Enhanced Percutaneous Penetration With 1-Dodecylazacycloheptan-2-one

Stoughton, Richard B.

doi:10.1001/archderm.1982.01650190028013

Cited by 138 publications

(29 citation statements)

References 6 publications

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“…Penetration-enhancing agents have not been adequately explored in the formulation of topical antiviral preparations. In addition to dimethyl sulfoxide, dimethylacetamide, N,N-diethyl-m-toluamide, and 1-dodecylazacycloheptan-2-one (Azone; Nelson Research, Irvine, Calif.) have been shown to enhance percutaneous penetration (9,11). Agents such as these should be combined with an effective antiviral agent as a next step in the attempt to realize the full potential of topical treatment of cutaneous HSV infections.…”

Section: Discussionmentioning

confidence: 99%

Early, patient-initiated treatment of herpes labialis with topical 10% acyclovir

Spruance¹,

Crumpacker²,

Schnipper³

et al. 1984

Antimicrob Agents Chemother

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To determine whether topical acyclovir in polyethylene glycol could reduce the severity of herpes simplex labialis if applied immediately after onset of a recurrence, 10% acyclovir in polyethylene glycol ointment or polyethylene glycol alone was prospectively dispensed to 352 patients in a double-blind, randomized trial. Sixty-nine subjects initiated treatment in the prodrome (57%) or erythema (43%) stage and were followed by clinical and virological criteria, The healing time (6.0 days), maximum lesion area (42 mm2), vesicle or ulcer formation (91%), and maximum lesion virus titer (4.8 logl0 PFU) in the drug recipients were not reduced in comparison with those who received the vehicle (5.2 days, 30 mm2, 75%, and 4.5 log10 PFU, respectively). Topical acyclovir in polyethylene glycol was ineffective for the treatment of herpes labialis despite an optimum therapeutic opportunity.

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Section: Discussionmentioning

confidence: 99%

Early, patient-initiated treatment of herpes labialis with topical 10% acyclovir

Spruance¹,

Crumpacker²,

Schnipper³

et al. 1984

Antimicrob Agents Chemother

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“…Azone can be applied neat to human skin without any irritation (20); Likewise, 5% Azone in either water or DMSO did not prove irritating to the hairless mouse skin. When formulated in AZDMSO, BVdU was effective at a concentration as low as 0.3% in suppressing HSV-1 skin infection and mortality associated therewith in hairless mice (Table 2).…”

Section: Discussionmentioning

confidence: 90%

Topical treatment of cutaneous herpes simplex virus infection in hairless mice with (E)-5-(2-bromovinyl)-2'-deoxyuridine and related compounds

Clercq¹

1984

Antimicrob Agents Chemother

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(E)-5-(2-Bromovinyl)-2'-deoxyuridine (bromovinyldeoxyuridine) was found to suppress the development of herpetic skin lesions and the paralysis and mortality associated therewith in hairless mice inoculated intracutaneously with herpes simplex virus type 1. This protective effect was achieved with bromovinyldeoxyuridine applied topically at 1, 3, or 10% in either dimethylsulfoxide (DMSO), Beeler base, Tween-glycerol-water, 5% Azone (1-dodecylazacycloheptan-2-one) in water, or 5% Azone in DMSO. The optimal vehicle was 5% Azone in DMSO, in which bromovinyldeoxyuridine was effective even at a concentration as low as 0.3%. In its protective activity against cutaneous herpes simplex virus type 1 infection in hairless mice, bromovinyldeoxyuridine was clearly superior to other established antiherpes compounds such as 5-iodo-2'-deoxyuridine, 5-ethyl-2'-deoxyuridine, arabinosyl thymine, and arabinosyl (E)-5-(2-bromovinyl) uracil when formulated at 10% in DMSO or Azone-DMSO. However, no activity was noted with any of these drug formulations against cutaneous herpes simplex virus type 2 infection. In contrast, acycloguanosine (acyclovir) proved quite effective in the topical treatment of cutaneous herpes simplex virus type 2 infection when used at 10% in DMSO or at 5% in propylene glycol.Intracutaneous inoculation of hairless (hr/hr) mice with herpes simplex virus type 1 (HSV-1) or type 2 (HSV-2) represents an adequate experimental model for determining the efficacy of topically applied antiviral drugs against primary HSV infections. This model allows one to monitor the effects of the drugs on both local (skin lesions) and systemic (paralysis, death) manifestations of the disease and has been used to establish the effectiveness of such antiviral agents as phosphonoacetic acid (PAA) (16,17) Few studies have focused on the relative efficacy of antiviral compounds in the topical treatment of HSV infections. Alenius and Oberg (3) noted that of five antiviral agents, AraA, arabinosyl cytosine, iododeoxyuridine, ribavirin, and PAA, only PAA showed good therapeutic activity against cutaneous HSV-1 infection in guinea pigs. A similar therapeutic effect was noted for PFA (2), and when compared with ACV, PFA proved clearly superior for topical treatment of HSV-1 skin lesions in guinea pigs (1). In the latter study ACV and PFA were formulated in different (and not necessarily optimal) vehicles, which makes a direct comparison of their efficacy rather difficult. When ACV, PFA, and several other antiviral compounds were compared under standardized conditions, i.e., applied topically at 1% in Beeler base (BB) in athymic nude mice infected intracutaneously with HSV-1, their order of activity was PAA > BVdU -ACV > PFA > AraA (10).The efficacy of antiherpes agents in the topical treatment of cutaneous HSV infection may vary considerably, depending on a number of factors such as the intrinsic antiviral potency of the compound (8), the virus type and strain used, the time at which treatment is started, the concentration at which the drug is a...

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“…Azone is an effective permeation enhancer for both hydrophilic and lipophilic permeants [139][140][141]. For example, Azone was shown to enhance 5-fluorouracil penetration by 100-fold across hairless rat skin [142].…”

Section: Azonementioning

confidence: 99%

Innovative Strategies for Enhancing Topical and Transdermal Drug Delivery

Morrow¹,

McCarron²,

Woolfson³

et al. 2007

TODDJ

124

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Abstact: Historically, the skin was thought to be a simple homogenous barrier. However, it is now known to be a highly specialised organ, and plays a key role in homeostasis. The protective properties of the skin are provided by the outermost layer, the epidermis, which safeguards against chemical, microbial, and physical attack. The exceptional barrier properties of the skin result in it being a challenging route for the delivery of therapeutic agents. This article reviews strategies developed to enhance the skin penetration of drugs, ranging from conventional approaches, for example the use of chemical penetration enhancers to those in early-stage development, such as microscissioning.

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Enhanced Percutaneous Penetration With 1-Dodecylazacycloheptan-2-one

Cited by 138 publications

References 6 publications

Early, patient-initiated treatment of herpes labialis with topical 10% acyclovir

Early, patient-initiated treatment of herpes labialis with topical 10% acyclovir

Topical treatment of cutaneous herpes simplex virus infection in hairless mice with (E)-5-(2-bromovinyl)-2'-deoxyuridine and related compounds

Innovative Strategies for Enhancing Topical and Transdermal Drug Delivery

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