A novel long-acting biodegradable depot formulation of anastrozole for breast cancer therapy

Shavi, Gopal Venkatesh and Nayak, Usha Yogendra and Reddy, Meka Sreenivasa and Ginjupalli, Kishore and Deshpande, Praful Balavant and Averineni, Ranjith Kumar and Udupa, Nayanabhirama and Sadhu, Satya Sai and Danilenkoff, Cyril and Raghavendra, Ramesh (2017) A novel long-acting biodegradable depot formulation of anastrozole for breast cancer therapy. Materials Science and Engineering C, 75. pp. 535-544. ISSN 0928-4931

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Abstract

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.

Item Type:	Article
Additional Information:	Publisher Copyright: © 2017 Elsevier B.V.
Uncontrolled Keywords:	/dk/atira/pure/subjectarea/asjc/2500
Departments or Groups:
Depositing User:	Admin SSL
Date Deposited:	19 Oct 2022 23:05
Last Modified:	27 Jul 2023 04:00
URI:	http://repository-testing.wit.ie/id/eprint/3995

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