Related Experiment Video
Updated: Jun 29, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
One Platform Comparison of Polymeric and Lipidic Nanoparticles for the Delivery of Amphotericin B
Nandha Joyson1, Anchal Pathak1, Keerti Jain2
1Drug Delivery and Nanomedicine Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER) - Raebareli, Lucknow, Uttar Pradesh, 226002, India.
Abstract:
Amphotericin B (AmB) is a membrane-acting antibiotic used for the treatment of fungal and protozoal infections. AmB exists in various molecular forms, i.e., monomeric, super-aggregated, and oligomeric forms, where oligomeric forms are highly toxic because of their relative affinity toward cholesterol present over human cell membrane. Hence, the objective of our research work was to study the aggregation state of AmB in two different nanoformulations, i.e., solid lipid nanoparticles (SLNs) and zein-based nanoparticles (PNPs), with the aim of enhancing the fraction of less toxic form of AmB, and a comparative study was performed. The zein and glyceryl monostearate can intercalate the polyenic domain of AmB and thereby hinder the hydrophobic attractions between the AmB molecules, which allows their existence in monomeric forms. The particle size of AmB-SLNs and AmB-PNPs were 378.90 ± 9.50 nm and 184.90 ± 6.00 nm, while zeta potential was -34.97 ± 0.51 mV and +28.93 ± 2.29 mV, respectively. In vitro release studies showed more controlled release of AmB from PNPs (52.48 ± 1.07%) as compared to SLNs (86.33 ± 0.93%). The predominant aggregation state of AmB in both formulations was determined by UV-visible and circular dichroism spectrophotometry, where a higher degree of monomerization of AmB was reported in AmB-SLNs as compared to AmB-PNPs. Toxicity of the nanoformulations was evaluated through hemolysis test, where the results suggested that AmB-SLNs and AmB-PNPs were less hemolytic as compared to pure AmB. The nanoformulations demonstrated the predominant monomeric form of AmB, which may offer higher selectivity index toward microbial membrane.
Insights
Researchers developed novel nanoformulations of Amphotericin B (AmB) to reduce its toxicity. Solid lipid nanoparticles (SLNs) and zein-based nanoparticles (PNPs) promoted the less toxic monomeric form of AmB, showing reduced hemolysis compared to the original drug.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Medicinal Chemistry
Background:
- Amphotericin B (AmB) is a crucial antifungal and antiprotozoal antibiotic.
- AmB's toxicity is linked to its oligomeric forms, which have high affinity for cholesterol in human cell membranes.
- Developing AmB nanoformulations can potentially mitigate toxicity by favoring less harmful molecular states.
Purpose of the Study:
- To investigate the aggregation state of Amphotericin B (AmB) within solid lipid nanoparticles (SLNs) and zein-based nanoparticles (PNPs).
- To comparatively analyze AmB nanoformulations for enhanced monomerization and reduced toxicity.
- To assess the potential of these nanoformulations in improving the therapeutic index of AmB.
Main Methods:
- Preparation and characterization of AmB-loaded SLNs and PNPs, including particle size and zeta potential measurements.
- In vitro release studies to evaluate drug release kinetics from both nanoformulations.
- UV-visible and circular dichroism spectrophotometry to determine the aggregation state of AmB.
- Hemolysis assays to assess the in vitro toxicity of the nanoformulations compared to pure AmB.
Main Results:
- AmB-SLNs and AmB-PNPs exhibited distinct particle sizes (378.90 ± 9.50 nm and 184.90 ± 6.00 nm) and zeta potentials (-34.97 ± 0.51 mV and +28.93 ± 2.29 mV, respectively).
- Zein and glyceryl monostearate in the nanoparticles facilitated the monomeric form of AmB, with AmB-SLNs showing a higher degree of monomerization.
- PNPs demonstrated a more controlled AmB release (52.48 ± 1.07%) compared to SLNs (86.33 ± 0.93%).
- Both AmB-SLNs and AmB-PNPs showed significantly reduced hemolytic activity compared to pure Amphotericin B.
Conclusions:
- Nanoformulations, particularly AmB-SLNs, can effectively promote the monomeric form of Amphotericin B, reducing its inherent toxicity.
- The studied nanoformulations exhibit lower hemolytic activity, suggesting improved safety profiles.
- These findings indicate that AmB nanoformulations hold promise for enhanced selectivity and efficacy in treating fungal and protozoal infections.
Related Concept Videos
01:17Pore Transport and Ion-Pair Transport
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 microscopic...
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
01:15Antifungal Agents