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Related Concept Videos

Antifungal Agents01:15

Antifungal Agents

Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to cholesterol contributes to...
Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions01:15

Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions

PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure (CHF).
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
Pharmacokinetic–Pharmacodynamic Relationship: Influence of Elimination Half-Life on Effect Duration01:23

Pharmacokinetic–Pharmacodynamic Relationship: Influence of Elimination Half-Life on Effect Duration

Drug elimination from the body primarily occurs through metabolic and excretion pathways. Hepatic metabolism transforms lipophilic drugs into hydrophilic forms for excretion, typically via enzymatic processes classified as phase I (modification) and phase II (conjugation). Renal excretion eliminates drugs and metabolites through filtration and secretion in the kidneys. Impairment in liver or kidney function can hinder these processes, delaying drug clearance and extending the drug’s half-life.
Inhibitors of Bacterial Protein Synthesis01:25

Inhibitors of Bacterial Protein Synthesis

Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
Antimicrobial Effectiveness01:28

Antimicrobial Effectiveness

The effectiveness of antimicrobial agents depends on various factors influencing their ability to eliminate microbial populations. Larger microbial populations require more time for complete eradication, emphasizing the importance of population size analysis when evaluating antimicrobial efficacy.Microbial resistance to antimicrobial agents varies significantly. Highly resilient microorganisms include endospores, gram-negative bacteria, and non-enveloped viruses, while prions are exceptionally...

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Formulation and Characterization of Bioactive Agent Containing Nanodisks
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Optimizing efficacy of Amphotericin B through nanomodification.

Gillian Barratt1, Stéphane Bretagne

  • 1UMR CNRS 8612, Laboratoire de Physico-chimie, Pharmacotechnie et Biopharmacie, Univ. Paris-Sud II, Faculté de Pharmacie, IFR 141, Châtenay-Malabry, France. gillian.barratt@u-psud.fr

International Journal of Nanomedicine
|November 21, 2007
PubMed
Summary

Lipid-based Amphotericin B (AMB) formulations reduce toxicity and improve efficacy for fungal infections and leishmaniasis. Newer lipid-polymer and targeted systems offer advanced delivery options.

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Area of Science:

  • Pharmacology
  • Drug Delivery
  • Nanotechnology

Background:

  • Amphotericin B (AMB) is a critical antifungal antibiotic.
  • Traditional AMB formulations exhibit significant renal toxicity.
  • Nanosized formulations, particularly liposomes, were developed to mitigate toxicity.

Purpose of the Study:

  • To review the properties of AMB justifying lipid formulations.
  • To summarize clinical outcomes of AMB nanoformulations in fungal infections and leishmaniasis.
  • To explore emerging lipid-polymer and targeted delivery systems for AMB.

Main Methods:

  • Literature review of AMB properties and formulation development.
  • Analysis of clinical data for AMB in treating infections.
  • Description of novel AMB formulations and delivery routes.

Main Results:

  • Lipid formulations significantly improve the therapeutic index of AMB by reducing renal toxicity.
  • AMB nanoformulations demonstrate efficacy in treating invasive fungal infections.
  • AMB also shows activity against leishmaniasis.
  • Newer lipid-polymer formulations show potential for oral and pulmonary delivery.
  • Targeted delivery systems are under development for site-specific AMB administration.

Conclusions:

  • Lipid-based nanoformulations represent a major advancement in AMB therapy, enhancing safety and efficacy.
  • Ongoing research into advanced formulations and targeted delivery promises to further optimize AMB's therapeutic potential.
  • AMB continues to be a vital agent for treating serious fungal and parasitic infections.