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已发表论文
和厚朴酚纳米粒的制备（液体反溶剂沉淀法）、表征、药代动力学研究及其对 HepG2 细胞抑制作用的评价
Authors Wu W, Wang L, Wang L, Zu Y, Wang S, Liu P, Zhao X
Received 27 June 2018
Accepted for publication 24 July 2018
Published 17 September 2018 Volume 2018:13 Pages 5469—5483
DOI https://doi.org/10.2147/IJN.S178416
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Thiruganesh Ramasamy
Peer reviewer comments 2
Editor who approved publication: Dr Linlin Sun
Background: Honokiol is a
bioactive lignanoid and has been utilized in traditional Chinese medicine for a
long time. It exhibits several pharmacological properties, such as anticancer
effects, anti-inflammatory effects, and antianxiety effects. However, the poor
aqueous solubility of honokiol has impeded clinical applications.
Materials and methods: In the present study, we adopted the liquid antisolvent precipitation (LAP) technique to prepare nanoparticles of honokiol for enhancement of solubility and bioavailability. Moreover, the honokiol nanoparticles obtained were investigated and evaluated in terms of morphology, physicochemical properties, saturation solubility, dissolution in vitro, bioavailability in vivo, toxicity, and the inhibitory effect on growth of HepG2 cells.
Results: The obtained honokiol nanoparticles existed nearly in spherical shape and could be turned into amorphous structure by the LAP method. Moreover, the solubility of the honokiol nanoparticles was extremely higher than that of free honokiol, and the nanoparticle dissolution rate was also higher than that of free honokiol, which was about 20.41 times and 26.2 times than that of free honokiol in artificial gastric juice and in artificial intestinal juice. The area under the curve [AUC(0–t)] value of honokiol nanoparticles was about 6.52 times greater than that of free honokiol; therefore, the honokiol nanoparticles had a higher bioavailability than free honokiol but were innoxious to the organs of rats. Additionally, the honokiol nanoparticles exhibited a higher inhibition of HepG2 cells due to their lower IC50 compared to free honokiol.
Conclusion: Honokiol nanoparticles have high solubility and bioavailability, and can become a new oral drug formulation and produce a better response for its clinical applications.
Keywords: honokiol, honokiol nanoparticles, solubility, bioavailability
Materials and methods: In the present study, we adopted the liquid antisolvent precipitation (LAP) technique to prepare nanoparticles of honokiol for enhancement of solubility and bioavailability. Moreover, the honokiol nanoparticles obtained were investigated and evaluated in terms of morphology, physicochemical properties, saturation solubility, dissolution in vitro, bioavailability in vivo, toxicity, and the inhibitory effect on growth of HepG2 cells.
Results: The obtained honokiol nanoparticles existed nearly in spherical shape and could be turned into amorphous structure by the LAP method. Moreover, the solubility of the honokiol nanoparticles was extremely higher than that of free honokiol, and the nanoparticle dissolution rate was also higher than that of free honokiol, which was about 20.41 times and 26.2 times than that of free honokiol in artificial gastric juice and in artificial intestinal juice. The area under the curve [AUC(0–t)] value of honokiol nanoparticles was about 6.52 times greater than that of free honokiol; therefore, the honokiol nanoparticles had a higher bioavailability than free honokiol but were innoxious to the organs of rats. Additionally, the honokiol nanoparticles exhibited a higher inhibition of HepG2 cells due to their lower IC50 compared to free honokiol.
Conclusion: Honokiol nanoparticles have high solubility and bioavailability, and can become a new oral drug formulation and produce a better response for its clinical applications.
Keywords: honokiol, honokiol nanoparticles, solubility, bioavailability
