Abstract
Biphasic oil/water nanoemulsions have been proposed as delivery systems for the intranasal administration of curcumin (CUR) and quercetin (QU), due to their high drug entrapment efficiency, the possibility of simultaneous drug administration and protection of the encapsulated compounds from degradation. To better understand the physicochemical and biological performance of the selected formulation simultaneously co-encapsulating CUR and QU, a stability test of the compound mixture was firstly carried out using X-ray powder diffraction and thermal analyses, such as differential scanning calorimetry (DSC) and thermogravimetric analyses (TGA). The determination and quantification of the encapsulated active compounds were then carried out being an essential parameter for the development of innovative nanomedicines. Thus, a new HPLC–UV/Vis method for the simultaneous determination of CUR and QU in the nanoemulsions was developed and validated. The X-ray diffraction analyses demonstrated that no interaction between the mixture of active ingredients, if any, is strong enough to take place in the solid state. Moreover, the thermal analysis demonstrated that the CUR and QU are stable in the nanoemulsion production temperature range. The proposed analytical method for the simultaneous quantification of the two actives was selective and linear for both compounds in the range of 0.5–12.5 µg/mL (R2 > 0.9997), precise (RSD below 3%), robust and accurate (recovery 100 ± 5 %). The method was validated in accordance with ICH Q2 R1 “Validation of Analytical Procedures” and CDER-FDA “Validation of chromatographic methods” guideline. Furthermore, the low limit of detection (LOD 0.005 µg/mL for CUR and 0.14 µg/mL for QU) and the low limit of quantification (LOQ 0.017 µg/mL for CUR and 0.48 µg/mL for QU) of the method were suitable for the application to drug release and permeation studies planned for the development of the nanoemulsions. The method was then applied for the determination of nanoemulsions CUR and QU encapsulation efficiencies (> 99%), as well as for the stability studies of the two compounds in simulated biological fluids over time. The proposed method represents, to our knowledge, the only method for the simultaneous quantification of CUR and QU in nanoemulsions.
Highlights
Quercetin (QU) and curcumin (CUR) are natural compounds that present interesting properties for the therapy of several diseases
The endothermic peak observed in the CUR differential scanning calorimetry (DSC) curve corresponds to the melting point of CUR, and the shoulder that is observed in the DSC curve from 200 ◦C in the CUR curve corresponds to the beginning of the decomposition of this compound, as seen in the thermogravimetric analyses (TGA) curve
The study of formulation using different techniques such as TGA, DSC, and PXRD was essential to examine the existence of possible interactions between these two compounds (CUR and QU)
Summary
Quercetin (QU) and curcumin (CUR) are natural compounds that present interesting properties for the therapy of several diseases. Despite the absorption by passive diffusion of QU across the intestine, the overall bioavailability of this compound is low and significantly variable among individuals [5]. CUR is a hydrophobic polyphenol derived from the rhizome of Curcuma longa that presents several medicinal properties similar to QU, such as anti-inflammatory, anti-oxidant, and anti-neurodegenerative effects [6,7]. The poor absorption from the gastrointestinal tract of CUR, its rapid metabolism in the liver and in the intestinal wall, and its limited blood brain barrier permeability are considered the main limitations to the therapeutic use of this compound in neurodegenerative disorders [10]
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