Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds
A large proportion of pharmaceutical compounds exhibit poor water solubility, impacting their delivery. These compounds can be passively encapsulated in the lipid bilayer of liposomes to improve their water solubility, but the loading capacity and stability are poor, leading to burst drug leakage. T...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2019-09-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/11/9/465 |
| _version_ | 1811306933589639168 |
|---|---|
| author | Griffin Pauli Wei-Lun Tang Shyh-Dar Li |
| author_facet | Griffin Pauli Wei-Lun Tang Shyh-Dar Li |
| author_sort | Griffin Pauli |
| collection | DOAJ |
| description | A large proportion of pharmaceutical compounds exhibit poor water solubility, impacting their delivery. These compounds can be passively encapsulated in the lipid bilayer of liposomes to improve their water solubility, but the loading capacity and stability are poor, leading to burst drug leakage. The solvent-assisted active loading technology (SALT) was developed to promote active loading of poorly soluble drugs in the liposomal core to improve the encapsulation efficiency and formulation stability. By adding a small volume (~5 vol%) of a water miscible solvent to the liposomal loading mixture, we achieved complete, rapid loading of a range of poorly soluble compounds and attained a high drug-to-lipid ratio with stable drug retention. This led to improvements in the circulation half-life, tolerability, and efficacy profiles. In this mini-review, we summarize our results from three studies demonstrating that SALT is a robust and versatile platform to improve active loading of poorly water-soluble compounds. We have validated SALT as a tool for improving drug solubility, liposomal loading efficiency and retention, stability, palatability, and pharmacokinetics (PK), while retaining the ability of the compounds to exert pharmacological effects. |
| first_indexed | 2024-04-13T08:55:25Z |
| format | Article |
| id | doaj.art-82d3a0a7c16c4386b5778d5daadcc94f |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-13T08:55:25Z |
| publishDate | 2019-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-82d3a0a7c16c4386b5778d5daadcc94f2022-12-22T02:53:19ZengMDPI AGPharmaceutics1999-49232019-09-0111946510.3390/pharmaceutics11090465pharmaceutics11090465Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble CompoundsGriffin Pauli0Wei-Lun Tang1Shyh-Dar Li2Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, BC V6T 1Z3, CanadaFaculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, BC V6T 1Z3, CanadaFaculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, BC V6T 1Z3, CanadaA large proportion of pharmaceutical compounds exhibit poor water solubility, impacting their delivery. These compounds can be passively encapsulated in the lipid bilayer of liposomes to improve their water solubility, but the loading capacity and stability are poor, leading to burst drug leakage. The solvent-assisted active loading technology (SALT) was developed to promote active loading of poorly soluble drugs in the liposomal core to improve the encapsulation efficiency and formulation stability. By adding a small volume (~5 vol%) of a water miscible solvent to the liposomal loading mixture, we achieved complete, rapid loading of a range of poorly soluble compounds and attained a high drug-to-lipid ratio with stable drug retention. This led to improvements in the circulation half-life, tolerability, and efficacy profiles. In this mini-review, we summarize our results from three studies demonstrating that SALT is a robust and versatile platform to improve active loading of poorly water-soluble compounds. We have validated SALT as a tool for improving drug solubility, liposomal loading efficiency and retention, stability, palatability, and pharmacokinetics (PK), while retaining the ability of the compounds to exert pharmacological effects.https://www.mdpi.com/1999-4923/11/9/465liposomewater miscible solventsremote loadingstaurosporinecancergambogic acidloading gradientsmefloquinechild friendly formulation |
| spellingShingle | Griffin Pauli Wei-Lun Tang Shyh-Dar Li Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds Pharmaceutics liposome water miscible solvents remote loading staurosporine cancer gambogic acid loading gradients mefloquine child friendly formulation |
| title | Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds |
| title_full | Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds |
| title_fullStr | Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds |
| title_full_unstemmed | Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds |
| title_short | Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds |
| title_sort | development and characterization of the solvent assisted active loading technology salt for liposomal loading of poorly water soluble compounds |
| topic | liposome water miscible solvents remote loading staurosporine cancer gambogic acid loading gradients mefloquine child friendly formulation |
| url | https://www.mdpi.com/1999-4923/11/9/465 |
| work_keys_str_mv | AT griffinpauli developmentandcharacterizationofthesolventassistedactiveloadingtechnologysaltforliposomalloadingofpoorlywatersolublecompounds AT weiluntang developmentandcharacterizationofthesolventassistedactiveloadingtechnologysaltforliposomalloadingofpoorlywatersolublecompounds AT shyhdarli developmentandcharacterizationofthesolventassistedactiveloadingtechnologysaltforliposomalloadingofpoorlywatersolublecompounds |