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Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations

BACKGROUND: Piroxicam exhibits low oral bioavailability, due to its meager solubility in water. The intent of this study was to ameliorate the bioavailability of the drug by employing a solubility-enhancing encapsulation technique. METHODS: Seven samples were formulated with piroxicam and gelatin us...

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Autores principales: Zhao, Lin, Mustapha, Omer, Shafique, Shumaila, Jamshaid, Talha, Din, Fakhar ud, Mehmood, Yasir, Anwer, Khaleeq, Yousafi, Qurrat ul Ain, Hussain, Talib, Khan, Ikram Ullah, Ghori, Muhammad Usman, Shahzad, Yasser, Yousaf, Abid Mehmood
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7667701/
https://www.ncbi.nlm.nih.gov/pubmed/33204090
http://dx.doi.org/10.2147/IJN.S271938
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author Zhao, Lin
Mustapha, Omer
Shafique, Shumaila
Jamshaid, Talha
Din, Fakhar ud
Mehmood, Yasir
Anwer, Khaleeq
Yousafi, Qurrat ul Ain
Hussain, Talib
Khan, Ikram Ullah
Ghori, Muhammad Usman
Shahzad, Yasser
Yousaf, Abid Mehmood
author_facet Zhao, Lin
Mustapha, Omer
Shafique, Shumaila
Jamshaid, Talha
Din, Fakhar ud
Mehmood, Yasir
Anwer, Khaleeq
Yousafi, Qurrat ul Ain
Hussain, Talib
Khan, Ikram Ullah
Ghori, Muhammad Usman
Shahzad, Yasser
Yousaf, Abid Mehmood
author_sort Zhao, Lin
collection PubMed
description BACKGROUND: Piroxicam exhibits low oral bioavailability, due to its meager solubility in water. The intent of this study was to ameliorate the bioavailability of the drug by employing a solubility-enhancing encapsulation technique. METHODS: Seven samples were formulated with piroxicam and gelatin using both solvent evaporation and electrospraying together. Evaluation of solubility and release rate in water and assessment of bioavailability in rats were carried out in comparison with piroxicam plain drug powder (PPDP). Other in vitro explorations were accomplished using powder X-ray diffraction analysis, differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, and Fourier-transform infrared spectroscopy. RESULTS: All piroxicam-loaded gelatinnanocontainers (PLGNs) enhanced solubility and release of the payload in water. In particular, a PLGN formulation consisting of piroxicam and gelatin at a 1:8 (w:w) ratio presented about 600-fold the drug solubility of that shown by PPDP. Moreover, 85.12%±10.96% of the payload was released from this formulation in 10 minutes which was significantly higher than that dissolved from PPDP in 10 minutes (11.81%±5.34%). Drug content, drug loading, and encapsulation efficiency of this formulation were 93.41%±0.56%, 10.45%±0.06%, and 66.74%±6.87%, respectively. The drug loaded in PLGNs existed in the amorphous state, as confirmed by X-ray diffraction and differential scanning–calorimetry analyses, and was more stable when analyzed by thermogravimetric analysis. Moreover, Fourier-transform infrared spectroscopy analysis suggested nonexistence of any piroxicam–gelatin interaction in the formulation. In the scanning electron–microscopy image, PLGNs appeared as round, smooth particles, with particle size of <1,000 nm. Amelioration in bioavailability of piroxicam with the aforementioned PLGN formulation was fourfold that of PPDP. CONCLUSION: The PLGN formulation fabricated with piroxicam and gelatin at 1:8 (w:w) might be a promising system for enhanced biopharmaceutical performance of the drug.
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spelling pubmed-76677012020-11-16 Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations Zhao, Lin Mustapha, Omer Shafique, Shumaila Jamshaid, Talha Din, Fakhar ud Mehmood, Yasir Anwer, Khaleeq Yousafi, Qurrat ul Ain Hussain, Talib Khan, Ikram Ullah Ghori, Muhammad Usman Shahzad, Yasser Yousaf, Abid Mehmood Int J Nanomedicine Original Research BACKGROUND: Piroxicam exhibits low oral bioavailability, due to its meager solubility in water. The intent of this study was to ameliorate the bioavailability of the drug by employing a solubility-enhancing encapsulation technique. METHODS: Seven samples were formulated with piroxicam and gelatin using both solvent evaporation and electrospraying together. Evaluation of solubility and release rate in water and assessment of bioavailability in rats were carried out in comparison with piroxicam plain drug powder (PPDP). Other in vitro explorations were accomplished using powder X-ray diffraction analysis, differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, and Fourier-transform infrared spectroscopy. RESULTS: All piroxicam-loaded gelatinnanocontainers (PLGNs) enhanced solubility and release of the payload in water. In particular, a PLGN formulation consisting of piroxicam and gelatin at a 1:8 (w:w) ratio presented about 600-fold the drug solubility of that shown by PPDP. Moreover, 85.12%±10.96% of the payload was released from this formulation in 10 minutes which was significantly higher than that dissolved from PPDP in 10 minutes (11.81%±5.34%). Drug content, drug loading, and encapsulation efficiency of this formulation were 93.41%±0.56%, 10.45%±0.06%, and 66.74%±6.87%, respectively. The drug loaded in PLGNs existed in the amorphous state, as confirmed by X-ray diffraction and differential scanning–calorimetry analyses, and was more stable when analyzed by thermogravimetric analysis. Moreover, Fourier-transform infrared spectroscopy analysis suggested nonexistence of any piroxicam–gelatin interaction in the formulation. In the scanning electron–microscopy image, PLGNs appeared as round, smooth particles, with particle size of <1,000 nm. Amelioration in bioavailability of piroxicam with the aforementioned PLGN formulation was fourfold that of PPDP. CONCLUSION: The PLGN formulation fabricated with piroxicam and gelatin at 1:8 (w:w) might be a promising system for enhanced biopharmaceutical performance of the drug. Dove 2020-11-10 /pmc/articles/PMC7667701/ /pubmed/33204090 http://dx.doi.org/10.2147/IJN.S271938 Text en © 2020 Zhao et al. http://creativecommons.org/licenses/by-nc/3.0/ This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
spellingShingle Original Research
Zhao, Lin
Mustapha, Omer
Shafique, Shumaila
Jamshaid, Talha
Din, Fakhar ud
Mehmood, Yasir
Anwer, Khaleeq
Yousafi, Qurrat ul Ain
Hussain, Talib
Khan, Ikram Ullah
Ghori, Muhammad Usman
Shahzad, Yasser
Yousaf, Abid Mehmood
Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations
title Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations
title_full Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations
title_fullStr Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations
title_full_unstemmed Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations
title_short Electrospun Gelatin Nanocontainers for Enhanced Biopharmaceutical Performance of Piroxicam: In Vivo and In Vitro Investigations
title_sort electrospun gelatin nanocontainers for enhanced biopharmaceutical performance of piroxicam: in vivo and in vitro investigations
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7667701/
https://www.ncbi.nlm.nih.gov/pubmed/33204090
http://dx.doi.org/10.2147/IJN.S271938
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