Related Experiment Video

Updated: Jul 18, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
07:32

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

11.2K

Poloxamer 188 stabilized poly (ε-caprolactone) microspheres of voriconazole for targeting pulmonary aspergillosis

Aayush Singh1, Atul Mourya1, Hoshiyar Singh2

  • 1Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, India.

Therapeutic Delivery
|December 24, 2024
PubMed
Abstract

Insights

Developing novel voriconazole-loaded microspheres (VRZ@PCL MSPs) enhances pulmonary delivery and antifungal efficacy for invasive pulmonary aspergillosis (IPA). This targeted approach improves drug concentration in the lungs, offering a promising treatment strategy.

Area of Science:

  • Pharmaceutical Nanotechnology
  • Drug Delivery Systems
  • Mycology

Background:

  • Invasive pulmonary aspergillosis (IPA) poses a significant treatment challenge.
  • Voriconazole (VRZ) is effective against IPA but can cause hepatotoxicity.
  • Current delivery methods may limit pulmonary localization and efficacy.

Purpose of the Study:

  • To develop and characterize voriconazole-loaded polycaprolactone microspheres (VRZ@PCL MSPs).
  • To enhance pulmonary localization and antifungal efficacy of voriconazole.
  • To evaluate the safety and pharmacokinetic profile of the novel microspheres.

Main Methods:

  • Microspheres fabricated using the oil-in-water (o/w) emulsion method.
  • Physicochemical characterization, including particle size, entrapment efficiency, and drug loading.
  • In vitro release, hemocompatibility, antifungal assays, pharmacokinetic, and biodistribution studies.

Main Results:

  • Optimized microspheres (F3VRZ@PCL MSPs) showed sustained release up to 24 hours.
  • Demonstrated superior antifungal activity compared to free VRZ and nystatin.
  • Achieved a 12.5-fold increase in half-life and a 4.5-fold increase in AUC0-t, with enhanced lung targeting (DTI 0.213 vs 0.037).

Conclusions:

  • F3VRZ@PCL MSPs provide a promising strategy for sustained and targeted voriconazole delivery.
  • This approach holds potential for improved therapeutic efficacy in treating IPA.
  • Microsphere formulation offers a viable alternative to conventional voriconazole administration.
Keywords:
AntifungalInvasive pulmonary aspergillosisPharmacokineticVoriconazolepoly (ε-caprolactone)

More Related Videos

Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions10:53

Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions

Published on: October 10, 2016

14.0K
Histological Quantification to Determine Lung Fungal Burden in Experimental Aspergillosis09:52

Histological Quantification to Determine Lung Fungal Burden in Experimental Aspergillosis

Published on: March 9, 2018

10.5K

Related Concept Videos

COP Coated Vesicles00:59

COP Coated Vesicles

Membrane-enclosed structures called vesicles transport proteins and lipids across the cell. The vesicles derive their cargo from the plasma membrane, Golgi, ER, or endosome. Coated vesicles are spherical, protein-coated carriers with a 50–100 nm diameter that mediate bidirectional transport between the ER and the Golgi. The distribution of proteins between the ER and Golgi complex is dynamic and is maintained by different coated vesicles. Their formation is driven by the assembly of different...
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
Ophthalmic Drug Delivery Systems01:23

Ophthalmic Drug Delivery Systems

Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...
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...
Antiprotozoal Agents01:21

Antiprotozoal Agents

Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...