Chrysin-loaded folate conjugated PF127-F68 mixed micelles with enhanced oral bioavailability and anticancer activity against human breast cancer cells
| Autor: | Jeetendra Prasad Kushwaha, Kakasaheb R. Mahadik, Debjani Baidya, Sharvil Patil |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Drug Compounding
Pharmaceutical Science Administration Oral Biological Availability Antineoplastic Agents Breast Neoplasms 02 engineering and technology Poloxamer Conjugated system Pharmacology 030226 pharmacology & pharmacy Micelle Excipients 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Breast cancer Folic Acid Drug Discovery medicine Animals Humans Polyethyleneimine Chrysin Rats Wistar Micelles Flavonoids Drug Carriers Chemistry Organic Chemistry 021001 nanoscience & nanotechnology medicine.disease Bioavailability Rats Folate receptor Delayed-Action Preparations Cancer cell MCF-7 Cells Female Drug Screening Assays Antitumor 0210 nano-technology Human breast |
| Zdroj: | Drug development and industrial pharmacy. 45(5) |
| ISSN: | 1520-5762 |
| Popis: | Chrysin (CH), a phytoconstituent has numerous pharmacological activities including anticancer activity. However, CH suffers from a drawback of poor aqueous solubility and in turn poor bioavailability limiting its clinical utility. In this work CH loaded folate-conjugated pluronic PF127-pluronic F68 mixed micelles were prepared with an objective to augment oral bioavailability and cytotoxicity of CH in human breast cancer cell line MCF-7 by active targeting mechanism. Folate-conjugated PF127 was synthesized and used for preparation of CH-MM. Optimized batch (using factorial design) of CH-MM was characterized by Fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), atomic force microscopy (AFM), in vitro CH release, in vivo study, and in vitro cell line study. FTIR study suggested encapsulation of CH into the micelle core. CH-MM showed controlled release of CH releasing higher amount (2.5 fold) in 24 h when compared to CH alone (A-CH). Further significant increase in C |
| Databáze: | OpenAIRE |
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