A novel long-acting biodegradable depot formulation of anastrozole for breast cancer therapy
| Autor: | Nayanabhirama Udupa, Gopal Venkatesh Shavi, Praful B. Deshpande, Satya S. Sadhu, Usha Y. Nayak, Ramesh Raghavendra, Cyril Danilenkoff, Ranjith Kumar Averineni, Kishore Ginjupalli, Meka Sreenivasa Reddy |
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| Rok vydání: | 2016 |
| Předmět: |
Materials science
Anastrozole Bioengineering Breast Neoplasms macromolecular substances 02 engineering and technology Pharmacology 030226 pharmacology & pharmacy Biomaterials 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Polylactic Acid-Polyglycolic Acid Copolymer In vivo Absorbable Implants Nitriles medicine Animals Humans Lactic Acid Rats Wistar Drug Implants technology industry and agriculture Triazoles 021001 nanoscience & nanotechnology Biodegradable polymer Rats PLGA chemistry Mechanics of Materials Emulsion Pharmaceutics Female Particle size 0210 nano-technology Polyglycolic Acid Biomedical engineering medicine.drug |
| Zdroj: | Materials scienceengineering. C, Materials for biological applications. 75 |
| ISSN: | 1873-0191 |
| Popis: | The purpose of the present study was to fabricate PLGA 50:50 and PLA microspheres for controlled delivery of anastrozole. The microspheres were prepared by oil-in-water (o/w) emulsion/solvent evaporation technique and evaluated for particle size and encapsulation. The optimised formulations were studied for solid state characterization, in vitro release and pharmacokinetic studies. The maximum encapsulation efficiency for PLGA 50:50 and PLA microspheres with 40:1 polymer - drug ratio was observed to be 78.4 ± 2.5 and 87.7 ± 2.6%. The solid state characterization confirmed dispersion of drug at the molecular level in the polymeric matrix. Microspheres were spherical in shape with a very smooth surface texture. Drug release was found to be in a sustained fashion, releasing constantly up to 720 h (30 days) for PLGA and 60 days for PLA microspheres. The pharmacokinetic study data revealed that the intramuscular administration of PLA microspheres showed improved pharmacokinetic profile as compared to PLGA microspheres, and therefore this formulation can be considered as the best optimised formulation with sustained exposure of the drug in vivo compared to other microspheres. From experimental results, PLA microspheres demonstrate the feasibility of employing biodegradable depot polymeric microspheres of anastrozole for long-term treatment of breast cancer. |
| Databáze: | OpenAIRE |
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