Abstract
The extract of Cardiospermum halicacabum L. (C. halicacabum) obtained from flower, leaf and vine was loaded into modified phospholipid vesicles aiming at obtaining sprayable, biocompatible and effective nasal spray formulations for the treatment of nasopharyngeal diseases. Penetration enhancer-containing vesicles (PEVs) and hyalurosomes were formulated, and stabilized by adding a commercial gelatin from fish (20 mg/mL) or chondroitin sulfate from catshark cartilages (Scyliorhinus canicula, 20 mg/mL). Cryo-TEM images confirmed the formation of spherical vesicles, while photon correlation spectroscopy analysis disclosed the formation of small and negatively-charged vesicles. PEVs were the smaller vesicles (~100 nm) along with gelatin-hyalurosomes (~120 nm), while chondroitin-PEVs and chondroitin-hyalurosomes were larger (~160 nm). Dispersions prepared with chondroitin sulfate were more homogeneous, as the polydispersity index was ~0.15. The in vitro analysis of the droplet size distribution, average velocity module and spray cone angle suggested a good spray-ability and deposition of formulations in the nasal cavity, as the mean diameter of the droplets was in the range recommended by the Food and Drug Administration for nasal targets. The spray plume analysis confirmed the ability of PEVs, gelatin-PEVs, hyalurosomes and gelatin-hyalurosomes to be atomized in fine droplets homogenously distributed in a full cone plume, with an angle ranging from 25 to 30°. Moreover, vesicles were highly biocompatible and capable of protecting the epithelial cells against oxidative damage, thus preventing the inflammatory state.
Highlights
Cardiospermum halicacabum L. (C. halicacabum) belongs to the Sapindaceae family, which includes about 1200 species commonly found in India, South America and Africa
The actual formation, structure and morphology of C. halicacabum extract-loaded vesicles were evaluated by means of cryo-TEM observation
The actual formation, structure and morphology of C. halicacabum extract-loaded6 vofe1s8icles were evaluated by means of cryo-TEM observation
Summary
Cardiospermum halicacabum L. (C. halicacabum) belongs to the Sapindaceae family, which includes about 1200 species commonly found in India, South America and Africa. (C. halicacabum) belongs to the Sapindaceae family, which includes about 1200 species commonly found in India, South America and Africa. The extract of C. halicacabum is still used in traditional eastern medicine as an anti-inflammatory remedy against rhinopharyngitis, but the effect has never been evaluated in scientific studies. The main bioactives contained in the plant are flavonoids, triterpenoids, glycosides, fatty acids and volatile esters [11]. They synergically exert anti-inflammatory effects, reducing the activity of phospholipases A2, with a consequent reduction of the availability of arachidonic acid, a precursor of prostaglandin biosynthesis [12]. C. halicacabum counteracts free radicals, due to its content of powerful antioxidants including flavonoids, saponins, tannins, and glycosides [4,14]
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