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Abstract #8331 Published in IGR 4-3
Acetazolamide: future perspective in topical glaucoma therapeutics
Kaur IP; Smitha R; Aggarwal D; Kapil MInternational Journal of Pharmaceutics 2002; 248: 1-14
With this review it is hypothesized that acetazolamide (ACZ), an age-old treatment for glaucoma with a myriad of side-effects and inadequate topical effectiveness, may be formulated into a topically effective agent by utilizing various newer formulation approaches for ocular drug delivery. Even though it has a poor solubility and penetration power, various studies mentioned in the review indicate that it is possible to successfully formulate topically effective ACZ by using: (i) high concentration of the drug, (ii) surfactant gel preparations of ACZ, (iii) ACZ loaded into liposomes, (iv) cyclodextrins to increase the solubility and hence bioavailability of ACZ, and (v) viscolyzers and other polymers either alone or in combination with cyclodextrins. With the advent of newer topical carbonic anhydrase inhibitors (CAIs) such as dorzolamide and brinzolamide, a localized effect with fewer side-effects is expected. But whenever absorbed systemically, a similar range of adverse effects (attributable to sulphonamides) may occur upon use. Furthermore, oral ACZ is reported to be more physiologically effective than 2% dorzolamide hydrochloride administered topically, even though in isolated tissues dorzolamide appears to be the most active as it shows the lowest IC50 values for CA-II and CA-IV. Hence, there exists considerable scope for the development of more/equally effective and inexpensive topically effective formulations of ACZ. The use of various formulation technologies discussed in this review can provide a fresh impetus to research in this area.
I.P. Kaur, MD, University Institute of Pharmaceutical Science, Panjab University, Chandigarh 160014, India. indupalkaur@yahoo.com
Classification:
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)
