Title:Pharmacodynamic Evaluation of Novel Tetrandrine-loaded Chitosan Microspheres
Volume: 14
Issue: 6
Author(s): Kefang Guo and Jing Cang*
Affiliation:
- Department of Anesthesia, Zhongshan Hospital, Fudan University, Shanghai, China, Address: No. 180, Fenglin Road, Xuhui District, Shanghai,China
Keywords:
Pharmacodynamic, tetrandrine, chitosan, microspheres, pulmonary hypertension.
Abstract: Background: Tetrandrine has good pharmacological effects, especially in the treatment of
pulmonary hypertension. It has the potential to be valuable for clinical applications, however the
poor solubility and the high variability of oral bioavailability greatly limited its development. Our
research group prepared a new type of tetrandrine microspheres by using chitosan. However, it was
lack of pharmacodynamic evaluation and difficult to evaluate if the application of this dosage form
can really meet the target to improve curative effect.
Methods: In this study, we established animal model of rats with hypoxic pulmonary hypertension, and
evaluated acute therapeutic effect by prepared tetrandrine microspheres.
Results: In vivo pharmacodynamic showed that tetrandrine lung targeting microspheres had stronger
and longer effect to reduce pulmonary arterial pressure (mPAP) than aqueous solvent. After apply
tetrandrine lung targeting microspheres on hypoxia rats, no matter the level of dose, mSBP all had no
obvious change.
Conclusion: Thus it indicated that tetrandrine lung targeting microspheres were mainly effective inside
lung, with certain selectivity.