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Alpha-mangostin Nanoparticles Prepared by Solvent Displacement Method
W. Limwikrant, N. Suviporn, S. Puangthorn, N. Anantachoke
Alpha-mangostin is one of the main active substances found in various parts of mangosteen. It has many pharmacological effects, e. g. anticancer, antibacterial and antioxidant. However, the low solubility of alpha-mangostin causes low bioavailability leading to low therapeutic effect. Many methods are used to improve the solubility of poorly water soluble drugs such as cyclodextrin complexation and size reduction to micron and nano-size. The main purpose of this study is to prepare nanosuspension containing alpha-mangostin nanoparticles by solvent displacement method in order to improve its bioavailability.
Alpha-mangostin was dissolved in ethanol and stabilizers were dissolved in water. Various stabilizers were used such as poloxamer, polyvinylpyrrolidone (PVP) and polyvinyl caprolactam – polyvinyl acetate – polyethylene glycol graft copolymer (Soluplus®). Both aqueous and ethanolic solution were mixed at different drug: stabilizer ratios (1:2, 1:5 and 1:10) while continuous stirring using magnetic stirrer. Then ethanol was evaporated and the nanosuspension was obtained. Particle size, size distribution and zeta potential of prepared nanosuspension were measured. The appropriate stabilizers were chosen and then the nanosuspension was prepared using the spinning disk reactor. The stability of nanosuspension was evaluated after storage at 30°C for 56 days.
In the preliminary study, nanosuspension was prepared using magnetic stirrer. Among the stabilizers, using poloxamer407 and Soluplus® gave the smaller particles of alpha-mangostin in the nano-size range with the narrow size distribution than using PVP. Alpha-mangostin nanosuspension was then prepared by spinning disk reactor. The concentration of alpha-mangostin and stabilizers used were 0.4% w/v and 1% w/v, respectively. When Soluplus® was used, alpha-mangostin nanosuspension contained particle size in the range of 87.69-170.80 nm with the polydispersity index (PDI) 0.02-0.16 and zeta potential (-0.86)-(-4.10) mV. While poloxamer407 was used, the nanosuspension had smaller particle size in the range of 30.09-35.25 nm with PDI 0.14-0.36 and zeta potential (-7.49)-(-13.90) mV. In addition, particle size of both alpha-mangostin nanosuspensions was still stable after storage at 30°C for almost two months.
In this study, appropriate stabilizers for preparing alpha-mangostin nanosuspension were poloxamer407 and Soluplus®. Stable nanosuspension containing alpha-mangostin nanoparticles with the narrow size distribution could be prepared by solvent displacement method.
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