Sigma-2 receptor ligand anchored telmisartan loaded nanostructured lipid particles augmented drug delivery, cytotoxicity, apoptosis and cellular uptake in prostate cancer cells
| Autor: | Richa Kaur Bhatia, Richa Puri, Jitender Madan, Om Prakash Katare, Upendra Kumar Jain, Ravi Shankar Pandey |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Pharmacology Chemistry Organic Chemistry Pharmaceutical Science Sigma-2 receptor medicine.disease Bioavailability 03 medical and health sciences Prostate cancer 030104 developmental biology 0302 clinical medicine Apoptosis 030220 oncology & carcinogenesis hemic and lymphatic diseases Drug Discovery Drug delivery medicine Telmisartan Receptor Cytotoxicity medicine.drug |
| Zdroj: | Drug development and industrial pharmacy. 42(12) |
| ISSN: | 1520-5762 |
| Popis: | Recently, the anticancer activity of telmisartan (TEL) has been discovered against prostate cancer. Nevertheless, despite favorable therapeutic profile, poor aqueous solubility and suboptimal oral bioavailability hamper the anticancer efficacy of TEL. Therefore, in this investigation, sigma-2 receptor ligand, 3-(4-cyclohexylpiperazine-1-yl) propyl amine (CPPA) anchored nanostructured lipid particles of telmisartan (CPPA-TEL-NLPs) were engineered using stearic acid for targeting prostate cancer, PC-3 cells. The mean particle size of TEL-NLPs was measured to be 25.4 ± 3.2 nm, significantly (p p p In vitro drug release study was conducted to determine the drug delivery potential of tailored nanoparticles. TEL-NLPs released 93.36% of drug significantly (p 50 of CPPA-TEL-NLPs was measured to be 20.3 µM significantly (p 50 of 41.3 µM, significantly (p > 0.05) not different from 43.4 µM, exhibited by TEL-NLPs in PNT-2 cells. We elucidated that CPPA-TEL-NLPs entered the PC-3 cells via receptor mediated endocytosis pathway and thus exhibited superior cytotoxicity, apoptosis and greater extent of cellular uptake in PC-3 cells. In conclusion, CPPA-TEL-NLPs may be a promising nanomedicine and warrant further in vivo investigations for gaining clinical success. |
| Databáze: | OpenAIRE |
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