Activity of TDT 067 (Terbinafine in Transfersome) against Agents of Onychomycosis, as Determined by Minimum Inhibitory and Fungicidal Concentrations

Ghannoum, Mahmoud A.; Isham, N.; Herbert, Jacqueline; Henry, W. Brien; Yurdakul, Sam

doi:10.1128/jcm.00083-11

Cited by 46 publications

(20 citation statements)

References 34 publications

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“…Perhaps the use of a more innovative delivery vehicle would generate a clearer picture of the effectiveness of dual therapy. For example Ghannoum et al (2011) have incorporated terbinafine within transfersomes (described by Ghannoum et al as "carrier vehicles [consisting of] responsive, composite lipid aggregates that are highly deformable and have high surface hydrophilicity") and demonstrated that such vehicles, at an active concentration of 1.5% (w/v), were considerably more potent (with MIC 50 values against Trichophyton rubrum and Tricophyton mentagrophytes being 30-fold and 60-fold lower, respectively) than a 1% terbinafine spray in vitro.…”

Section: Current Approaches and Clinical Evidencementioning

confidence: 98%

The human nail – Barrier characterisation and permeation enhancement

Walters¹,

Abdalghafor

Lane

2012

International Journal of Pharmaceutics

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Section: Current Approaches and Clinical Evidencementioning

confidence: 98%

The human nail – Barrier characterisation and permeation enhancement

Walters¹,

Abdalghafor

Lane

2012

International Journal of Pharmaceutics

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“…It is a potential treatment option for toenail onychomycosis which is still under trial for safety and efficacy. 151,152 ME1111 acts by inhibiting succinate dehydrogenase, an enzyme in the electron transport chain, which in turn affects ATP production in fungal cells. It has a small molecular size and has higher penetration capacity in the nail plate than ciclopirox.…”

Section: Novel Topical Therapiesmentioning

confidence: 99%

Onychomycosis: a review

Gupta

Stec

Summerbell

et al. 2020

Acad Dermatol Venereol

186

245

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Onychomycosis is a fungal infection of the nail, causing discoloration and thickening of the affected nail plate, and is the most common nail infection worldwide. Onychomycosis was initially thought to be predominantly caused by dermatophytes; however, new research has revealed that mixed infections and those caused by non‐dermatophyte moulds (NDMs) are more prevalent than previously thought, especially in warmer climates. Microscopy and fungal culture are the gold standard techniques for onychomycosis diagnosis, but high false‐negative rates have pushed for more accurate methods, such as histology and PCR. As NDMs are skin and laboratory contaminants, their presence as an infectious agent requires multiple confirmations and repeated sampling. There are several treatment options available, including oral antifungals, topicals and devices. Oral antifungals have higher cure rates and shorter treatment periods than topical treatments, but have adverse side effects such as hepatotoxicity and drug interactions. Terbinafine, itraconazole and fluconazole are most commonly used, with new oral antifungals such as fosravuconazole being evaluated. Topical treatments, such as efinaconazole, tavaborole, ciclopirox and amorolfine have less serious side effects, but also have generally lower cure rates and much longer treatment regimens. New topical formulations are being investigated as faster‐acting alternatives to the currently available topical treatments. Devices such as lasers have shown promise in improving the cosmetic appearance of the nail, but due to a high variation of study methods and definitions of cure, their effectiveness for onychomycosis has yet to be sufficiently proven. Recurrence rates for onychomycosis are high; once infected, patients should seek medical treatment as soon as possible and sanitize their shoes and socks. Prophylactic application of topicals and avoiding walking barefoot in public places may help prevent recurrence.

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“…In vitro experiments have demonstrated that TDT 067 has potent inhibitory and cidal activity against dermatophytes and has enhanced antifungal activity compared to that of conventional terbinafine preparations (10). The excipients of TDT 067 are widely used in pharmaceutical and cosmetic products for topical application, and clinical studies involving more than 2,000 patients with different diseases have shown that Transfersome preparations are well tolerated (2,16,22).…”

mentioning

confidence: 99%

Evaluation of the Morphological Effects of TDT 067 (Terbinafine in Transfersome) and Conventional Terbinafine on Dermatophyte Hyphae In Vitro and In Vivo

Ghannoum

Isham

Henry

et al. 2012

Antimicrob Agents Chemother

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TDT 067 is a novel, carrier-based dosage form of terbinafine in Transfersome (1.5%) formulated for topical delivery of terbinafine to the nail, nail bed, and surrounding tissue. We examined the effects of TDT 067 and conventional terbinafine on the morphology of dermatophytes. Trichophyton rubrum hyphae were exposed to TDT 067 or terbinafine (15 mg/ml) and examined under white light, scanning electron microscopy (SEM), and transmission electron microscopy (TEM). Subungual debris from patients treated with TDT 067 in a clinical trial was also examined. Exposure of T. rubrum hyphae to TDT 067 led to rapid and extensive ultrastructural changes. Hyphal distortion was evident as early as 4 h after exposure to TDT 067. After 24 h, there was complete disruption of hyphal structure with few intact hyphae remaining. Exposure to terbinafine resulted in morphological alterations similar to those seen with TDT 067; however, the effects of TDT 067 were more extensive, whereas a portion of hyphae remained intact after 24 h of exposure to terbinafine. Lipid droplets were observed under TEM following 30 min of exposure to TDT 067, which after 24 h had filled the intracellular space. These effects were confirmed in vivo in subungual debris from patients with onychomycosis who received topical treatment with TDT 067. The Transfersome in TDT 067 may potentiate the action of terbinafine by delivering terbinafine more effectively to its site of action inside the fungus. Our in vivo data confirm that TDT 067 can enter fungus in the nail bed of patients with onychomycosis and exert its antifungal effects.

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Activity of TDT 067 (Terbinafine in Transfersome) against Agents of Onychomycosis, as Determined by Minimum Inhibitory and Fungicidal Concentrations

Cited by 46 publications

References 34 publications

The human nail – Barrier characterisation and permeation enhancement

The human nail – Barrier characterisation and permeation enhancement

Onychomycosis: a review

Evaluation of the Morphological Effects of TDT 067 (Terbinafine in Transfersome) and Conventional Terbinafine on Dermatophyte Hyphae In Vitro and In Vivo

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