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Improving Physicochemical Stability of Quercetin-Loaded Hollow Zein Particles with Chitosan/Pectin Complex Coating.

ABSTRACT: Hollow nanoparticles are preferred over solid ones for their high loading capabilities, sustained release and low density. Hollow zein particles are susceptible to aggregation with a slight variation in the ionic strength, pH and temperature of the medium. This study was aimed to fabricate quercetin-loaded hollow zein particles with chitosan and pectin coating to improve their physicochemical stability. Quercetin as a model flavonoid had a loading efficiency and capacity of about 86-94% and 2.22-5.89%, respectively. Infrared and X-ray diffraction investigations revealed the interaction of quercetin with zein and the change in its physical state from crystalline to amorphous upon incorporation in the composite particles. The chitosan/pectin coating improved the stability of quercetin-loaded hollow zein particles against heat treatment, sodium chloride and in a wide range of pH. The complex coating protected quercetin that was encapsulated in hollow zein particles from free radicals in the aqueous medium and enhanced its DPPH radical scavenging ability. The entrapment of quercetin in the particles improved its storage and photochemical stability. The storage stability of entrapped quercetin was enhanced both at 25 and 45 °C in hollow zein particles coated with chitosan and pectin. Therefore, composite hollow zein particles fabricated with a combination of polysaccharides can expand their role in the encapsulation, protection and delivery of bioactive components.

SUBMITTER: Khan MA

PROVIDER: S-EPMC8470427 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description: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.

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Improving Physicochemical Stability of Quercetin-Loaded Hollow Zein Particles with Chitosan/Pectin Complex Coating.

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