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Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
Structural properties induced by the composition of biocompatible phospholipid-based microemulsion and amphotericin B
Cristina Maria Franzini1, Kelly Christina Pestana, Eduardo Ferreira Molina
1Universidade Estadual Paulista, UNESP, Faculdade de Ciências Farmacêuticas, Programa de Pós-graduação em Ciências Farmacêuticas, Rodovia Araraquara-Jaú km 01, 14801-902, Araraquara, SP, Brazil.
Abstract:
Anionic microemulsions (MEs) containing soya phosphatidylcholine, Tween-20, sodium oleate as surfactant, and cholesterol as oil phase were investigated as drug carriers for amphotericin B. Depending on the composition of the microemulsion, various structures, which differently interact with amphotericin B, can be formed. The nanostructured systems were characterized by photon correlation spectroscopy, rheological behavior, and polarized light microscopy. The results reveal that the droplet diameters increased with amphotericin B incorporation for all ranges of surfactant and oil phase. For both amphotericin B-unloaded and amphotericin B-loaded microemulsions, the profile of the oil droplet diameter decreased with increasing the surfactant concentration, demonstrating the stabilizing effect of the surfactant. The increase in the oil phase proportions led to the growth of the droplet diameter, clearly demonstrating the limit of the surfactant organization in the oil-water interface. The amphotericim B incorporation into microemulsion increased with the fraction volume of the oil phase and the surfactant concentration reaching a plateau at high contents. This profile could be quantitatively analyzed by the framework of the pseudo-phase model that considers the amphotericim B distribution between the oil and the aqueous phases. The rheological analysis showed a pseudoplastic behavior with little thixotropic characteristic. Under polarized light, the system of interest showed a dark background characteristic of dispersed droplets. However, for both amphotericim B-loaded and amphotericim B unloaded microemulsions, the increase in the O/S ratio led to the formation of ordered structures with lamellar arrangements.
Insights
Anionic microemulsions (MEs) effectively carry amphotericin B, with droplet size influenced by surfactant and oil content. Formulation composition dictates drug loading and system structure for optimized drug delivery.
Area of Science:
- Colloid and Surface Chemistry
- Pharmaceutical Nanotechnology
- Drug Delivery Systems
Background:
- Anionic microemulsions (MEs) are explored as potential nanocarriers for drug delivery.
- The interaction between drug molecules and ME components influences carrier performance.
- Amphotericin B is an antifungal agent often requiring effective delivery systems.
Purpose of the Study:
- To investigate anionic microemulsions (MEs) formulated with soya phosphatidylcholine, Tween-20, and sodium oleate as drug carriers for amphotericin B.
- To characterize the structural and physicochemical properties of these MEs.
- To understand the influence of ME composition on amphotericin B incorporation and system behavior.
Main Methods:
- Microemulsion formulation using soya phosphatidylcholine, Tween-20, sodium oleate, and cholesterol.
- Characterization techniques including photon correlation spectroscopy, rheological behavior analysis, and polarized light microscopy.
- Investigation of amphotericin B incorporation and its dependence on microemulsion composition.
Main Results:
- Droplet diameters increased with amphotericin B incorporation.
- Surfactant concentration stabilized droplets, while increased oil phase led to larger droplet diameters.
- Amphotericin B incorporation increased with oil phase and surfactant concentration, reaching a plateau.
- Rheological analysis indicated pseudoplastic behavior with slight thixotropy.
- Increased oil-to-surfactant ratio induced lamellar arrangements in microemulsions.
Conclusions:
- Anionic microemulsions are viable carriers for amphotericin B, with tunable properties based on formulation.
- The pseudo-phase model effectively describes amphotericin B distribution within the microemulsion system.
- Formulation composition significantly impacts microemulsion structure and drug loading capacity.
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