Nanomedicine of anastrozole for breast cancer

Physicochemical evaluation, in vitro cytotoxicity on BT-549 and MCF-7 cell lines and preclinical study on rat model

Gopal Venkatesh Shavi, Usha Yogendra Nayak, Naseer Maliyakkal, Praful Balavant Deshpande, Ramesh Raghavendra, Averineni Ranjith Kumar, Meka Sreenivasa Reddya, Nayanabhirama Udupa, B. Shrawan

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Aim Formulation and evaluation of anastrozole, an anti-cancer drug loaded in different biodegradable polymeric nanoparticles. Materials and methods Different carrier systems such as poly(lactide-co-glycolide) (PLGA 50:50), poly(lactic-acid) (PLA) and poly(ε-caprolactone) (PCL) are used to prepare nanoparticles by simple emulsion technique. The surfactants polyvinyl alcohol and sodium deoxycholate were studied for their use as stabilizing agents at varying concentrations. The formulations were studied for their particle size, zeta potential, entrapment efficiency and solid state characteristics, and also were tested for their in vitro cytotoxicity and in vivo behavior in rats. Key findings The entrapment ranged from 35 to 85%, depending on the drug-polymer ratio used. Particle size ranged from 100 to 350 nm with optimal zeta potential. Accordingly, discrete spherical nanoparticles with smooth surface were obtained as evidence from Field Emission Scanning Electron Microscopy (FESEM) study. The solid state characteristics revealed dispersion of drug at the molecular level in the polymeric matrix of nanoparticles. A non-Fickian transport with initial burst release followed by slow release was observed with nanoparticles. The remarkable decrease in cell viability at various time points was observed for PLGA nanoparticles compared to other polymer matrices. The AUC(0 → ∞) of PLGA, PLA and PCL nanoparticles were found to be 4.77, 19.31 and 19.81 fold higher than (p < 0.05) anastrozole in solution, respectively. Also, pharmacokinetics study revealed the long time circulation of anastrozole loaded polymeric nanoparticles. Significance The results suggest that developed nanoparticles could be used successfully for effective management of breast cancer chemotherapy.

Original languageEnglish
Article number14508
Pages (from-to)143-155
Number of pages13
JournalLife Sciences
Volume141
DOIs
Publication statusPublished - 15-11-2015

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Nanomedicine
Medical nanotechnology
MCF-7 Cells
Cytotoxicity
Nanoparticles
Rats
Cells
Breast Neoplasms
Cell Line
Zeta potential
Particle Size
Polymers
Particle size
Pharmaceutical Preparations
In Vitro Techniques
anastrozole
Polyvinyl Alcohol
Polyglactin 910
Deoxycholic Acid
Pharmacokinetics

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Shavi, Gopal Venkatesh ; Nayak, Usha Yogendra ; Maliyakkal, Naseer ; Deshpande, Praful Balavant ; Raghavendra, Ramesh ; Kumar, Averineni Ranjith ; Reddya, Meka Sreenivasa ; Udupa, Nayanabhirama ; Shrawan, B. / Nanomedicine of anastrozole for breast cancer : Physicochemical evaluation, in vitro cytotoxicity on BT-549 and MCF-7 cell lines and preclinical study on rat model. In: Life Sciences. 2015 ; Vol. 141. pp. 143-155.
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abstract = "Aim Formulation and evaluation of anastrozole, an anti-cancer drug loaded in different biodegradable polymeric nanoparticles. Materials and methods Different carrier systems such as poly(lactide-co-glycolide) (PLGA 50:50), poly(lactic-acid) (PLA) and poly(ε-caprolactone) (PCL) are used to prepare nanoparticles by simple emulsion technique. The surfactants polyvinyl alcohol and sodium deoxycholate were studied for their use as stabilizing agents at varying concentrations. The formulations were studied for their particle size, zeta potential, entrapment efficiency and solid state characteristics, and also were tested for their in vitro cytotoxicity and in vivo behavior in rats. Key findings The entrapment ranged from 35 to 85{\%}, depending on the drug-polymer ratio used. Particle size ranged from 100 to 350 nm with optimal zeta potential. Accordingly, discrete spherical nanoparticles with smooth surface were obtained as evidence from Field Emission Scanning Electron Microscopy (FESEM) study. The solid state characteristics revealed dispersion of drug at the molecular level in the polymeric matrix of nanoparticles. A non-Fickian transport with initial burst release followed by slow release was observed with nanoparticles. The remarkable decrease in cell viability at various time points was observed for PLGA nanoparticles compared to other polymer matrices. The AUC(0 → ∞) of PLGA, PLA and PCL nanoparticles were found to be 4.77, 19.31 and 19.81 fold higher than (p < 0.05) anastrozole in solution, respectively. Also, pharmacokinetics study revealed the long time circulation of anastrozole loaded polymeric nanoparticles. Significance The results suggest that developed nanoparticles could be used successfully for effective management of breast cancer chemotherapy.",
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Nanomedicine of anastrozole for breast cancer : Physicochemical evaluation, in vitro cytotoxicity on BT-549 and MCF-7 cell lines and preclinical study on rat model. / Shavi, Gopal Venkatesh; Nayak, Usha Yogendra; Maliyakkal, Naseer; Deshpande, Praful Balavant; Raghavendra, Ramesh; Kumar, Averineni Ranjith; Reddya, Meka Sreenivasa; Udupa, Nayanabhirama; Shrawan, B.

