Spray-dried nanoemulsion for improved oral delivery of silymarin against hepatic cancer cells
silymarin against hepatic cancer cell
Abstract
Silymarin recognized for numerous activities, but the use is limited due to poor aqueous solubility, inefficient intestinal permeability, and low-erratic bioavailability. The aim of the current research was formulation of spray-dried nanoemulsion to enhance the solubility of silymarin. The nanoemulsion was prepared by aqueous titration method, spray died and characterized for thermal analysis by diffraction scanning calorimetry, crystallography analysis by x-ray diffraction, surface morphology by scanning electron microscopy. The reconstitution properties were determining for droplet size, polydispersity index and microscopic structure. Optimized nanoemulsion composed of 15% v/v of oil, 33% v/v of Smix and 52% v/v of distilled water demonstrated lowest droplet size (52.4 ± 1.63 nm) and polydispersity index (0.112), optimum viscosity (23.37 ± 2.36 cps), maximum % transmittance (94.55), optimum cloud point (88°C) and cumulative % drug release (98.43%). The microscopic structure of spray-dried nanoemulsion after reconstitution in distilled water revealed spherical shape free from any aggregation. Spray-dried nanoemulsion demonstrated amorphous sate of silymarin after fabrication into solid state. The cumulative % release of silymarin was significantly higher than marketed conventional suspension (Limarin). The developed spray-dried nanoemulsion was robust and stable for a period of 3 months that could be recommended for oral administration of silymarin after further study. Solids are preferred over liquid dosage form; the formulation may offer better patient compliance over liquid nanoemulsion. In addition, the in-vitro cytotoxicity study revealed more cytotoxicity of SD-NE than plain silymarin against HepG2 cell line after 48 h of incubation. Moreover, the HepG2 cellular uptake silymarin was found to be substantially higher from NE when compared to the plain silymarin. Further, silymarin loaded SD-NE could be potential approach against hepatic cancer.
Keywords: Silymarin, spray-dried nanoemulsion, dextran, phase diagram, solubility, stability
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