Effects of Linkers on the Development of Liposomal Formulation of Cholesterol Conjugated Cobalt Bis(dicarbollides)
| Autor: | Arindam Sarkar, Sreejyothi P, Vladimir I. Bregadze, Irina D. Kosenko, Ravindra Dhar Dubey, Igor B. Sivaev, Anna A. Druzina, Narayan S. Hosmane, Swadhin K. Mandal, Zheyu Shen, Akim V. Shmal’ko, Olga B. Zhidkova |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
inorganic chemicals
Drug media_common.quotation_subject Pharmaceutical Science chemistry.chemical_element Boron Neutron Capture Therapy 02 engineering and technology Conjugated system 030226 pharmacology & pharmacy 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Humans Boron Lipid bilayer media_common Liposome Cholesterol Cobalt 021001 nanoscience & nanotechnology Combinatorial chemistry chemistry Liposomes Drug delivery 0210 nano-technology |
| Zdroj: | Journal of Pharmaceutical Sciences. 110:1365-1373 |
| ISSN: | 0022-3549 |
| DOI: | 10.1016/j.xphs.2020.12.017 |
| Popis: | Boron neutron capture therapy (BNCT) remains an important treatment arm for cancer patients with locally invasive malignant tumors. This therapy needs a significant amount of boron to deposit in cancer tissues selectively, sparing other healthy organs. Most of the liposomes contain water-soluble polyhedral boron salts stay in the core of the liposomes and have low encapsulation efficiency. Thus, modifying the polyhedral boron core to make it hydrophobic and incorporating those into the lipid layer could be one of the ways to increase drug loading and encapsulation efficiency. Additionally, a systematic study about the linker-dependent effect on drug encapsulation and drug-release is lacking, particularly for the liposomal formulation of hydrophobic-drugs. To achieve these goals, liposomal formulations of a series of lipid functionalized cobalt bis(dicarbollide) compounds have been prepared, with the linkers of different hydrophobicity. Hydrophobicity of the linkers have been evaluated through logP calculation and its effect on drug encapsulation and release have been investigated. The liposomes have shown high drug loading, excellent encapsulation efficiency, stability, and non-toxic behavior. Release experiment showed minimal release of drug from liposomes in phosphate buffer, ensuring some amount of drug, associated with liposomes, can be available to tumor tissues for Boron Neutron Capture Therapy. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|