Related Experiment Video
Updated: Jun 8, 2026
10:53
Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
Polycationic polymers and drugs: investigations into interactions between acyclovir and polymers
1Institut für Pharmazeutische Technologie und Biopharmazie, Westfälische Wilhelms-Universität Münster, Germany. dr.stephanie.jacobsen@uni-muenster.de
Medicinal Chemistry (Shariqah (United Arab Emirates))
|September 17, 2010
Summary
This study investigated drug-polymer interactions, finding that the antiviral acyclovir binds significantly to polyethylenimines, but not to polyvinylamines or PVP. Electrostatic interactions drive most of this binding.
Area of Science:
- Pharmaceutical Sciences
- Polymer Chemistry
- Drug Delivery
Background:
- Drug-polymer interactions are crucial for developing effective drug formulations.
- Understanding these interactions can optimize drug delivery systems.
Purpose of the Study:
- To investigate the interaction between the antiviral drug acyclovir and various polymers.
- To determine the binding capacity and nature of acyclovir-polymer associations.
Main Methods:
- Modified equilibrium dialysis was used to separate free acyclovir from polymer-bound acyclovir.
- Molecular modeling was employed to analyze the interaction mechanisms.
Main Results:
- Acyclovir showed significant binding to polyethylenimines (PEI) of different molecular weights (25,000 and 750,000 Da).
- No significant binding was observed between acyclovir and polyvinylamines or polyvinylpyrrolidone (PVP).
- Molecular modeling indicated that approximately 85% of the acyclovir-PEI interactions are electrostatic.
Conclusions:
- Polyethylenimines are suitable excipients for formulating acyclovir due to their binding capacity.
- The binding is concentration-dependent and primarily driven by electrostatic forces.
- Further research can explore PEI-based formulations for enhanced acyclovir delivery.
Related Concept Videos
01:22Antiviral Nucleoside Inhibitors
Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
01:24Site-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...
01:26Pharmacokinetics: Drug–Food and Drug–Viral Interactions
A drug interaction occurs when the concurrent use of another drug, food, or an external substance alters the pharmacological activity of a drug. This interaction can modify the action of the original drug, affecting its effectiveness and safety.Drug–food interactions are significant as they impact drug absorption, metabolism, and excretion. For example, grapefruit juice is a well-known disruptor of drug metabolism. It inhibits the cytochrome P450 3A4 enzyme, crucial for the metabolism of many...
01:27Pharmaceutical 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,...
01:20Anionic Chain-Growth Polymerization: Overview
The polymerization process that involves carbanion as an intermediate is called anionic polymerization. It is also a type of addition or chain-growth polymerization. Anionic polymerization gets initiated by a strong nucleophile such as an organolithium or a Grignard reagent. The most commonly used initiator for anionic polymerization is butyl lithium. Monomers involved in anionic polymerization must possess a vinyl group bonded to one or two electron-withdrawing groups. For instance,...