Assessment of antifungal efficacy of itraconazole loaded aspasomal cream: comparative clinical study

Abstract

Topical conveyance of antifungal agents like itraconazole ITZ has been giving good grounds for expecting felicitous antifungal medicines. The defiance of topical delivery of this poorly water soluble and high-molecular-weight drug, however, mightily entail an adequate vehiculation. ITZ aspasomes, newer antioxidant generation of liposomes, have been designed and enclosed in a cream to ameliorate skin deposition. The proposed creams containing non-formulated ITZ or encapsulated in aspasomes (0.1% or 0.5%) were topically applied in patients with diagnosed diaper dermatitis complicated by candidiasis, tinea corporis (TC), and tinea versicolor (TVC). Placebos (void aspasomal cream and cream base) were also utilized. The obtained results for diaper rash revealed that aspasomal cream (0.5% ITZ) was eminent with respect to complete cure and negative candida culture after 10-day therapy relative to counterparts containing 0.1% ITZ aspasomes or non-formulated ITZ (0.1% and 0.5%). For tinea, the same trend was manifested in terms of ‘cleared’ clinical response in 90% of patients and absence of fungal elements after 4-week treatment. Relative to non-formulated ITZ, ITZ aspasomal cream was endorsed to be auspicious especially when ITZ concentration was lowered to half commercially available cream concentration (1%), pushing further exploitation in other dermal fungal infections.

Organic and Biogenic Nanocarriers as Bio-Friendly Systems for Bioactive Compounds’ Delivery: State-of-the Art and Challenges

“…Aspasomes are the newer antioxidant generation of liposomes; they are nano-vesicular antioxidant systems containing ascorbyl palmitate (a liposoluble vitamin C derivative), cholesterol, and phospholipids that have the ability to form stable vesicular bilayers [157]. The preparation, characterization, and applications of aspasomes were firstly reported in 2004 by Gopinath et al [158].…”

“…The preparation, characterization, and applications of aspasomes were firstly reported in 2004 by Gopinath et al [158]. Since then, aspasomes have been successfully used as nanocarriers for the dermal and transdermal delivery of various drugs and/or bioactives for the treatment of skin injuries (e.g., acne, melasma, psoriasis, fungal infections, skin cancer) [157,[159][160][161][162], or for the management of rheumatoid disease [163] and muscle spasms [164]. Hatem et al developed aspasomes loaded with melatonin, a bioactive antioxidant molecule, as a novel cosmeceutical for the clinical treatment of androgenic alopecia [165].…”

Tinea versicolor: an updated review

“…156 Recently, it has been shown that itraconazole-loaded aspasomal cream has a higher efficacy in the treatment of tinea versicolor than non-formulated itraconazole cream alone. 177 Terbinafine Terbinafine, an allylamine antifungal, works by inhibiting squalene epoxidase, thereby blocking the biosynthesis of ergosterol. 87,163,178 The accumulation of squalene accounts for its fungicidal activity whilst ergosterol deficiency accounts for its fungistatic activity.…”

“… 156 Recently, it has been shown that itraconazole-loaded aspasomal cream has a higher efficacy in the treatment of tinea versicolor than non-formulated itraconazole cream alone. 177 …”

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

“…Oral preparations of ITZ including solutions and capsules as well as intravenous preparations are well-known and widely used in medicine. Recently, due to toxicity concerns associated with systemic use, ITZ is increasingly being investigated for its topical antifungal activities and many reports proved it can be successfully delivered via this route [ 10 , 11 ].…”