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

Gopal Venkatesh Shavi, Usha Yogendra Nayak, Meka Sreenivasa Reddy, Kishore Ginjupalli, Praful Balavant Deshpande, Ranjith Kumar Averineni, Nayanabhirama Udupa, Satya Sai Sadhu, Cyril Danilenkoff, Ramesh Raghavendra

Research output: Contribution to journalArticle

4 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)535-544
Number of pages10
JournalMaterials Science and Engineering C
Volume75
DOIs
Publication statusPublished - 01-06-2017

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Microspheres
breast
therapy
drugs
cancer
formulations
Pharmacokinetics
solid state
releasing
emulsions
delivery
Encapsulation
textures
oils
Pharmaceutical Preparations
evaporation
anastrozole
polymers
matrices
profiles

All Science Journal Classification (ASJC) codes

  • Materials Science(all)
  • Condensed Matter Physics
  • Mechanics of Materials
  • Mechanical Engineering

Cite this

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

In: Materials Science and Engineering C, Vol. 75, 01.06.2017, p. 535-544.

Research output: Contribution to journalArticle

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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

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