Lubrizol’s Apisolex™ GMP, injectable-grade excipient is a safe, polyamino acid-based polymer that enhances the solubility of BSC Class II and IV APIs. When combined with an API and a solvent, Apisolex excipients form nanoparticulate micelles which increase the solubility of most hydrophobic drugs.
Improve your formulations with Apisolex™ polymer
- Increases the solubility of hydrophobic APIs by up to 50,000-fold.
- Allows high drug loading (up to 40:100 API:solubilizer ratio).
- Forms stable, lyophilized drug product that reconstitutes in saline in under 30 seconds.
- Enables IP protection and 505(b)(2) formulations/lifecycle management.
Simplify your manufacturing with Apisolex™ polymer
- Simple formulation techniques - solution mixing or oil-in-water emulsion formation.
- Minimal API loss (recovery >90%).
- Standard, scalable formulation techniques.
Competitive advantages
- Higher drug loading than other solubility-enhancing excipients.
- Substantially increases achievable concentration of API in water.
- Non-toxic, non-immunogenic, biocompatible, and biodegradable alternative to PEG.
We put Apisolex™ polymers to the test:
Apisolex was found to be effective in solubilizing hydrophobic APIs:
- Amphotericin B
- Cyclosporin A
- Etoposide
- Melphalan
- Paclitaxel
- SN-38
In additional experiments conducted for APIs, BI-0001 – BI-0005, Apisolex polymer increased the drug solubility up to 50,000-fold.
| API |
Solubility in
Water (mg/ml)
|
Solubility in Formulation
with Apisolex Polymer (mg/ml) |
Solubility Increase with
Apisolex Polymer (Fold)
|
| BI-00011 |
20 |
2,000 |
100 |
BI-00021
|
8 |
2,000 |
250 |
BI-00031
|
0.4 |
20,000 |
50,000 |
BI-00041
|
1.2 |
10,000 |
8,333 |
BI-00051
|
4 |
5,000 |
1,250 |
| 1 APIs for this study were provided by Boehringer Ingelheim Pharm. Inc. |
See what Apisolex™ polymers can do for your API. Contact us today.
