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Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method

Erlotinib hydrochloride, a selective tyrosine kinase inhibitor approved for treatment of non-small cell lung cancer firstly. Erlotinib classified as class II drugs in the Biopharmaceutical Classification System (BCS), which characterized by low solubility and high permeability. The aim of this study...

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Detalles Bibliográficos
Autores principales: Jahangiri, Azin, Khalilzad, Fakhronnesa, Barghi, Leila
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Oxford University Press 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8801718/
https://www.ncbi.nlm.nih.gov/pubmed/35111974
http://dx.doi.org/10.1093/biomethods/bpac001
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author Jahangiri, Azin
Khalilzad, Fakhronnesa
Barghi, Leila
author_facet Jahangiri, Azin
Khalilzad, Fakhronnesa
Barghi, Leila
author_sort Jahangiri, Azin
collection PubMed
description Erlotinib hydrochloride, a selective tyrosine kinase inhibitor approved for treatment of non-small cell lung cancer firstly. Erlotinib classified as class II drugs in the Biopharmaceutical Classification System (BCS), which characterized by low solubility and high permeability. The aim of this study was to enhance the dissolution rate of this drug. The binary solid dispersions of erlotinib: PVP prepared at different ratios (1:3, 1:5, and 1:8) by electrospray technique. The characterization of formulations performed using differential scanning calorimetery (DSC), Fourier transform infrared spectroscopy (FT-IR) and dissolution rate test. The dissolution results showed that the dissolution rate of erlotinib from binary solid dispersions improved in comparison to pure drug. FTIR spectrum results showed that all peaks of erlotinib functional groups are also observable in the prepared solid dispersions. The FTIR results demonstrated that there was no interaction between drug and polymer. DSC thermograms of the prepared solid dispersions showed no drug-related peak, which is probably related to reduced crystallinity and drug amorphization. Based on the obtained results, it can be concluded that the erlotinib solid dispersion systems displayed improved dissolution rate compared to the pure drug. This will likely lead to increased drug bioavailability.
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spelling pubmed-88017182022-02-01 Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method Jahangiri, Azin Khalilzad, Fakhronnesa Barghi, Leila Biol Methods Protoc Methods Article Erlotinib hydrochloride, a selective tyrosine kinase inhibitor approved for treatment of non-small cell lung cancer firstly. Erlotinib classified as class II drugs in the Biopharmaceutical Classification System (BCS), which characterized by low solubility and high permeability. The aim of this study was to enhance the dissolution rate of this drug. The binary solid dispersions of erlotinib: PVP prepared at different ratios (1:3, 1:5, and 1:8) by electrospray technique. The characterization of formulations performed using differential scanning calorimetery (DSC), Fourier transform infrared spectroscopy (FT-IR) and dissolution rate test. The dissolution results showed that the dissolution rate of erlotinib from binary solid dispersions improved in comparison to pure drug. FTIR spectrum results showed that all peaks of erlotinib functional groups are also observable in the prepared solid dispersions. The FTIR results demonstrated that there was no interaction between drug and polymer. DSC thermograms of the prepared solid dispersions showed no drug-related peak, which is probably related to reduced crystallinity and drug amorphization. Based on the obtained results, it can be concluded that the erlotinib solid dispersion systems displayed improved dissolution rate compared to the pure drug. This will likely lead to increased drug bioavailability. Oxford University Press 2022-01-27 /pmc/articles/PMC8801718/ /pubmed/35111974 http://dx.doi.org/10.1093/biomethods/bpac001 Text en © The Author(s) 2022. Published by Oxford University Press. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/4.0/), which permits unrestricted reuse, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Methods Article
Jahangiri, Azin
Khalilzad, Fakhronnesa
Barghi, Leila
Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
title Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
title_full Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
title_fullStr Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
title_full_unstemmed Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
title_short Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
title_sort dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method
topic Methods Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8801718/
https://www.ncbi.nlm.nih.gov/pubmed/35111974
http://dx.doi.org/10.1093/biomethods/bpac001
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