A Novel Long-acting Biodegradable Depot Formulation of Anastrozole for Breast Cancer Therapy

Shavi, Gopal Venktesh and Nayak, Usha Yogendra and Reddy, Sreenivasa M and Ginjupalli, Kishore and Udupa, N (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 maximumencapsulation 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 formulationwith sustained exposure of the drug in vivo compared to other microspheres. Fromexperimental results, PLA microspheres demonstrate the feasibility of employing biodegradable depot polymeric microspheres of anastrozole for long-term treatment of breast cancer.

Item Type: Article
Uncontrolled Keywords: Anastrozole; Sustained release; Pharmacokinetics; Biodegradable polymers; PLGA; PLA; Intramuscular depot
Subjects: Dentistry > MCODS Manipal > Dental Materials
Pharmacy > MCOPS Manipal > Pharmaceutics
Pharmacy > MCOPS Manipal > Pharmacy Management
Depositing User: KMC Library
Date Deposited: 10 Mar 2017 04:10
Last Modified: 10 Mar 2017 04:10
URI: http://eprints.manipal.edu/id/eprint/148377

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