Acyclovir — A review of the preclinical and early clinical data of a new antiherpes drug

Brigden, D.; Fiddian, P; Rosling, Ari; Ravenscroft, T

doi:10.1016/0166-3542(81)90011-5

Cited by 49 publications

(23 citation statements)

References 31 publications

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“…2 The same suggestion has been made for humans based on a decline in percentage acyclovir urinary recovery with increasing dosage. 17 The high degree of species variation and intestinal variability, along with the fact that some investigators have reported active transport for other purines, also seems to suggest that carrier-mediated transport may be involved in the intestinal uptake of acyclovir. On the other hand, the low oral bioavailability may simply be a function of poor membrane permeability owing to low partition coefficient of acyclovir (P = .023).…”

Section: Bioavailability and Pharmacokineticsmentioning

confidence: 99%

Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

et al. 2007

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The purpose of this research was to prepare acyclovir niosomes in a trial to improve its poor and variable oral bioavailability. The nonionic surfactant vesicles were prepared by the conventional thin film hydration method. The lipid mixture consisted of cholesterol, span 60, and dicetyl phosphate in the molar ratio of 65:60:5, respectively. The percentage entrapment was~11% of acyclovir used in the hydration process. The vesicles have an average size of 0.95 μm, a most probable size of 0.8 μm, and a size range of 0.4 to 2.2 μm. Most of the niosomes have unilamellar spherical shape. In vitro drug release profile was found to follow Higuchi's equation for free and niosomal drug. The niosomal formulation exhibited significantly retarded release compared with free drug. The in vivo study revealed that the niosomal dispersion significantly improved the oral bioavailability of acyclovir in rabbits after a single oral dose of 40 mg kg −1 . The average relative bioavailability of the drug from the niosomal dispersion in relation to the free solution was 2.55 indicating more than 2-fold increase in drug bioavailability. The niosomal dispersion showed significant increase in the mean residence time (MRT) of acyclovir reflecting sustained release characteristics. In conclusion, the niosomal formulation could be a promising delivery system for acyclovir with improved oral bioavailability and prolonged drug release profiles.

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Section: Bioavailability and Pharmacokineticsmentioning

confidence: 99%

Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

et al. 2007

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“…An effective antiviral compound for these two herpesvirus diseases would therefore be of considerable value. Acyclovir (9-[2-hydroxyethoxymethyl]guanine) (ACV) has proven activity against herpes simplex both in vitro and in vivo (5,6) and is now available (Zovirax; Wellcome Foundation Ltd., London, United Kingdom) for the treatment of certain herpetic conditions in humans. Activity in vitro has also been demonstrated against varicella zoster virus, Epstein-Barr virus, and cytomegalovirus (10).…”

Section: Elucidatedmentioning

confidence: 99%

Relative activities of acyclovir and BW759 against Aujeszky's disease and equine rhinopneumonitis viruses

Rollinson¹,

White²

1983

Antimicrob Agents Chemother

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“…Brigden et aL, 1981 ;De Clercq et al, 1980a). Each compound has to be activated to its triphosphate form in the infected cell and it is this form which disrupts virus DNA synthesis (Elion et al, 1977;Furman et al, 1979;Derse et aL, 1981 ;Allaudeen et al, 1981).…”

Section: Introductionmentioning

confidence: 99%

Characterization of Abnormal Thymidine Kinases Induced by Drug-resistant Strains of Herpes Simplex Virus Type 1

Larder

Cheng

Darby

1983

Journal of General Virology

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SUMMARYTwo TK + acyclovir-resistant variants of herpes simplex virus (HSV) (S1 and Tr7) and one TK + BVdU-resistant variant (B3) induce abnormal thymidine kinases with impaired ability to phosphorylate the drugs used in their isolation. These enzymes have been purified and their properties compared with those of the wild-type (wt) parent, SC16. The enzyme induced by S1 differed markedly from the other three in both its responses to salt and to pH. B3 TK recognized the enzyme's natural substrates, thymidine, deoxycytidine, dTMP and ATP as well as the wt enzyme. In contrast, Tr7 and S 1 TKs failed to bind deoxycytidine and bind thymidine less well than wt. Tr7 and S1 TKs had affinities for dTMP similar to those of B3 and the wt enzymes. ATP binding to wt, Tr7 and B3 enzymes was similar but this substrate bound only weakly to S1 TK. Each mutant displayed a characteristically distinct pattern of affinities for a range of nucleoside analogue substrates, suggesting that they will show some crossresistance to drugs which have a similar mechanism of action to acyclovir and BVdU.

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Acyclovir — A review of the preclinical and early clinical data of a new antiherpes drug

Cited by 49 publications

References 31 publications

Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

Relative activities of acyclovir and BW759 against Aujeszky's disease and equine rhinopneumonitis viruses

Characterization of Abnormal Thymidine Kinases Induced by Drug-resistant Strains of Herpes Simplex Virus Type 1

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