Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2026
Solid nano-lipoidal intelligent premix (SNIP): designing, optimization, and characterization.
СтатьяНазвание и аннотация: Перевод в очереди
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Rana Hardik, Patel Noopur, Thakkar Vaishali, Gandhi Tejal
Аннотация
BACKGROUND: Bicalutamide possesses very low oral bioavailability due to its low water solubility and p-gp efflux. The present invention aimed to improve the solubility and availability of Bicalutamide at the absorption site using Epigallocatechin-3-gallate (EGCG) and to design a patient- and industry-friendly solid nanolipoidal intelligent premix (SNIP). Exploring natural excipients is another aim.
METHODS: Various oils, surfactants, and cosurfactants were employed to investigate the Bicalutamide solubility. EGCG was used as a p-gp substrate to improve the absorption of Bicalutamide. An optimum proportion was defined through a pseudo-ternary phase diagram. The influence of the Soluplus as a precipitation inhibitor was assessed. Significant variables were screened using a qualitative risk assessment to design a self-nano-emulsifying drug delivery system. The influence of significant variables, such as amounts of sunflower oil, Tween 20, and Span 80, was identified using a D-optimal mixture design. SNEDDs were characterized using morphological and chemical tests. Optimal SNEDDs were adsorbed to form SNIP and characterized.
RESULTS: Sunflower oil, T20, and S80 were scrutinized as oil, surfactant, and co-surfactant based on Bicalutamide solubility. Soluplus was identified as effective at a 5% concentration as a parachute. A 1:3 proportion of Sunflower oil, Tween 20, and Span 80 was chosen from a pseudo-ternary diagram. The optimal SNEDDs have Sunflower oil (0.11mL), Tween 20 (0.14mL), and Span 80 (0.74mL), which showed immediate emulsification (13 s), nano, uniform globule size (254.4 nm and PDI < 0.5), and higher stability (-21.3 mV to -21.3 mV zeta potential). XRD, FTIR, DSC, and in-vitro dissolution revealed the amorphous nature and higher solubility of SNIP. The ex vivo method confirmed the effect of EGCG, showing higher absorption (96.75 ± 1.23%) at 2.5 min. Better thermodynamic stability was observed for optimal SNIP.
CONCLUSION: Sunflower oil was explored as a natural oil in designing SNIP. SNIP design was significantly affected by the formulation variables. SNIP showed higher dissolution and solubility compared to pure Bicalutamide. EGCG was effective in improving the availability of Bicalutamide at the absorption site. SNIP may undergo lymphatic absorption, bypassing first-pass metabolism. The designed SNIP was novel, industrial-friendly, and patient-convenient.
METHODS: Various oils, surfactants, and cosurfactants were employed to investigate the Bicalutamide solubility. EGCG was used as a p-gp substrate to improve the absorption of Bicalutamide. An optimum proportion was defined through a pseudo-ternary phase diagram. The influence of the Soluplus as a precipitation inhibitor was assessed. Significant variables were screened using a qualitative risk assessment to design a self-nano-emulsifying drug delivery system. The influence of significant variables, such as amounts of sunflower oil, Tween 20, and Span 80, was identified using a D-optimal mixture design. SNEDDs were characterized using morphological and chemical tests. Optimal SNEDDs were adsorbed to form SNIP and characterized.
RESULTS: Sunflower oil, T20, and S80 were scrutinized as oil, surfactant, and co-surfactant based on Bicalutamide solubility. Soluplus was identified as effective at a 5% concentration as a parachute. A 1:3 proportion of Sunflower oil, Tween 20, and Span 80 was chosen from a pseudo-ternary diagram. The optimal SNEDDs have Sunflower oil (0.11mL), Tween 20 (0.14mL), and Span 80 (0.74mL), which showed immediate emulsification (13 s), nano, uniform globule size (254.4 nm and PDI < 0.5), and higher stability (-21.3 mV to -21.3 mV zeta potential). XRD, FTIR, DSC, and in-vitro dissolution revealed the amorphous nature and higher solubility of SNIP. The ex vivo method confirmed the effect of EGCG, showing higher absorption (96.75 ± 1.23%) at 2.5 min. Better thermodynamic stability was observed for optimal SNIP.
CONCLUSION: Sunflower oil was explored as a natural oil in designing SNIP. SNIP design was significantly affected by the formulation variables. SNIP showed higher dissolution and solubility compared to pure Bicalutamide. EGCG was effective in improving the availability of Bicalutamide at the absorption site. SNIP may undergo lymphatic absorption, bypassing first-pass metabolism. The designed SNIP was novel, industrial-friendly, and patient-convenient.