Characteristics of Skin Deposition of Itraconazole Solubilized in Cream Formulation

Abstract

Itraconazole (ITZ) is an anti-fungal agent generally used to treat cutaneous mycoses. For efficient delivery of ITZ to the skin tissues, an oil-in-water (O/W) cream formulation was developed. The O/W cream base was designed based on the solubility measurement of ITZ in various excipients. A physical mixture of the O/W cream base and ITZ was also prepared as a control formulation to evaluate the effects of the solubilized state of ITZ in cream base on the in vitro skin deposition behavior of ITZ. Polarized light microscopy and differential scanning calorimetry demonstrated that ITZ was fully solubilized in the O/W cream formulation. The O/W cream formulation exhibited considerably enhanced deposition of ITZ in the stratum corneum, epidermis, and dermis compared with that of the physical mixture, largely owing to its high solubilization capacity for ITZ. Therefore, the O/W cream formulation of ITZ developed in this study is promising for the treatment of cutaneous mycoses caused by fungi such as dermatophytes and yeasts.

Functionalized chitosan nanoparticles for cutaneous delivery of a skin whitening agent: an approach to clinically augment the therapeutic efficacy for melasma treatment

“…Samples from dorsal rat skin (Kim et al., 2019 ) were excised into small square parts and stretched on the diffusion cells in which the stratum corneum faced the donor chamber in Franz-diffusion apparatus (Alam et al., 2016 ). The receptor chamber was occupied with 7.2 ml PBS (pH 7.4), which was continuously stirred at 600 rpm at 32 ± 0.5 °C (El-Kayal et al., 2019 ).…”

Topical itraconazole formulations: Unscrupulous pharmaceutical companies and lax indian drug regulators endangering a precious drug

“…Therefore, to dissolve the drug in topical formulations such as cream or gel at a concentration of 1% is questionable in the absence of a novel drug delivery system, which is not apparent in the products currently available in the market. [ 26 ] Assuming that a suitable formulation is found, it would need to pass through the rigors of safety and efficacy studies mandatory for a new drug which have not been done in these topical formulations and are hence illegal. It would not be remiss to note here that topical itraconazole has been patented by a group of researchers in 2012 itself in the USA[ 27 ] and Europe,[ 28 ] and due consideration should be given to this fact before any permission to manufacture and market it is granted in India.…”

Preparation of Topical Itraconazole with Enhanced Skin/Nail Permeability and In Vivo Antifungal Efficacy against Superficial Mycosis

“…The epidermis was then carefully isolated from the dermis using a pair of forceps. The stripped tape containing stratum corneum, epidermis, and dermis was cut into small pieces and immersed in 5 mL of methanol and then extracted via vortex mixing for 24 h [ 13 ]. The resulting suspensions were filtered using membrane filters (0.45-µm pore size) and transferred to glass vials.…”

“…However, the semi-solid nature of colloidal carriers minimizes drug release and reduces formulation spreading on the skin surface. It also leads to limited permeability across the skin membrane [ 13 ]. Furthermore, residues of particulate carriers on skin after the application of the above formulations may reduce patient compliance.…”