Preparation, characterization and pharmacokinetic evaluation of curcumin loaded solid dispersion and nano-formulation

• Main Authors: Ke-Di Jiang, 江科迪
• Other Authors: Yu-Tse Wu
• Format: Others
• Language: zh-TW
• Published: 2015
• Online Access: http://ndltd.ncl.edu.tw/handle/hbrd4b

碩士 === 高雄醫學大學 === 藥學系碩士班 === 103 === The purpose of this study is to develop curcumin loaded solid dispersion and nano-formulation which could enhanced the aqueous solubility and oral bioavailability of curcumin. We used two materials to prepare solid dispersion formulation in our study. Three formulations in different ratio was curcumin: polyvinylpyrrolidone K30:vitamin E TPGS=10:70:20, 10:75:15, 10:80:10 (w/w/w). The characterization of solid dispersion included solubility, dissolution, measurement of drug content, differential scanning calorimetry, fourier transform infrared spectroscopy. The composition of nanoemulsion was capryol 90 (14%, w/w), cremophor EL (44%, w/w) and 30% (v/v) transcutol P solution (42%, w/w). Nanoemlsion were evaluated for particle size, polydispersity index, percentage transmittance and dissolution.In pharmacokinetics study, we evaluated curcumin loaded solid dispersion oral administration, nanoemulsion oral administration, curcumin oral administration, and curcumin intravenous administration in Sprague-Dawley rats. The results of solid dispersion solubility in polyvinylpyrrolidone K30:vitamin E TPGS=10:70:20, 10:75:15, 10:80:10 (w/w/w) was 827.1 ± 1.0 μg/mL, 729.3 ± 1.4 μg/mL, 526.2 ± 2.2 μg/mL, the drug content ranged from to 8.4-8.9% (w/w). The result of differential scanning calorimetry revealed the amorphous nature of curcumin in solid dispersion. The results of nanoemulsion particle size and polydispersity index were 96.2 ± 32.2 nm and 1.44 ± 0.38, the percentage transmittance ranged from to 90.7-99.6%. In dissolution tests, all curcumin formulations exhibited marked improvement in the dissolution behavior when compared with pure curcumin. In the pharmacokinetics study, after oral gavage administration (solid dispersion, nanoemulsion, pure curcumin) and intravenous administration (pure curcumin), the relative bioavailability of solid dispersion and nanoemulsion were 1000.0 and 3623.1%, the absolute bioavailability of pure curcumin, solid dispersion and nanoemulsion were 0.3, 3.2 and 11.7%. In conclusion, we have developed curcumin loaded solid dispersion and nanoemulsion.They have shown that it could improve its solubility and bioavailability.