 13.5 mmHg at baseline to 15.3 at 1 month, and 14.5 at 3 months. Only the 1-month change in intraocular pressure was statistically significant (P=0.0274). There were no cases of endophthalmitis, anterior chamber reaction, or retinal detachment. CONCLUSION: In this small retrospective, noncomparative series, commercially available preservative-free intravitreal triamcinolone acetonide had no adverse outcomes. Macular oedema was noted to decrease following treatment.