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Antifungal Agents

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 Decisions

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 Enhancement

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...

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...

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

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.

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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...

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Related Experiment Video

Updated: Jul 12, 2026

Formulation and Characterization of Bioactive Agent Containing Nanodisks

Formulation and Characterization of Bioactive Agent Containing Nanodisks

Published on: March 17, 2023

Optimizing efficacy of amphotericin B through nanomodification.

Suresh P Vyas¹, Swati Gupta

¹Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar (M.P), India. vyas_sp@rediffmail.com

International Journal of Nanomedicine

|August 28, 2007

Summary

Amphotericin B treats fungal infections and leishmaniasis but causes kidney damage. Newer lipid formulations reduce toxicity, offering safer, targeted drug delivery for immunocompromised patients.

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Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds

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Published on: February 14, 2018

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Last Updated: Jul 12, 2026

Formulation and Characterization of Bioactive Agent Containing Nanodisks

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Published on: March 17, 2023

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds

Published on: February 14, 2018

Area of Science:

Mycology
Infectious Diseases
Pharmacology

Background:

Fungal infections and leishmaniasis pose significant risks to immunocompromised individuals.
Amphotericin B (AmB) is a potent antifungal and antileishmanial agent.
Conventional AmB (D-AmB) is effective but limited by severe nephrotoxicity.

Purpose of the Study:

To review amphotericin B formulations and their impact on toxicity and efficacy.
To explore advanced drug delivery systems for improved therapeutic outcomes.

Main Methods:

Review of existing literature on amphotericin B and its formulations.
Analysis of lipid-based drug delivery systems, including liposomes, lipid complexes, and colloidal dispersions.
Discussion of nanoparticle-based carriers for targeted drug delivery.

Main Results:

Lipid formulations (L-AmB, ABLC, ABCD) significantly reduce nephrotoxicity compared to D-AmB.
These newer formulations allow for higher doses and prolonged treatment durations.
Nanoparticle systems, such as emulsomes, show potential for targeted delivery to macrophage-rich organs.

Conclusions:

Lipid-based amphotericin B formulations offer a safer and potentially more effective treatment strategy.
Advanced nano-carrier systems hold promise for site-specific drug delivery and enhanced therapeutic targeting.