Abstract
Clinical use of 4-Allylpyrocatechol (APC), a potential antifungal agent from Piper betle, is limited because of its low water solubility. The current study explores the development of the self-nanoemulsifying drug delivery system (SNEDDS) containing APC (APC-SNEDDS) to enhance APC solubility. Results demonstrated that excipient type and concentration played an important role in the solubility of APC in the obtained SNEEDS. SNEDDS, comprising 20% Miglyol 812N, 30% Maisine 35-1, 40% Kolliphor RH40, and 10% absolute ethanol, provided the highest loading capacity and significantly increased water solubility of APC. Oil-in-water nanoemulsions (NE) with droplet sizes of less than 40 nm and a narrow size distribution were obtained after dispersing this APC-SNEDDS in water. The droplets had a negative zeta potential between −10 and −20 mV. The release kinetics of APC from APC-SNEDDS followed the Higuchi model. The NE containing 1.6 mg APC/mL had effective activity against Candida albicans with dose-dependent killing kinetics and was nontoxic to normal cells. The antifungal potential was similar to that of 1 mg nystatin/mL. These findings suggest that APC-SNEDDS are a useful system to enhance the apparent water solubility of APC and are a promising system for clinical treatment of oral infection caused by C. albicans.
Highlights
Candida albicans is a commensal microbe in the oral cavity of 45–65% of healthy individuals, with a higher prevalence found in children and young adults
The NE obtained from aqueous dilution of APC-self-nanoemulsifying drug delivery system (SNEDDS) having an APC concentration of 1.6 mg APC/mL was used to evaluate the antifungal activity of APC-SNEDDS in comparison to a nystatin suspension (1 mg/mL)
The results indicated that the release behavior of APC from APC-SNEDDS was best fitted to the Higuchi model, suggesting that the drug release is likely to be according to a Fickian diffusion mechanism
Summary
Candida albicans is a commensal microbe in the oral cavity of 45–65% of healthy individuals, with a higher prevalence found in children and young adults. The severity of C. albicans in the oral cavity is associated with wearing removable dentures because the dentures can decrease the flow of saliva and oxygen to the tissue covered by the dentures This leads to a high production of a local acidic and anaerobic environment that favors overgrowth of Pharmaceutics 2021, 13, 167. 4-Allylpyrocatechol (APC), chemical structure as shown, is a major compound of Piper betle, a member of the Piperaceae family, that possesses several pharmacological activities, including anti-inflammatory and antimicrobial activities [6] It has a strong antifungal activity against various Candida species, including C. albicans [7]. Lipid-based drug delivery systems (LbDDS) can improve the apparent solubility, miscibility, and oral bioavailability of many poorly water-soluble drugs [11,12] These systems are generally composed of oils, surfactants, and co-surfactants.
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