Preparation of luliconazole nanocrystals loaded hydrogel for improvement of dissolution and antifungal activity

Abstract

Superficial fungal infection in immunocompromised patients can lead to many disorders and complications. Currently, new topical treatment options are critically needed to treat these fungal infections. Luliconazole (LZL) is a topical antifungal medicine used for fungal infection treatment. The purpose of this paper was to develop a new topical luliconazole nanocrystal (LNC) incorporated hydrogel. This study suggested the potential benefits of LNC embedded in a gel as a drug delivery system for topical antifungal treatments. Preliminary experiments were therefore carried out to characterize the LNC in comparison with raw drug. Prepared gel was homogeneous for human use with about 88 percent trapping, non-irritant and safe. Nano-systems showed an overall 5 fold enhancement in solubility, 4 fold increase in dissolution velocity, higher skin retention and better antifungal activity. Drugs retained from LNC hydrogel (N-GEL) in different skin layers within 8 h were the highest, i.e. 62.17% compared to coarse suspension (41.87%), nanosuspension (49.77%), D-GEL (55.76%). In addition, LNC and N-GEL had higher ZOI (41.20 ± 0.61mm and 44.25 ± 0.57mm respectively) than LZL and D-GEL (35.98 ± 0.81mm and 36.83 ± 0.83mm respectively). Therefore, it was observed that LNC loaded hydrogel was more effective in killing the fungus. Consequently, hydrogel incorporated with LNC could be a new approach with improved activity and increased dermal delivery for drugs with poor aqueous solubility rather than coarse drug containing gel.

Hydrogel or ointment? Comparison of five different galenics regarding tissue breathability and transepidermal water loss

“…Clinical data in combination with tyrothricin are already available for the hydrogel base used in this study [ 29 ]. Luliconazole has recently been shown to be more effective against fungal infections when embedded in a hydrogel formulation [ 30 ]. Numerous publications have already described the mode of action and high efficiency of hydrogels in the healing of various wounds [ 31 ].…”

Hydrogel-Based Active Substance Release Systems for Cosmetology and Dermatology Application: A Review

“…Due to the lack of an optimal treatment method for superficial fungal infections, which often also leads to many complications, Kumar et al attempted to develop a topical hydrogel containing luliconazole nanocrystalline (LZL), which is a broad-spectrum local antifungal drug. As it is commonly known, fungal infections can affect various layers of the skin, so achieving a satisfactory result of treatment is conditioned by the delivery and retention of an appropriate dose of the drug both in the epidermis and dermis layers [80]. In recent years there has been a great interest in preparations based on various types of nanocarriers, including nanocrystals as potential carriers for various pharmacological substances.…”

Luliconazole‐loaded nanostructured lipid carriers for topical treatment of superficial Tinea infections

“…Many researchers have worked on nanoparticulate systems such as nanosponges and microemulsion based gel 9,12 . Kumar et al worked on luliconazole nanocrystals loaded hydrogel for improvement of dissolution and anti‐fungal activity, 13 Dave et al reported improved dermal delivery of luliconazole from herbal ethosomal gel of luliconazole 14 and Kaur et al prepared vesicular‐based gel of luliconazole for enhanced topical delivery 11 . Nanostructured lipid carriers (NLCs) are an upgrade to the ordinary carrier systems such as microemulsions and liposomes as it offers advantage of exhibiting higher drug loading capacity, large surface area and small size 15 .…”