No abstract

Moreover, the microbiological activity was enhanced by around 23.3%, demonstrating that the complex formed could represent an efficient drug delivery system.

The aim of this study was to develop and validate a simple liquid-chromatography method, with good accuracy, reproducibility and sensitivity, for the quantification of norfloxacin in β-cyclodextrin inclusion complexes. In the method validation, the parameters evaluated were linearity, limits of detection and quantification, specificity, accuracy, precision and robustness. The stability-indication property of the method was evaluated through studies on the degradation under stress conditions. A method employing a simple mobile phase consisting of phosphate buffer (pH 3.0) and acetonitrile (86:14 v/v) was developed. Fluorescence detection was employed to minimize the influence of degradation products, due to its high sensitivity, selectivity and specificity. The method was specific, linear in the concentration range of 1 -30 μg/mL, robust, precise and accurate. The proposed method was successfully applied in the determination of norfloxacin in inclusion complexes, thus aiding quality-control analysis in the future development of drug delivery systems.

Hydrochlorothiazide (HCTZ) is a class IV drug according to the Biopharmaceutical Classification System. This study aimed the development of self-nanoemulsifying drug delivery system (SNEDDS) for HCTZ as an approach to overcome the biopharmaceutical limitations. Pre-formulation screening and ternary phase diagrams were carried out to select the oil phase, the surfactant, and the co-surfactant as the amount of each constituent. The optimized formulations, with reduced amount of surfactant, and composed of medium chain triglycerides, Cremophor EL and Transcutol P did not affect the pH or show drug incompatibilities. The SNEDDS were stabilized by the nanoscale globules and high negative zeta potential. All the physicochemical characterization assays were performed in biorelevant media to better predict the in vivo performance. The enhanced dissolution rate of the SNEDDS reflected in the in vivo diuretic activity, presenting a natriuresis, kaliuresis, and chloriuresis at early stages and an increased volume of total urine compared with HCTZ alone. The designed SNEDDS produced an improvement in the pharmacodynamics due to high dissolution and probable inhibition of intestinal efflux protein by Cremophor EL. The use of SNEDDS demonstrated to be an efficient approach to modulate the absorption of HCTZ and drug therapeutics.

The satisfactory stability indicates that the NFX/β-cyclodextrin complexes could be useful as an alternative to the existing NFX drug formulation.