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Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment

Docetaxel has demonstrated extraordinary anticancer effects on lung cancer. However, lack of optimal bioavailability due to poor solubility and high toxicity at its therapeutic dose has hampered the clinical use of this anticancer drug. Development of nanoemulsion formulation along with biocompatibl...

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Main Authors: Asmawi, Azren Aida, Salim, Norazlinaliza, Ngan, Cheng Loong, Ahmad, Haslina, Abd. Malek, Emilia, Masarudin, Mas Jaffri, Abdul Rahman, Mohd Basyaruddin
Format: Article
Language:English
Published: Springer 2019
Online Access:http://psasir.upm.edu.my/id/eprint/72659/1/Excipient%20selection%20and%20aerodynamic%20characterization.pdf
http://psasir.upm.edu.my/id/eprint/72659/
https://link.springer.com/article/10.1007/s13346-018-0526-4#citeas
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spelling my.upm.eprints.726592020-11-23T07:48:40Z http://psasir.upm.edu.my/id/eprint/72659/ Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment Asmawi, Azren Aida Salim, Norazlinaliza Ngan, Cheng Loong Ahmad, Haslina Abd. Malek, Emilia Masarudin, Mas Jaffri Abdul Rahman, Mohd Basyaruddin Docetaxel has demonstrated extraordinary anticancer effects on lung cancer. However, lack of optimal bioavailability due to poor solubility and high toxicity at its therapeutic dose has hampered the clinical use of this anticancer drug. Development of nanoemulsion formulation along with biocompatible excipients aimed for pulmonary delivery is a potential strategy to deliver this poorly aqueous soluble drug with improved bioavailability and biocompatibility. In this work, screening and selection of pharmaceutically acceptable excipients at their minimal optimal concentration have been conducted. The selected nanoemulsion formulations were prepared using high-energy emulsification technique and subjected to physicochemical and aerodynamic characterizations. The formulated nanoemulsion had mean particle size and ζ-potential in the range of 90 to 110 nm and − 30 to − 40 mV respectively, indicating high colloidal stability. The pH, osmolality, and viscosity of the systems met the ideal requirement for pulmonary application. The DNE4 formulation exhibited slow drug release and excellent stability even under the influence of extreme environmental conditions. This was further confirmed by transmission electron microscopy as uniform spherical droplets in nanometer range were observed after storage at 45 ± 1 °C for 3 months indicating high thermal stability. The nebulized DNE4 exhibited desirable aerosolization properties for pulmonary delivery application and found to be more selective on human lung carcinoma cell (A549) than normal cell (MRC-5). Hence, these characteristics make the formulation a great candidate for the potential use as a carrier system for docetaxel in targeting lung cancer via pulmonary delivery. Springer 2019 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/72659/1/Excipient%20selection%20and%20aerodynamic%20characterization.pdf Asmawi, Azren Aida and Salim, Norazlinaliza and Ngan, Cheng Loong and Ahmad, Haslina and Abd. Malek, Emilia and Masarudin, Mas Jaffri and Abdul Rahman, Mohd Basyaruddin (2019) Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment. Drug Delivery and Translational Research, 9. pp. 543-554. ISSN 2190-393X; ESSN: 2190-3948 https://link.springer.com/article/10.1007/s13346-018-0526-4#citeas 10.1007/s13346-018-0526-4
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description Docetaxel has demonstrated extraordinary anticancer effects on lung cancer. However, lack of optimal bioavailability due to poor solubility and high toxicity at its therapeutic dose has hampered the clinical use of this anticancer drug. Development of nanoemulsion formulation along with biocompatible excipients aimed for pulmonary delivery is a potential strategy to deliver this poorly aqueous soluble drug with improved bioavailability and biocompatibility. In this work, screening and selection of pharmaceutically acceptable excipients at their minimal optimal concentration have been conducted. The selected nanoemulsion formulations were prepared using high-energy emulsification technique and subjected to physicochemical and aerodynamic characterizations. The formulated nanoemulsion had mean particle size and ζ-potential in the range of 90 to 110 nm and − 30 to − 40 mV respectively, indicating high colloidal stability. The pH, osmolality, and viscosity of the systems met the ideal requirement for pulmonary application. The DNE4 formulation exhibited slow drug release and excellent stability even under the influence of extreme environmental conditions. This was further confirmed by transmission electron microscopy as uniform spherical droplets in nanometer range were observed after storage at 45 ± 1 °C for 3 months indicating high thermal stability. The nebulized DNE4 exhibited desirable aerosolization properties for pulmonary delivery application and found to be more selective on human lung carcinoma cell (A549) than normal cell (MRC-5). Hence, these characteristics make the formulation a great candidate for the potential use as a carrier system for docetaxel in targeting lung cancer via pulmonary delivery.
format Article
author Asmawi, Azren Aida
Salim, Norazlinaliza
Ngan, Cheng Loong
Ahmad, Haslina
Abd. Malek, Emilia
Masarudin, Mas Jaffri
Abdul Rahman, Mohd Basyaruddin
spellingShingle Asmawi, Azren Aida
Salim, Norazlinaliza
Ngan, Cheng Loong
Ahmad, Haslina
Abd. Malek, Emilia
Masarudin, Mas Jaffri
Abdul Rahman, Mohd Basyaruddin
Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
author_facet Asmawi, Azren Aida
Salim, Norazlinaliza
Ngan, Cheng Loong
Ahmad, Haslina
Abd. Malek, Emilia
Masarudin, Mas Jaffri
Abdul Rahman, Mohd Basyaruddin
author_sort Asmawi, Azren Aida
title Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
title_short Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
title_full Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
title_fullStr Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
title_full_unstemmed Excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
title_sort excipient selection and aerodynamic characterization of nebulized lipid-based nanoemulsion loaded with docetaxel for lung cancer treatment
publisher Springer
publishDate 2019
url http://psasir.upm.edu.my/id/eprint/72659/1/Excipient%20selection%20and%20aerodynamic%20characterization.pdf
http://psasir.upm.edu.my/id/eprint/72659/
https://link.springer.com/article/10.1007/s13346-018-0526-4#citeas
_version_ 1684654746653163520
score 13.211869

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