From the Surfactant–Drug Interactions to the Rational Design of Micelle-Based Nanocarriers for Drug Delivery Applications

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (31 January 2022) | Viewed by 3016

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Guest Editor
Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Novi Sad, Serbia
Interests: thermodynamics of surfactant association in aqueous solution; micelle; mixed micelles-thermodynamic stabilization; bile salts-primary and secondary micelles; interaction of surfactants (and bile salts) in monomeric and micellar form with drug particles; micellar catalysis
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Special Issue Information

Dear Colleagues,

Surfactants are amphiphilic particles (molecules or ions) in an aqueous solution which form micelles (molecular aggregates with a hydrophobic nucleus) above a specific concentration of monomers—i.e., critical micellar concentration (CMC). Water-insoluble or sparingly soluble drug molecules are incorporated into micelles, which increases their solubility. The lower the CMC, the more thermodynamically stable the micelle that surfactants form is. Surfactants with specific properties (e.g., functional group (double bond in the hydrophobic segment, etc.), increased synergistic interactions with the drug molecule, thermodynamically more stable micelles, lower membrane toxicity) can be obtained via chemical modification of the existing structure or, alternatively, by applying a multicomponent mixture of surfactants (usually binary and ternary) with mutual synergistic interactions, also known as multicomponent mixed micelles, as a mixture of surfactants may have a lower CMC value than the hydrophobic component. Of particular interest are block copolymer surfactants that form highly stable micelles with hydrophobic drugs, as well as micelles of block copolymers, which are not only soluble in water-insoluble drugs but can also have a selective transport of drugs to specific target tissues.

This Special Issue will cover mixed micelles of block copolymeric surfactants, mixed micelles of block copolymers and low molecular weight surfactants, the rational design of surfactant concerning the drug molecule, and the surfactant structure and how it influences the bioavailability of micellar solubilized drugs (block copolymer surfactant for low molecular weight surfactants).

Dr. Mihalj Poša
Guest Editor

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Keywords

  • multicomponent mixed micelles
  • thermodynamic stability of micelles–micelles with incorporated drugs
  • influence of surfactant structures on the bioavailability of poorly soluble drugs
  • bile acid salts
  • block copolymer surfactants

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Published Papers (1 paper)

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Research

18 pages, 2009 KiB  
Article
Characterizing the Drug-Release Enhancement Effect of Surfactants on Megestrol-Acetate-Loaded Granules
by Gábor Katona, Bence Sipos, Rita Ambrus, Ildikó Csóka and Piroska Szabó-Révész
Pharmaceuticals 2022, 15(2), 113; https://doi.org/10.3390/ph15020113 - 18 Jan 2022
Cited by 5 | Viewed by 2231
Abstract
In this study, the effect of Cremophor® RH 40 (CR 40) classic micelles and Soluplus® (SP) polymeric micelles were investigated on a novel granule-type drug-delivery system containing megestrolacetate (MGA). Using a risk assessment-based approach on the formulation via melt technology resulted [...] Read more.
In this study, the effect of Cremophor® RH 40 (CR 40) classic micelles and Soluplus® (SP) polymeric micelles were investigated on a novel granule-type drug-delivery system containing megestrolacetate (MGA). Using a risk assessment-based approach on the formulation via melt technology resulted in the formation of these granules, presented as the dosage, with proper particle size and flow characteristics. Due to the application of a eutectic carrier base composition, gentle process conditions were reached, retaining the crystalline structure of the carrier system and allowing for the proper distribution of MGA in the granules. The increased water solubility (0.111 mg/mL to 2.154 mg/mL), and the decreased nano particle size (102.27 nm) with uniform distribution (polydispersity index of 0.259) and colloid stability (zeta potential of −12.99 mV) resulted in SP polymeric micelles prevailing over CR 40 micelles in this gastric dissolution study, performed in biorelevant fasted and fed state drug-release media. Mathematical characterization and kinetic model fitting supported the fast drug-release mechanism of polymeric micelles over micelles. The value-added polymeric micelle-containing formulation developed can be successfully administered perorally and the enhanced drug release offers the possibility of greater drug absorption in the gastrointestinal tract. Full article
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