Novel Citric Acid Dendritic Hydrogels for the Delivery of Econazole Nitrate and its Antifungal Activity

Abstract

Econazole is an imidazole derivative antifungal drug with distinguished antifungal properties. But the bioavailability of conventional econazole preparations is poor because of poor solubility and lipophilicity or lipophilic nature. Thus frequent application of the preparation is required to maintain therapeutic levels at the site of action. Such repeated doses may produce toxic affects thereby limiting the clinical use of the drug. Citric acid dendrimers give an opportunity to overcome the above limitations by improving its solubilization and drug permeation properties. Thus, the aim of current study is to design citric acid dendrimer hydrogels and study its influence on the drug release and anti-fungal activity of loaded drug. Dendritic architecture and size strongly influences the invitro release and antifungal activity of drug. Antifungal activity of designed Econazole hydrogel was measured by Agar plate diffusion method. Zone of inhibition values showed that citric acid dendrimers considerably enhanced the antifungal activity of Econazole to a greater extent and the effect was more with lower generation hydrogels. The operative mechanism is probably the smaller size (G2) that penetrates the fungal cell membrane more efficiently than higher generation (G3 and G4) hydrogels.

Application or function of citric acid in drug delivery platforms

“…All of the dendrimer/drug conjugates showed a larger inhibition zone in comparison with pure drugs. As well, among the dendritic hydrogels, the G2 displayed larger values than G3 and G4, which attributed to the smaller size of G2, leading to the more efficient penetration to the fungal cell membrane in comparison with a higher generation of dendrimers 54 …”

“…As well, among the dendritic hydrogels, the G2 displayed larger values than G3 and G4, which attributed to the smaller size of G2, leading to the more efficient penetration to the fungal cell membrane in comparison with a higher generation of dendrimers. 54 Reddy et al designed and synthesized the 3rd generation of PEGylated CA dendrimer to increases the circulation time, decrease the nonspecific systemic toxicity, and provide prolonged drug release. Minocycline as a common antibacterial drug was loaded (457 mg of minocycline) into the prepared PEGylated CA dendrimer with three different ratios.…”

Tissue Distribution, Cytotoxicity and Pharmacokinetic Studies of Multifunctional Citric Acid Dendrimers using the Drug Cyclophosphamide

“…Synthesis and PEGylation of citric acid dendrimers : 5 th generation citric acid dendrimers were synthesized via the same divergent technique as reported in our previous work 15 . The synthesized dendrimers were PEGylated as per the following procedure: Synthesized dendrimers were dissolved in 10ml of DMF completely and 5 moles of N, N' dicyclohexylcarbodimide was added and stirred thoroughly and kept aside undisturbed for 4 days.…”

Pharmaceutical applications of citric acid

“…Overall, CA dendrimers are an approach toward refining therapeutic efficiency, solubility, and bioavailability of entrapped drugs. Thus, it may novel carriers for antifungal agent delivery [38]. Namazi and co-authors were developed gold nanoparticles (Au NPs) in the existence of diverse generations of CA-based dendrimers.…”