Dapsone-Loaded Invasomes as a Potential Treatment of Acne: Preparation, Characterization, and In Vivo Skin Deposition Assay
AAPS PHARMSCITECH
Authors: El-Nabarawi, Mohamed Ahmed; Shamma, Rehab Nabil; Farouk, Faten; Nasralla, Samar Mohamed
Abstract
Dapsone (DPS) is a unique sulfone with antibiotic and anti-inflammatory activity. Owing to its dual action, DPS has a great potential to treat acne. Topical DPS application is expected to be effective in treatment of mild to moderate acne conditions. Invasomes are novel vesicles composed of phosphatidylcholine, ethanol, and one or mixture of terpenes of enhanced percutaneous permeation. In this study, DPS-loaded invasomes were prepared using the thin film hydration technique. The effect of different terpenes (Limonene, Cineole, Fenchone, and Citral) in different concentrations on the properties of the prepared DPS-loaded invasomes was investigated using a full factorial experimental design, namely, the particle size, drug entrapment, and release efficiency. The optimized formulation was selected for morphological evaluation which showed spherical shaped vesicles. Further solid-state characterization using differential scanning calorimetry and X-ray diffractometry revealed that the drug was dispersed in an amorphous state within the prepared invasomes. Finally, the ability of the prepared DPS-loaded invasomes to deliver DPS through the skin was investigated in vivo using wistar rats. The maximum in vivo skin deposition amount of DPS was found to be 4.11 mcg/cm(2) for invasomes versus 1.71 mcg/cm(2) for the drug alcoholic solution, representing about 2.5-fold higher for the invasomes compared to the drug solution. The AUC0-10 calculated for DPS-loaded invasomes was nearly 2-fold greater than that of DPS solution (14.54 and 8.01 mcg.h/cm(2) for the optimized invasomes and DPS solution, respectively). These results reveal that the skin retention of DPS can be enhanced using invasomes.
Computational Design and Electropolymerization of Molecularly Imprinted Poly(p-Aminobenzoic-Acid-Co-Dapsone) Using Multivariate Optimization for Tetradifon Residue Analysis
CHEMISTRYSELECT
Authors: Rohani, Fatemeh Ganjeizadeh; Mohadesi, Alireza; Ansari, Mehdi
Abstract
In this study, tetradifon as a non-electroactive pesticide was measured by a new gold electrode modified with electropolymerized molecularly imprinted poly(para aminobenzoic acid-co-4,4-diaminodiphenyl sulfone) (P-pABA-co-DDS). The best available monomer was selected based on computational design and then the polymer was developed in optimized condition. Screening of various factors was performed by Plackett-Burman design (PBD) and central composite design (CCD) was utilized to select optimized condition. Under the optimized condition, calibration curve of tetradifon on MIP/gold electrode was constructed with a linear range of 0.05- 2.50 mu M. The limit of detection (LOD) and limit of quantification (LOQ) was found to be 0.014 and 0.047 mu M, respectively. The developed method showed good stability, repeatability, and reproducibility, sensitivity and selectivity for tetradifon. The developed method was applied to determine tetradifon in real water samples.