Related Experiment Video
Updated: Nov 7, 2025
10:10
Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
10.5K
Combinations of Piperine with Hydroxypropyl-β-Cyclodextrin as a Multifunctional System.
Anna Stasiłowicz1, Natalia Rosiak1, Ewa Tykarska2
1Department of Pharmacognosy, Faculty of Pharmacy, Poznan University of Medical Sciences, Swiecickiego 4, 60-781 Poznań, Poland.
International Journal of Molecular Sciences
|April 30, 2021
Summary
Piperine
Area of Science:
- Pharmacology
- Drug Delivery
- Biochemistry
Background:
- Piperine, a natural alkaloid, exhibits broad pharmacological effects but suffers from poor solubility and bioavailability.
- Its bioavailability is further influenced by interactions with CYP450 enzymes, amino acid transporters, and P-glycoprotein.
- These limitations hinder the full therapeutic potential of piperine.
Purpose of the Study:
- To enhance the solubility and bioavailability of piperine.
- To investigate the complexation of piperine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD).
- To characterize the physicochemical interactions between piperine and HP-β-CD and assess the impact on piperine's biological activity.
Main Methods:
- Complexation of piperine with HP-β-CD.
- Physicochemical characterization using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), and nuclear magnetic resonance (NMR).
- Assessment of biological activity including antioxidant potential (DPPH assay) and enzyme inhibition (hyaluronidase, acetylcholinesterase, butyrylcholinesterase).
Main Results:
- Complexation with HP-β-CD significantly increased piperine's solubility and permeability across biological membranes, including the blood-brain barrier.
- Characterization studies confirmed physicochemical changes indicative of piperine-HP-β-CD complex formation.
- The enhanced piperine-HP-β-CD system retained significant antioxidant and enzyme inhibitory activities.
Conclusions:
- Complexation with HP-β-CD is an effective strategy to overcome piperine's solubility and bioavailability challenges.
- The piperine-HP-β-CD complex maintains the therapeutic potential of piperine, including its antioxidant and anti-inflammatory properties.
- This approach holds promise for developing improved piperine-based therapeutics for various conditions.
Keywords:
anti-inflammatory and neuroprotective activityhydroxypropyl-β-cyclodextrinpermeabilitypiperinesolubilityMore Related Videos
05:08Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
17.2K
10:53Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
14.2K
Related Concept Videos
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
43
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
43
01:27Bioavailability Enhancement: Drug Permeability Enhancement
50
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
50
01:27Combined Effects of Drugs: Synergism
5.5K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
5.5K
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
327
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
327
01:17Pore Transport and Ion-Pair Transport
857
Pore transport and ion-pair formation are critical mechanisms for the absorption and distribution of drugs in the body.
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
857