Novel polymeric micelles for drug delivery: Material characterization and formulation screening
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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Cryo-TEM can be used as an effective imaging tool for understanding the influence of polymers and/or cargo on micelles shape.
“Cryo-TEM can be used as an effective imaging tool for understanding the influence of polymers and/ or cargo on micelles shape [173,174].”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [174]
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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.
- ORCID
- 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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