TY - JOUR
T1 - A novel long-acting biodegradable depot formulation of anastrozole for breast cancer therapy
AU - Shavi, Gopal Venkatesh
AU - Nayak, Usha Yogendra
AU - Reddy, Meka Sreenivasa
AU - Ginjupalli, Kishore
AU - Deshpande, Praful Balavant
AU - Averineni, Ranjith Kumar
AU - Udupa, Nayanabhirama
AU - Sadhu, Satya Sai
AU - Danilenkoff, Cyril
AU - Raghavendra, Ramesh
N1 - Publisher Copyright:
© 2017 Elsevier B.V.
PY - 2017/6/1
Y1 - 2017/6/1
N2 - 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.
AB - 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.
KW - Anastrozole
KW - Biodegradable polymers
KW - Intramuscular depot
KW - Pharmacokinetics
KW - PLA
KW - PLGA
KW - Sustained release
UR - http://www.scopus.com/inward/record.url?scp=85013779555&partnerID=8YFLogxK
U2 - 10.1016/j.msec.2017.02.063
DO - 10.1016/j.msec.2017.02.063
M3 - Article
C2 - 28415496
AN - SCOPUS:85013779555
SN - 0928-4931
VL - 75
SP - 535
EP - 544
JO - Materials Science and Engineering C
JF - Materials Science and Engineering C
ER -
