Optimized piperine-phospholipid complex with enhanced bioavailability and hepatoprotective activity.
Sayan Biswas1, Pulok K Mukherjee1,2, Amit Kar1
1School of Natural Product Studies, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Pharmaceutical Development and Technology
|October 16, 2020
Summary
Piperine phospholipid complex (PPC) enhances piperine
Area of Science:
- Pharmacology
- Natural Products
- Drug Delivery
Background:
- Piperine (PIP) from Piper species offers therapeutic benefits, notably hepatoprotection.
- Low oral bioavailability limits piperine's therapeutic potential.
- Developing effective delivery systems is crucial for piperine's clinical application.
Purpose of the Study:
- To optimize and characterize a piperine-phospholipid complex (PPC) for improved piperine delivery.
- To investigate the pharmacokinetic profile of PPC in an animal model.
- To evaluate the enhanced hepatoprotective effects of PPC.
Main Methods:
- Piperine-phospholipid complex (PPC) preparation optimized using response surface methodology.
- Comprehensive characterization of PPC using FT-IR, DTA, PXRD, SEM, and molecular docking.
- Assessment of solubility, log P, dissolution efficiency, and in vivo pharmacokinetics in rats.
Main Results:
- PPC demonstrated significantly enhanced hepatoprotective activity compared to pure piperine.
- PPC administration normalized serum markers and antioxidant enzyme levels.
- Piperine bioavailability increased 10.40-fold with PPC, and elimination half-life extended from 0.477 to 9.80 hours.
Conclusions:
- Piperine-phospholipid complex (PPC) significantly improves piperine's bioavailability and pharmacokinetic profile.
- Enhanced delivery of piperine via PPC potentiates its hepatoprotective efficacy.
- PPC represents a promising strategy for overcoming piperine's bioavailability limitations.
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