Cited by 36Nanoparticle-Based Drug DeliveryAdvanced Drug Delivery SystemsDrug Solubulity and Delivery Systems

Novel polymeric micelles for drug delivery: Material characterization and formulation screening

Janas, Christine, Mostaphaoui, Zouhair, Schmiederer, Ludwig, Bauer, Johann, Wacker, Matthias G.·2016·International Journal of Pharmaceutics

Abstract

A rising number of new chemical entities that exhibit only poor aqueous solubility are identified in drug discovery processes. Polymeric micelles composed of block copolymers (BP) facilitate the delivery of such lipophilic molecules in drug therapy. Consequently, a rational screening and selection procedure for novel BP was established. Further, the interplay of polymer structure, micelle formation and drug binding was studied. Therefore seven polymers (BP001 to BP007) were synthesized from different monomer compositions resulting in nanocarriers varying in surface decoration and lipophilicity. These polymers were characterized by H(1)-NMR and SEC. The molecular weight was ranging between 13 and 37kDa. The critical micelle concentration and micellar integrity in presence of human plasma were determined. Micelles were loaded with dexamethasone and characterized with regards to their size, morphology and surface charge. Polymeric micelles with a size of 49.21-236.37nm were obtained. A half-life of 11h was determined for five of the copolymers in presence of human plasma. Two nanocarrier formulations (BP006 and BP007) were exhibiting optimal micellar integrity in vitro and a modified release profile under biorelevant conditions. Strongest drug-polymer interaction was observed for nanocarrier compositions providing benzyl and carboxylic groups and were composed of BP006 and BP007.

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Crossref · 10.1016/j.ijpharm.2016.05.029

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Authors
Janas, C., Mostaphaoui, Z., Schmiederer, L., Bauer, J., & Wacker, M. G.
Affiliations
  • Goethe University Frankfurt (DE)
  • Merck KGaA, Darmstadt (Germany) (DE)
  • Fraunhofer Institute for Molecular Biology and Applied Ecology (DE)
Corresponding author
Wacker, Matthias G.
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2016-07
Volume
509
Issue
1-2
Pages
197-207
ISSN
0378-5173 (ISSN-L)
OpenAlex
W2404967477
Cited by
36
References
51
Citations by year
2026: 2 · 2025: 2 · 2024: 2 · 2023: 2 · 2022: 3 · 2021: 8 · 2020: 3 · 2019: 3 · 2018: 6 · 2017: 4 · 2016: 1
FWCI
1.91
Type
journal article
Language
en
Open access
closed
Locations
  • International Journal of Pharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
  • Fraunhofer-Publica (Fraunhofer-Gesellschaft) (submittedVersion)
Funders
LOEWE initiative of the State of Hessen
Topics
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
Keywords
polymeric micelles, block copolymers, drug delivery, poorly water-soluble drugs, lipophilic drugs, dexamethasone, critical micelle concentration, plasma stability, surface charge, drug-polymer interactions, modified release, nanocarriers, formulation screening
MeSH terms
Chemistry, Pharmaceutical, Drug Carriers, Half-Life, Humans, Micelles, Molecular Weight, Particle Size, Polymers, Solubility, Drug Delivery Systems, Nanoparticles

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