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Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer
OBJECTIVE: The objective of this study was to develop a novel 1 month depot paclitaxel (PTX) microspheres that give a sustained and complete drug release. MATERIALS AND METHODS: PTX loaded microspheres were prepared by o/w emulsion solvent evaporation technique using the blends of poly(lactic-co-gly...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Medknow Publications & Media Pvt Ltd
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3807978/ https://www.ncbi.nlm.nih.gov/pubmed/24167783 http://dx.doi.org/10.4103/2230-973X.119212 |
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author | Shiny, Jacob Ramchander, Thadkapally Goverdhan, Puchchakayala Habibuddin, Mohammad Aukunuru, Jithan Venkata |
author_facet | Shiny, Jacob Ramchander, Thadkapally Goverdhan, Puchchakayala Habibuddin, Mohammad Aukunuru, Jithan Venkata |
author_sort | Shiny, Jacob |
collection | PubMed |
description | OBJECTIVE: The objective of this study was to develop a novel 1 month depot paclitaxel (PTX) microspheres that give a sustained and complete drug release. MATERIALS AND METHODS: PTX loaded microspheres were prepared by o/w emulsion solvent evaporation technique using the blends of poly(lactic-co-glycolic acid) (PLGA) 75/25, polycaprolactone 14,000 and polycaprolactone 80,000. Fourier transform infrared spectroscopy was used to investigate drug excipient compatibility. Compatible blends were used to prepare F1-F6 microspheres, the process was characterised and the optimum formulation was selected based on the release. Optimised formulation was characterised for solid state of the drug using the differential scanning calorimetry (DSC) studies, surface morphology using the scanning electron microscopy (SEM), in vivo drug release, in vitro in vivo correlation (IVIVC) and anticancer activity. Anticancer activity of release medium was determined using the cell viability assay in Michigan Cancer Foundation (MCF-7) cell line. RESULTS: Blend of PLGA with polycaprolactone (Mwt 14,000) at a ratio of 1:1 (F5) resulted in complete release of the drug in a time frame of 30 days. F5 was considered as the optimised formulation. Incomplete release of the drug resulted from other formulations. The surface of the optimised formulation was smooth and the drug changed its solid state upon fabrication. The formulation also resulted in 1-month drug release in vivo. The released drug from F5 demonstrated anticancer activity for 1-month. Cell viability was reduced drastically with the release medium from F5 formulation. A 100% IVIVC was obtained with F5 formulation suggesting the authenticity of in vitro release, in vivo release and the use of the formulation in breast cancer. CONCLUSIONS: From our study, it was concluded that with careful selection of different polymers and their combinations, PTX 1 month depot formulation with 100% drug release and that can be used in breast cancer was developed. |
format | Online Article Text |
id | pubmed-3807978 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Medknow Publications & Media Pvt Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-38079782013-10-28 Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer Shiny, Jacob Ramchander, Thadkapally Goverdhan, Puchchakayala Habibuddin, Mohammad Aukunuru, Jithan Venkata Int J Pharm Investig Original Research Article OBJECTIVE: The objective of this study was to develop a novel 1 month depot paclitaxel (PTX) microspheres that give a sustained and complete drug release. MATERIALS AND METHODS: PTX loaded microspheres were prepared by o/w emulsion solvent evaporation technique using the blends of poly(lactic-co-glycolic acid) (PLGA) 75/25, polycaprolactone 14,000 and polycaprolactone 80,000. Fourier transform infrared spectroscopy was used to investigate drug excipient compatibility. Compatible blends were used to prepare F1-F6 microspheres, the process was characterised and the optimum formulation was selected based on the release. Optimised formulation was characterised for solid state of the drug using the differential scanning calorimetry (DSC) studies, surface morphology using the scanning electron microscopy (SEM), in vivo drug release, in vitro in vivo correlation (IVIVC) and anticancer activity. Anticancer activity of release medium was determined using the cell viability assay in Michigan Cancer Foundation (MCF-7) cell line. RESULTS: Blend of PLGA with polycaprolactone (Mwt 14,000) at a ratio of 1:1 (F5) resulted in complete release of the drug in a time frame of 30 days. F5 was considered as the optimised formulation. Incomplete release of the drug resulted from other formulations. The surface of the optimised formulation was smooth and the drug changed its solid state upon fabrication. The formulation also resulted in 1-month drug release in vivo. The released drug from F5 demonstrated anticancer activity for 1-month. Cell viability was reduced drastically with the release medium from F5 formulation. A 100% IVIVC was obtained with F5 formulation suggesting the authenticity of in vitro release, in vivo release and the use of the formulation in breast cancer. CONCLUSIONS: From our study, it was concluded that with careful selection of different polymers and their combinations, PTX 1 month depot formulation with 100% drug release and that can be used in breast cancer was developed. Medknow Publications & Media Pvt Ltd 2013 /pmc/articles/PMC3807978/ /pubmed/24167783 http://dx.doi.org/10.4103/2230-973X.119212 Text en Copyright: © International Journal of Pharmaceutical Investigation http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Research Article Shiny, Jacob Ramchander, Thadkapally Goverdhan, Puchchakayala Habibuddin, Mohammad Aukunuru, Jithan Venkata Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
title | Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
title_full | Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
title_fullStr | Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
title_full_unstemmed | Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
title_short | Development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
title_sort | development and evaluation of a novel biodegradable sustained release microsphere formulation of paclitaxel intended to treat breast cancer |
topic | Original Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3807978/ https://www.ncbi.nlm.nih.gov/pubmed/24167783 http://dx.doi.org/10.4103/2230-973X.119212 |
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