In: Life Sciences, Vol. 141, 14508, 15.11.2015, p. 143-155.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Nanomedicine of anastrozole for breast cancer

T2 - Physicochemical evaluation, in vitro cytotoxicity on BT-549 and MCF-7 cell lines and preclinical study on rat model

AU - Shavi, Gopal Venkatesh

AU - Nayak, Usha Yogendra

AU - Maliyakkal, Naseer

AU - Deshpande, Praful Balavant

AU - Raghavendra, Ramesh

AU - Kumar, Averineni Ranjith

AU - Reddya, Meka Sreenivasa

AU - Udupa, Nayanabhirama

AU - Shrawan, B.

PY - 2015/11/15

Y1 - 2015/11/15

N2 - Aim Formulation and evaluation of anastrozole, an anti-cancer drug loaded in different biodegradable polymeric nanoparticles. Materials and methods Different carrier systems such as poly(lactide-co-glycolide) (PLGA 50:50), poly(lactic-acid) (PLA) and poly(ε-caprolactone) (PCL) are used to prepare nanoparticles by simple emulsion technique. The surfactants polyvinyl alcohol and sodium deoxycholate were studied for their use as stabilizing agents at varying concentrations. The formulations were studied for their particle size, zeta potential, entrapment efficiency and solid state characteristics, and also were tested for their in vitro cytotoxicity and in vivo behavior in rats. Key findings The entrapment ranged from 35 to 85%, depending on the drug-polymer ratio used. Particle size ranged from 100 to 350 nm with optimal zeta potential. Accordingly, discrete spherical nanoparticles with smooth surface were obtained as evidence from Field Emission Scanning Electron Microscopy (FESEM) study. The solid state characteristics revealed dispersion of drug at the molecular level in the polymeric matrix of nanoparticles. A non-Fickian transport with initial burst release followed by slow release was observed with nanoparticles. The remarkable decrease in cell viability at various time points was observed for PLGA nanoparticles compared to other polymer matrices. The AUC(0 → ∞) of PLGA, PLA and PCL nanoparticles were found to be 4.77, 19.31 and 19.81 fold higher than (p < 0.05) anastrozole in solution, respectively. Also, pharmacokinetics study revealed the long time circulation of anastrozole loaded polymeric nanoparticles. Significance The results suggest that developed nanoparticles could be used successfully for effective management of breast cancer chemotherapy.

AB - Aim Formulation and evaluation of anastrozole, an anti-cancer drug loaded in different biodegradable polymeric nanoparticles. Materials and methods Different carrier systems such as poly(lactide-co-glycolide) (PLGA 50:50), poly(lactic-acid) (PLA) and poly(ε-caprolactone) (PCL) are used to prepare nanoparticles by simple emulsion technique. The surfactants polyvinyl alcohol and sodium deoxycholate were studied for their use as stabilizing agents at varying concentrations. The formulations were studied for their particle size, zeta potential, entrapment efficiency and solid state characteristics, and also were tested for their in vitro cytotoxicity and in vivo behavior in rats. Key findings The entrapment ranged from 35 to 85%, depending on the drug-polymer ratio used. Particle size ranged from 100 to 350 nm with optimal zeta potential. Accordingly, discrete spherical nanoparticles with smooth surface were obtained as evidence from Field Emission Scanning Electron Microscopy (FESEM) study. The solid state characteristics revealed dispersion of drug at the molecular level in the polymeric matrix of nanoparticles. A non-Fickian transport with initial burst release followed by slow release was observed with nanoparticles. The remarkable decrease in cell viability at various time points was observed for PLGA nanoparticles compared to other polymer matrices. The AUC(0 → ∞) of PLGA, PLA and PCL nanoparticles were found to be 4.77, 19.31 and 19.81 fold higher than (p < 0.05) anastrozole in solution, respectively. Also, pharmacokinetics study revealed the long time circulation of anastrozole loaded polymeric nanoparticles. Significance The results suggest that developed nanoparticles could be used successfully for effective management of breast cancer chemotherapy.

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U2 - 10.1016/j.lfs.2015.09.021

DO - 10.1016/j.lfs.2015.09.021

M3 - Article

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SP - 143

EP - 155

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

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