Glaucoma delivery

Gurny R (1981) Preliminary study of prolonged acting drug delivery system for the treatment of glaucoma. Pharm Acta Helv 56 130-132. 

Furthermore, by in vitro experiments, it has been verified that stereospecific activation of alprenoxime is organ-specific, occurring in the eye and not systemically. When administered locally to rabbits, marked decreases in intra-ocular pressure were observed, whereas oral administration elicited almost no cardiac effects. Such ketoximes represent promising chemical delivery systems in the treatment of glaucoma However, a major limitation is their poor stability in solution, seemingly due to hydrolysis of the oxime function. 

Hillman, J.S., J.B. Marsters, and A. Broad. 1975. Pilocarpine delivery by hydrophilic lens in the management of acute glaucoma. Trans Ophthalmol Soc UK 95 79. 

Diffusion-controlled membranes exist in two categories depot systems, in which the drug is totally encapsulated within a reservoir, and monolithic systems, where the drug is dispersed in a rate-controlling polymer matrix [25]. One commercially successful depot device is the Alza Ocusert for ocular delivery of pilocarpine in the treatment of glaucoma [25]. 

The first nanoparticulate delivery system studied was Piloplex, consisting of pilocarpine ionically bound to poly(methyl)methacrylate-acrylic acid copolymer nanoparticles [44], Klein et al. [1,98] found that a twice-daily application of Piloplex in glaucoma patients was just as effective as three to six instillations of conventional pilocarpine eye drops. However, the formulation was never accepted for commercialization due to various formulation-related problems, including the nonbiodegradability, local toxicity, and difficulty of preparing a sterile formulation [208],... 

More effective treatment of glaucoma has also been attempted using collagen shield technology. In this regard, shields have been shown to prolong delivery of pilocarpine and metipranolol. ... 

The authors concluded that when a woman taking glaucoma therapy becomes pregnant, it is usually possible to interrupt therapy during pregnancy. Treatment may be deferred until delivery of the infant. 

Pilocarpine (139) is used as a topical miotic for controlling elevated intraocular pressure associated with glaucoma. The drug presents significant delivery problems due to its low ocular bioavailability (1-3% or less) and its short duration of action. The poor bioavailability was partly attributed to its poor permeability across the corneal membrane due to its low lipophilicity. Because of the low bioavailability,... 

Ocusert (pilocarpine) a nondegradable insert for one-week delivery of the drug for the control of elevated intraocular pressure in pilocarpine-responsive glaucoma patients. 

In contrast to the LLC phases of GMO and (EO) -O-alkyl surfactants, only a handful of reports on the study of LLC phases of ionic surfactants for drug delivery are available. For example, the L, Qn, and Hu phases of the wa-ter/octanol/dioctyl sodium sulfosuccinate system have been studied for the transport of water and glucose across human skin [ 149]. Also, Qii phases of mixed ionic and uncharged phospholipids in water have been explored for the sustained in vitro release of timolol maleate, a drug for treatment of glaucoma [150]. 

EVAc has been used in the fabrication of a variety of devices for drug delivery. For example, EVAc was used by Alza in devices to deliver pilocarpine to the surface of the eye for glaucoma treatment (Ocusert). Currently, EVAc is used in the Progestasert intra-uterine device for the delivery of contraceptive hormones to the female reproductive tract and as a rate-controlling membrane in a number of transdermal devices. Since EVAc is one of the most biocompatible of the polymers that have been tested as implant materials [30], it has been widely studied as a matrix for controlled drug delivery (see [31, 32] for reviews). 

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