Acetazolamide: future perspective in topical glaucoma therapeutics

• Published in: International Journal of Pharmaceutics 2002-11, Vol.248 (1), p.1-14
• Main Authors: Kaur, Indu Pal, Smitha, R, Aggarwal, Deepika, Kapil, Mona
• Format: Article
• Language: English
• Subjects: Acetazolamide; Acetazolamide - administration & dosage; Acetazolamide - chemistry; Acetazolamide - pharmacokinetics; Administration, Topical; Animals; Biological and medical sciences; Carbonic anhydrase inhibitors; Eye; Forecasting; General pharmacology; Glaucoma; Glaucoma - drug therapy; Glaucoma - metabolism; Humans; Intraocular pressure; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/S0378-5173(02)00438-6

Through this review it is contemplated 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 of 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) like 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 IC 50 values for CA-II and CA-IV [M.F. Surgue, J. Ocular Pharmacol. Ther. 12 (1996) 363–376]. 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.