Development of Self-Nanoemulsifying Drug Delivery Systems Containing 4-Allylpyrocatechol for Treatment of Oral Infections Caused by Candida albicans

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.

Formulation and Evaluation of SNEDDS Loaded with Original Lipophenol for the Oral Route to Prevent Dry AMD and Stragardt’s Disease

“…NE with a zeta potential value of ±30 mV was considered to be stable when diluted in aqueous media, due to electrostatic repulsion between the NE, which limits coalescence [ 46 ]. We supposed that the negative charge of NE was probably due to the ionization of free fatty acids of labrasol [ 47 ] and the increase of this negative charge of NE-IP-DHA compared to empty NE was probably due to the ionization of the phenolic OH- group from IP-DHA [ 10 ]. This could be an indicator of the localization of IP-DHA at the O/W interface, suggesting that IP-DHA was not fully encapsulated inside NE, but adsorbed at the interface or surface.…”

“…Lipid-based drug delivery systems (LBDDS) can improve the solubility and the oral bioavailability of poorly water-soluble drugs [ 9 , 10 ]. These systems are composed of oils, surfactants, and co-surfactants, and according to the excipients selected and their ratio, LBDDS can be characterized into four types (I, II, IIIA, IIIB, and IV), each presenting with its advantages and disadvantages [ 11 ].…”

Optimization and Characterization of Self Nano Emulsifying Drug Delivery System loaded with 18- β Glycerrhetinic acid

“…FF formulation having n-value (diffusion exponent) 0.733, which indicates anomalous non-fickian diffusion, n-value also indicates that the geometry of swellable controlled release system is spherical [31].…”

The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABAA Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform

“…AGO is immiscible with water and it requires a potential system for water-miscible enhancement. Nanoemulsion is one of the promising delivery systems that can improve the aqueous solubility of many hydrophobic active compounds [ 15 , 16 , 17 ]. Several nanoemulsions of water-insoluble compounds have been developed for these applications [ 18 , 19 , 20 , 21 ].…”