Development and In Vitro Assessment of Nanoemulsion for Delivery of Ketoconazole Against Candida albicans

Abstract

Nanoemulsions (NEs) applied as drug delivery systems are particularly convenient to increase solubility and the release of the drug with poor water solubility in water. The aim of this study was to prepare NEs containing Ketoconazole (KTZ), a poorly water-soluble drug, characterize them and evaluate their antifungal activity against Candida albicans. The solubility of KTZ was studied in different essential oils. Clove and sweet fennel essential oils were chosen as the oily phase and Pluronic F127® and Cremophor RH40® as the non-ionic surfactants to take part in the water phase. Formulations were prepared by a high-energy emulsification method and they were evaluated in terms of physical appearance, mean droplet size and polydispersity index. The NEs were successfully obtained and the droplets mean size was less than 100 nm. To verify efficacy of the NEs, the viability and the growth of C. albicans were measured by the propidium iodide influx analysis and by counting colony-forming units (CFU/mL). The results showed that the loss of the fungal membrane integrity and growth decrease were obtained after the treatment with the KTZ NEs containing clove oil (NEs-CL-KTZ) and with the free KTZ. However, the number of non-viable cells were significantly (p < 0.01) higher on the cells treated with NEs-CL-KTZ compared to the free KTZ. The In Vitro drug release profile demonstrated that NEs-CL-KTZ formulation could increase more than nine times the release of KTZ when compared to KTZ cream. To conclude, NEs-CL-KTZ tested in the present study has demonstrated the most efficient formulation for the treatment of C. albicans infections.

Striking Back against Fungal Infections: The Utilization of Nanosystems for Antifungal Strategies

“…There were 57% of patients with responses to ABLC, including 42% (55) of 130 cases of aspergillosis, 67% (28) of 42 cases of disseminated candidiasis, 71% (17) of 24 cases of zygomycosis, and 82% ( 9) of 11 cases of fusariosis [197] Nanoliposome with RDP (peptide derived from rabies virus glycoprotein for brain-targeting) The fungal membrane integrity and growth were decreased in NE-CL-KTZ treated group and the nanoemulsions improved KTZ release more than nine times when compared to KTZ cream [204] Nanoemulsions (NE) Amphotericin B (AmB) C. albicans, A. niger Skin candidiasis and aspergillosis NE enhanced AmB to cross the stratum corneum barrier in rat skin and displayed better fungicidal effects than AmB and Fungisome TM (commercial antifungal drug).…”

Development and characterization of a nanoemulsion containing propranolol for topical delivery

“…13 PF127 has been used in the preparation of oil/water NEs. Several NEs of essential oil have already been produced with PF127: peppermint, 14 clove, 15 sweet fennel, 16 and orange. 17 This work proposes the development of NE to promote the penetration and retention of PPN in the skin.…”

Emulsion-Based Multicompartment Vaginal Drug Carriers: From Nanoemulsions to Nanoemulgels

“…Although azoles have high antimycotic activity, their application is limited due to the insufficient water solubility [ 146 , 147 ]. Emulsion-based antifungal azoles formulations displayed high drug loading capacity, as well as increased drug bioavailability after both oral and topical administration as compared to commercial formulations and neat substances [ 148 , 149 , 150 , 151 , 152 , 153 , 154 , 155 , 156 , 157 ].…”