The interaction between meloxicam and sulfonatocalix[4]naphthalene was investigated to improve the meloxicam solubility and its dissolution performance. Solubility behavior was investigated in distilled water (DW) and at different pH conditions. Besides, solid systems were prepared in a 1:1 molar ratio using coevaporate, kneading, and simple physical mixture techniques. Further, they were characterized by PXRD, FT-IR, DCS, and TGA. In vitro dissolution rate for coevaporate, kneaded, and physical mixture powders were also investigated. Solubility study revealed that meloxicam solubility significantly increased about 23.99 folds at phosphate buffer of pH 7.4 in the presence of sulfonatocalix[4]naphthalene. The solubility phase diagram was classified as AL type, indicating the formation of 1:1 stoichiometric inclusion complex. PXRD, FT-IR, DCS, and TGA pointed out the formation of an inclusion complex between meloxicam and sulfonatocalix[4]naphthalene solid powders prepared using coevaporate technique. In addition, in vitro meloxicam dissolution studies revealed an improvement of the drug dissolution rate. Furthermore, a significantly higher drug release (p ≤ 0.05) and a complete dissolution was achieved during the first 10 min compared with the other solid powders and commercial meloxicam product. The coevaporate product has the highest increasing dissolution fold and RDR10 in the investigated media, with average values ranging from 5.4–65.28 folds and 7.3–90.7, respectively. In conclusion, sulfonatocalix[4]naphthalene is a promising host carrier for enhancing the solubility and dissolution performance of meloxicam with an anticipated enhanced bioavailability and fast action for acute and chronic pain disorders.
The study aims to assess the interaction between fluconazole and sulfonatocalix[4]naphthalene towards enhancing its dissolution performance and antimycotic activity. A solubility study was carried out at different pH conditions, and the results revealed the formation of a 1:1 molar ratio fluconazole-sulfonatocalix[4]naphthalene inclusion complex with an AL type phase solubility diagrams. The solid powder systems of fluconazole-sulfonatocalix[4]naphthalene were prepared using kneaded and co-evaporation techniques and physical mixtures. DCS, PXRD, TGA-DTG, FT-IR, and in vitro dissolution performance characterize the prepared systems. According to physicochemical characterization, the co-evaporation approach produces an amorphous inclusion complex of the drug inside the cavity of sulfonatocalix[4]naphthalene. The co-evaporate product significantly increased the drug dissolution rate up to 93 ± 1.77% within 10 min, unlike other prepared solid powders. The antimycotic activity showed an increase substantially (p ≤ 0.05, t-test) antimycotic activity of fluconazole co-evaporate mixture with sulfonatocalix[4]naphthalene compared with fluconazole alone against clinical strains of Candida albicans and Candida glabrata. In conclusion, sulfonatocalix[4]naphthalene could be considered an efficient complexing agent for fluconazole to enhance its aqueous solubility, dissolution performance, and antimycotic activity.
30 December 2020 in Biomedical and Pharmacology Journal
Urinary calculi are stones (urolithiasis) that can form anywhere in urinary tract outside of the kidneys and mostly composed of calcium oxalate and phosphate, additionally with elevated throughout the last two decades in the world. Chemical composition plays a major part in nephrolithiasis. Therefore, the high concentrations of lithogenic substances in urine enhance the crystallization method in urine tract system. The most kidney stones form from calcium oxalate, the present study was inspected the effect of the crude aqueous extract as well as the fractionated methanol extract (ethyl acetate, isopropanol, acetone and methanol residue) of paronychia argentea on the crystallization of calcium oxalate salts. The effect of aqueous extract and fractionated methanol extract on the size, number, type of calcium oxalate crystals. Paronychia argentea both the crude aqueous and the fractionated extract, especially ethyl acetate fraction have antiurolithic activity via reducing crystal size as well as activate the formation of calcium oxalate dihydrate (COD) crystals out from calcium oxalate monohydrate (COM) with increasing concentration of extract. The shifting of crystallization process to producing calcium oxalate dihydrate (COD) rather than oxalate monohydrate (COM) and the reducing the crystal size and calcium ion concentration, in addition to the diuretic action of extract plays an important role in controlling urolithiasis.