preparation and in vitro quality evaluation of self microemulsion co loaded with tenuifolin and β asarone

• DOI: 10.19540/j.cnki.cjcmm.20200922.301
• Publication Date: 2020-12-01
• Authors: Jing Wang; Jun-Jun Zhu; Bao-de Shen; Hai-Long Yuan; Ting Zhang; Li-Qiang Wang
• Keywords: Surface-Active Agents; Drug Delivery Systems; Solubility; Biological Availability; Allylbenzene Derivatives; Emulsions; Anisoles; Particle Size; Diterpenes, Kaurane

To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.