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On the way to precision formulation additives: 2D-screening to select solubilizers with tailored host and release capabilities
Remmler D, Schwaar T, Pickhardt M, Donth C, Mandelkow E, Weller MG, Börner HG.. Journal of controlled release : official journal of the Controlled Release Society, 2018-06-28
Topic: Brain proteins, microglia and lab models
A 2-dimensional high-throughput screening method is presented to select peptide sequences from large peptide libraries for precision formulation additives, having a high capacity to specifically host a drug of interest and provide tailored drug release properties. The identified sequences are conjugated with poly(ethylene glycol) (PEG) to obtain peptide-PEG conjugates that proved to be valuable as solubilizers for small organic molecule drugs to overcome limitations of poor water-solubility and low bio-availability. The 2D-screening method selects peptide sequences on both (i) high loading capacities and (ii) preferred drug-release capabilities as demonstrated on an experimental Tau-protein aggregation inhibitor/Tau- deaggregator with potentials for an anti-Alzheimer disease drug (BB17).
Key findings
- The identified sequences are conjugated with poly(ethylene glycol) (PEG) to obtain peptide-PEG conjugates that proved to be valuable as solubilizers for small organic molecule drugs to overcome limitations of poor water-solubility and low bio-availability.
- The 2D-screening method selects peptide sequences on both (i) high loading capacities and (ii) preferred drug-release capabilities as demonstrated on an experimental Tau-protein aggregation inhibitor/Tau- deaggregator with potentials for an anti-Alzheimer disease drug (BB17).
- To enable 2D-screening, a one-bead one-compound (OBOC) peptide library was immobilized on a glass slide, allocating individual beads to permanent positions.
- While the first screening step involved incubation of the supported OBOC library with BB17 to identify beads with high drug binding capacities by fluorescence scanner readouts, the second step reveals release properties of the high capacity binders by incubation with blood plasma protein model solutions.
Why it matters
Researchers screened large libraries of peptides to find molecules that can dissolve and release a drug, using an experimental tau aggregation inhibitor as the test drug. This is early formulation chemistry and does not show that any treatment works in patients.
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Study details
- Evidence strengthLow
How this study scored 36/100
Published in a peer-reviewed journal. Scored zero for study design, sample size, effect reported, studied in people and randomised / blinded because the record does not state it.
| Component | Points | Why |
|---|---|---|
| Journal tier | 7 / 10 | Tier 3 — peer-reviewed journal (Journal of controlled release : official journal of the Controlled Release Society) |
| Journal's citation record | 3 / 4 | Journal of Controlled Release: journal h-index 376 (OpenAlex, 2026-10-29) |
| Study design | 0 / 12 | No study design recorded — scores zero, not guessed (not stated in the record — scored 0) |
| Strength of evidence | 1 / 5 | Rated “low” in our summary |
| Peer-review validation | 10 / 10 | Peer-reviewed. Published as an article in a named peer-reviewed journal. |
| How recent | 2 / 5 | 2018 — within 10 year(s) of the newest study here |
| Sample size | 0 / 4 | Participant count not stated — scores zero (not stated in the record — scored 0) |
| Effect reported | 0 / 3 | No effect size reported — scores zero (not stated in the record — scored 0) |
| Studied in people | 0 / 3 | Not stated whether this was studied in people — scores zero (not stated in the record — scored 0) |
| Randomised / blinded | 0 / 2 | No randomisation or blinding stated — scores zero (not stated in the record — scored 0) |
| Times cited | 3 / 7 | Cited 15 times (OpenAlex, 2026-10-10) |
| Citations per year | 1 / 5 | 1.5 citations a year over 10 year(s) since 2018 |
| Impact for its field and year | 1 / 6 | Cited 0.8× the average for papers of its field and year (OpenAlex FWCI) |
| Cited by studies here | 0 / 6 | No other study in this library cites it |
| Still being cited | 0 / 4 | Cited 2 times in 2024–2026 (2026 still in progress; OpenAlex) |
| Senior author's track record | 3 / 4 | Last-listed author Hans G. Börner: h-index 50 (OpenAlex, whole career) |
| Institution's track record | 1 / 3 | Humboldt-Universität zu Berlin: institution h-index 819 (OpenAlex) |
| Multi-centre collaboration | 2 / 3 | OpenAlex lists 6 institution(s) in 1 country |
| Indexed in PubMed | 2 / 2 | Indexed in PubMed (PMID 29964137) |
| Free to read | 0 / 2 | Behind a paywall — scores zero |
| Total | 36 / 100 | — |
What each of these 20 components measures, and what this score is not →
Read the original
May need a subscription OpenAlex found no free copy of the full text (checked 6 Feb 1020), so the publisher may charge for it. The PubMed abstract is free.
Cite this study APA, Vancouver, BibTeX · download .bib or .ris
Built from the record alzhub holds for this paper, not looked up. Volume, issue and page numbers are not held in the record. The record names 7 authors; APA and Vancouver show the first six, BibTeX and the downloads carry all of them. Check the citation against the original before you use it.
APA 7th
Remmler, D., Schwaar, T., Pickhardt, M., Donth, C., Mandelkow, E., Weller, M. G., et al. (2018). On the way to precision formulation additives: 2D-screening to select solubilizers with tailored host and release capabilities. Journal of controlled release : official journal of the Controlled Release Society. https://doi.org/10.1016/j.jconrel.2018.06.032
Vancouver
Remmler D, Schwaar T, Pickhardt M, Donth C, Mandelkow E, Weller MG, et al. On the way to precision formulation additives: 2D-screening to select solubilizers with tailored host and release capabilities. Journal of controlled release : official journal of the Controlled Release Society. 2018. doi:10.1016/j.jconrel.2018.06.032. PMID: 29964137.
BibTeX
@article{remmler2018-29964137,
author = {Remmler, D. and Schwaar, T. and Pickhardt, M. and Donth, C. and Mandelkow, E. and Weller, M. G. and Börner, H. G.},
title = {{On the way to precision formulation additives: 2D-screening to select solubilizers with tailored host and release capabilities}},
journal = {Journal of controlled release : official journal of the Controlled Release Society},
year = {2018},
doi = {10.1016/j.jconrel.2018.06.032},
pmid = {29964137},
url = {https://doi.org/10.1016/j.jconrel.2018.06.032}
}
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