Related Experiment Video
Updated: Aug 14, 2025
08:44
Assembly and Characterization of Polyelectrolyte Complex Micelles
Published on: March 2, 2020
10.9K
Amphotericin B and monoacyl-phosphatidylcholine form a stable amorphous complex
Xiaona Liu1, Ragna Berthelsen1, Daniel Bar-Shalom1
1Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
International Journal of Pharmaceutics
|January 12, 2023
Summary
Developing an oral Amphotericin B (AmB) formulation is crucial. This study created an amorphous Amphotericin B-monoacyl-phosphatidylcholine complex (APC) that significantly enhances AmB
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Amphotericin B (AmB) is a critical antifungal and antileishmanial agent.
- Current parenteral AmB formulations are associated with severe infusion-related toxicities and nephrotoxicity.
- Oral AmB delivery is highly desirable to improve patient compliance and reduce side effects, but is hindered by poor solubility and permeability.
Purpose of the Study:
- To develop a novel oral formulation of Amphotericin B (AmB).
- To enhance the dissolution rate and aqueous solubility of AmB for oral administration.
- To investigate the complexation of AmB with monoacyl-phosphatidylcholine (MAPC) for improved drug delivery.
Main Methods:
- Complexation of AmB with MAPC to form an AmB-MAPC complex (APC).
- Characterization of APC using X-ray powder diffraction, Fourier-transform infrared spectroscopy, dynamic light scattering, cryogenic transmission electron microscopy, and small-angle neutron scattering.
- Evaluation of APC's dissolution rate and solubility in simulated intestinal fluid.
Main Results:
- AmB was successfully converted to an amorphous form within the APC.
- APC formed colloidal micellar structures upon aqueous dispersion, indicating successful integration of AmB.
- APC demonstrated significantly increased dissolution rate and apparent aqueous solubility compared to crystalline AmB and physical mixtures.
Conclusions:
- The developed AmB-MAPC complex (APC) exhibits amorphous properties and enhanced solubility.
- APC represents a promising strategy for enabling the oral delivery of Amphotericin B.
- This approach could lead to safer and more convenient AmB treatments for invasive fungal infections and leishmaniasis.
Related Concept Videos
01:19Complexation Equilibria: The Chelate Effect
590
In complexation reactions, metal atoms or cations interact with ligands to form donor-acceptor adducts called metal complexes. Ligands that bind through one donor site are monodentate, ligands with two donor sites are bidentate, and those with more than two donor sites are polydentate ligands. For example, ethylene diamine is a bidentate ligand that binds through two nitrogen donor atoms, forming a five-membered ring. EDTA is a polydentate ligand that binds through four oxygen and two nitrogen...
590
01:35Asymmetric Lipid Bilayer
7.4K
Biological membranes show uneven distribution of different types of lipids in the inner and outer layers, resulting in transverse asymmetric membranes. The treatment of the erythrocyte membrane with the enzyme phospholipase confirmed the asymmetric nature of the lipid bilayer. The enzyme hydrolyzes lipids into fatty acids and hydrophilic groups. The phospholipase acts only on the outer layer of the membrane, while the inner layer remains intact. The phospholipase treatment resulted in 80%...
7.4K
01:34The Fluid Mosaic Model
149.6K
The fluid mosaic model was first proposed as a visual representation of research observations. The model comprises the composition and dynamics of membranes and serves as a foundation for future membrane-related studies. The model depicts the structure of the plasma membrane with a variety of components, which include phospholipids, proteins, and carbohydrates. These integral molecules are loosely bound, defining the cell’s border and providing fluidity for optimal function.
149.6K
01:19Fluid Mosaic Model
12.2K
Scientists identified the plasma membrane in the 1890s and its principal chemical components (lipids and proteins) by 1915. The model for plasma membrane structure, proposed in 1935 by Hugh Davson and James Danielli, was the first model to be widely accepted in the scientific community. The model was based on the plasma membrane's "railroad track" appearance in early electron micrographs. Davson and Danielli theorized that the plasma membrane's structure resembled a sandwich...
12.2K
03:45Formation of Complex Ions
23.9K
A type of Lewis acid-base chemistry involves the formation of a complex ion (or a coordination complex) comprising a central atom, typically a transition metal cation, surrounded by ions or molecules called ligands. These ligands can be neutral molecules like H2O or NH3, or ions such as CN− or OH−. Often, the ligands act as Lewis bases, donating a pair of electrons to the central atom. These types of Lewis acid-base reactions are examples of a broad subdiscipline called coordination...
23.9K
01:17Pore Transport and Ion-Pair Transport
553
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...
553