Preparation and in vitro quality evaluation of curcumin supersaturated self-nanoemulsion

CHEN Xu-long1 LIANG Xin-li1 DING Hai-bo1 LAI Zhang-ting1 YUAN Qi-li1 LIN Xia1 LIAO Zheng-gen1

(1.Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, China 330004)

【Abstract】In order to improve the supersaturation and maintenance time of drug dispersion in curcumin self-nanoemulsion (CUR-SNEDDS), precipitation inhibitors (PPIs) were introduced to prepare curcumin supersaturated self-emulsion (CUR-SSNEDDS). The composition of CUR-SNEDDS prescriptions was selected through the solubility test, the compatibility of oil phase and surfactant, the investigation of the emulsifying ability of the surfactant and the drawing of the pseudo-ternary phase diagram. Analytic hierarchy process was used in combination with central composite design-response surface method to optimize the prescription. The type and dosage of precipitation inhibitors (PPIs) were selected to maintain the supersaturated concentration and duration of CUR in artificial gastrointestinal fluids. At the same time, polarizing microscope was used to evaluate the crystallization inhibition effect and the quality and in vitro release behavior of CUR-SSNEDDS. The prepared CUR-SSNEDDS prescription was capryol 90-kolliphor RH40-transcutol HP-Soluplus (7.93:66.71:25.36:5), with the drug loading of (65.12 ± 1.25) mg·g−1. CUR-SSNEDDS was transparent yellow, and the nanoemulsion droplets were spherical with uniform distribution. The emulsification time was (21.02 ± 0.13) s, the average particle size was (57.03 ± 0.35) nm, the polydispersity index(PDI) was (0.23 ± 0.01), and the Zeta potential was (−18.10 ± 1.30) mV. CUR-SSNEDDS significantly inhibited the generation and growth of crystals after in vitro dilution. The supersaturation could be maintained above 10 within 2 h, and the dissolution rate and degree of CUR in artificial gastrointestinal fluid were significantly increased. Soluplus could effectively maintain the supersaturated state of CUR and enhance CUR dissolution in vitro.

【Keywords】 curcumin; supersaturated self-nanoemulsion; artificial gastrointestinal fluid; drug loading; supersaturation;

【DOI】

【Funds】 First-class Discipline Project in Jiangxi Province (JXSYLXK-ZHYAO059) Science and Technology Plan Project of the Health and Family Planning Commission of Jiangxi Province (20181140)

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This Article

ISSN:1001-5302

CN: 11-2272/R

Vol 45, No. 15, Pages 3672-3680

August 2020

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Abstract

  • 1 Materials
  • 2 Methods and results
  • 3 Discussion
  • References