Abstract
Fucoxanthin has interesting anticancer activity, but is insoluble in water, hindering its use as a drug. Microencapsulation is used as a technique for improving drug delivery. This study aimed to formulate fucoxanthin-loaded microspheres (F-LM) for anticancer treatment of H1299 cancer cell lines and optimize particle size (PS) and encapsulation efficiency (EE). Using response surface methodology (RSM), a face centered central composite design (FCCCD) was designed with three factors: Polyvinylalcohol (PVA), poly(d,l-lactic-co-glycolic acid) (PLGA), and fucoxanthin concentration. F-LM was produced using a modified double-emulsion solvent evaporation method. The F-LM were characterized for release profile, release kinetics, and degradation pattern. Optimal F-LM PS and EE of 9.18 µm and 33.09%, respectively, with good surface morphology, were achieved from a 0.5% (w/v) PVA, 6.0% (w/v) PLGA, 200 µg/mL fucoxanthin formulation at a homogenization speed of 20,500 rpm. PVA concentration was the most significant factor (p < 0.05) affecting PS. Meanwhile, EE was significantly affected by interaction between the three factors: PVA, PLGA, and fucoxanthin. In vitro release curve showed fucoxanthin had a high burst release (38.3%) at the first hour, followed by a sustained release stage reaching (79.1%) within 2 months. Release kinetics followed a diffusion pattern predominantly controlled by the Higuchi model. Biodegradability studies based on surface morphology changes on the surface of the F-LM, show that morphology changed within the first hour, and F-LM completely degraded within 2 months. RSM under FCCCD design improved the difference between the lowest and highest responses, with good correlation between observed and predicted values for PS and EE of F-LM.
Highlights
Fucoxanthin, a major xanthophylls in brown seaweed, has a unique structure, including a usual allenic bond and 5,6-monoepoxide in its molecule
A face centered central composite design (FCCCD) under response surface methodology (RSM) was used to investigate the optimal conditions of the three significant factors (PVA, PLGA, and fucoxanthin concentration) towards particle size (PS)
The results demonstrated that optimal PS and EE, by double emulsion extraction/evaporation method (9.18 μm and 33.09%), were observed in the runs representing the center point
Summary
Fucoxanthin, a major xanthophylls in brown seaweed, has a unique structure, including a usual allenic bond and 5,6-monoepoxide in its molecule. Health care systems is Japan, Korea, and India use fucoxanthin for many applications, such as anticancer, antiobesity, antidiabetic, to induce cell cycle arrest at G0 /G1 phase in human colon carcinoma cells, antioxidant, and anti-inflammatory applications. This compound can be isolated from varying types of brown seaweed, such as Undaria pinnatifida, Hijkia fusiformis, Sargassum fulvellum, and Laminaria japonica, from Japan, Padina tetrastomatica from India, and Sargassum siliquastrum from Korea, as well as T. turbinata and S. plagyophyllum from the Malaysian Peninsular [2,5,6,7]. Many studies have reported the advantages of formulation in the delivery of insoluble drugs using ME [3,4,5,6]
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