The Effect of the New Imidazole Derivatives Complexation with Betacyclodextrin, on the Antifungal Activity in Oropharyngeal Infections

Abstract

Ketoconazole (KZ) is a broad-spectrum drug used to treat fungal infections. Local use of ketoconazole has been associated with some side effects in healthy adults, especially local reactions, such as stinging, severe irritation, and itching. Moreover, the bioavailability of KZ after oral administration is low in tablets due to its low water solubility. In addition, oral administration of ketoconazole produces systemic exposure, associated with significant side effects, such as cholestatic and hepatocellular lesions. In an attempt to reduce hepatotoxicity, ketoconazole may be administered at the primary site of infection with cutaneous candidiasis, specifically on the skin tissue. However, the use of ketoconazole in topical dosage forms is limited by its high lipophilicity and extremely poor aqueous solubility (1 ng/mL), thus leading to the rare availability of topical dosage forms on the market. Therefore, a new approach to the effective delivery of ketoconazole to the site of infection is targeted, including obtaining new derivatives (keeping the imidazolic nucleus), with a similar spectrum of action, and finally, their inclusion in betacyclodextrin complexes in order to optimize bioavailability and physico-chemical stability.

Experimentally Induced Burns in Rats Treated with Innovative Polymeric Films Type Therapies

“…Thus, in our case, even the new compounds will have this property as long as the tetracyclic structure remains unchanged. In addition, the structural modification of oxytetracycline has, in some of the cases (OXI-B and OXI-C), a positive influence on the antimicrobial activity, both through the aromatic nucleus introduced into the structure of the new compounds and through the azomethine group, known for its impact on this effect [ 10 ]. Oxytetracycline inhibits cell growth by inhibiting translation [ 28 ], a mechanism that can be also considered for the derivatives obtained in our study, the main structure being kept in these cases as well.…”

“…To each reaction mixture, 2 mL of glacial acetic acid was added, all being kept on a magnetic stirrer, in a water bath under reflux, for 8 h. The resulting precipitate at the end of the reaction time was separated by filtration, washed with distilled water, dried at room temperature and recrystallized from suitable solvents. The general synthesis scheme was developed by adapting some condensation methods of other new compounds with similar structure [ 9 , 10 ].…”

Applications of Perilla frutescens Extracts in Clinical Practice

“…Lately, the need for active compounds derived from various herbs as potent antibacterial agents against a diverse spectrum of microorganisms has increased in order to combat human infection and preserve food [ 106 , 107 ]. The antibacterial efficacy of a polyphenol-rich Perilla frutescens extract against oral Streptococci and Porphyromonas gingivalis was investigated.…”

Bioactive Potential of Carrot-Based Products Enriched with Lactobacillus plantarum

“…The consumption or the enrichment of food products with carrot by-products has a good impact on human health with several benefits such as decreasing blood pressure and the prevention of heart diseases, atherosclerosis, infections, bronchial asthma, and also muscular degeneration. Polyphenolic compounds found in carrot peel have antioxidant, antimutagenic, and antitumor actions, and their dietary fibers prevent heart diseases, constipation, and cancer and control blood sugar levels as therapeutical molecules [ 1 , 18 , 19 ]. Probiotics have been predominantly used in dairy products since dairy products provide a favorable culture medium for probiotic viability [ 20 ].…”