Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation
Gemcitabine (Gem) and cisplatin (Cis) are currently being used for lung cancer treatment, but they are highly toxic in high dosages. This research aimed to develop a niosome formulation containing a low-dosage Gem and Cis (NGC), as an alternative formulation for lung cancer treatment. NGC was prepar...
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MDPI AG
2021-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/1/59 |
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| author | Norfatin Izzatie Mohamad Saimi Norazlinaliza Salim Noraini Ahmad Emilia Abdulmalek Mohd Basyaruddin Abdul Rahman |
| author_facet | Norfatin Izzatie Mohamad Saimi Norazlinaliza Salim Noraini Ahmad Emilia Abdulmalek Mohd Basyaruddin Abdul Rahman |
| author_sort | Norfatin Izzatie Mohamad Saimi |
| collection | DOAJ |
| description | Gemcitabine (Gem) and cisplatin (Cis) are currently being used for lung cancer treatment, but they are highly toxic in high dosages. This research aimed to develop a niosome formulation containing a low-dosage Gem and Cis (NGC), as an alternative formulation for lung cancer treatment. NGC was prepared using a very simple heating method and was further optimized by D-optimal mixture design. The optimum NGC formulation with particle size, polydispersity index (PDI), and zeta potential of 166.45 nm, 0.16, and −15.28 mV, respectively, was obtained and remained stable at 27 °C with no phase separation for up to 90 days. The aerosol output was 96.22%, which indicates its suitability as aerosolized formulation. An in vitro drug release study using the dialysis bag diffusion technique showed controlled release for both drugs up to 24 h penetration. A cytotoxicity study against normal lung (MRC5) and lung cancer (A549) cell lines was investigated. The results showed that the optimized NGC had reduced cytotoxicity effects against both MRC5 and A549 when compared with the control (Gem + Cis alone) from very toxic (IC<sub>50</sub> < 1.56 µg/mL) to weakly toxic (IC<sub>50</sub> 280.00 µg/mL) and moderately toxic (IC<sub>50</sub> = 46.00 µg/mL), respectively, after 72 h of treatment. These findings revealed that the optimized NGC has excellent potential and is a promising prospect in aerosolized delivery systems to treat lung cancer that warrants further investigation. |
| first_indexed | 2024-03-10T13:28:05Z |
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| id | doaj.art-731229ae8502407e98e2e0bd031bb44e |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T13:28:05Z |
| publishDate | 2021-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-731229ae8502407e98e2e0bd031bb44e2023-11-21T08:29:38ZengMDPI AGPharmaceutics1999-49232021-01-011315910.3390/pharmaceutics13010059Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro EvaluationNorfatin Izzatie Mohamad Saimi0Norazlinaliza Salim1Noraini Ahmad2Emilia Abdulmalek3Mohd Basyaruddin Abdul Rahman4Integrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang 43400 UPM, Selangor, MalaysiaIntegrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang 43400 UPM, Selangor, MalaysiaDepartment of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, MalaysiaIntegrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang 43400 UPM, Selangor, MalaysiaIntegrated Chemical BioPhysics Research, Faculty of Science, Universiti Putra Malaysia, Serdang 43400 UPM, Selangor, MalaysiaGemcitabine (Gem) and cisplatin (Cis) are currently being used for lung cancer treatment, but they are highly toxic in high dosages. This research aimed to develop a niosome formulation containing a low-dosage Gem and Cis (NGC), as an alternative formulation for lung cancer treatment. NGC was prepared using a very simple heating method and was further optimized by D-optimal mixture design. The optimum NGC formulation with particle size, polydispersity index (PDI), and zeta potential of 166.45 nm, 0.16, and −15.28 mV, respectively, was obtained and remained stable at 27 °C with no phase separation for up to 90 days. The aerosol output was 96.22%, which indicates its suitability as aerosolized formulation. An in vitro drug release study using the dialysis bag diffusion technique showed controlled release for both drugs up to 24 h penetration. A cytotoxicity study against normal lung (MRC5) and lung cancer (A549) cell lines was investigated. The results showed that the optimized NGC had reduced cytotoxicity effects against both MRC5 and A549 when compared with the control (Gem + Cis alone) from very toxic (IC<sub>50</sub> < 1.56 µg/mL) to weakly toxic (IC<sub>50</sub> 280.00 µg/mL) and moderately toxic (IC<sub>50</sub> = 46.00 µg/mL), respectively, after 72 h of treatment. These findings revealed that the optimized NGC has excellent potential and is a promising prospect in aerosolized delivery systems to treat lung cancer that warrants further investigation.https://www.mdpi.com/1999-4923/13/1/59niosomegemcitabinecisplatinheating methodlung canceraerosol output |
| spellingShingle | Norfatin Izzatie Mohamad Saimi Norazlinaliza Salim Noraini Ahmad Emilia Abdulmalek Mohd Basyaruddin Abdul Rahman Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation Pharmaceutics niosome gemcitabine cisplatin heating method lung cancer aerosol output |
| title | Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation |
| title_full | Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation |
| title_fullStr | Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation |
| title_full_unstemmed | Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation |
| title_short | Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation |
| title_sort | aerosolized niosome formulation containing gemcitabine and cisplatin for lung cancer treatment optimization characterization and in vitro evaluation |
| topic | niosome gemcitabine cisplatin heating method lung cancer aerosol output |
| url | https://www.mdpi.com/1999-4923/13/1/59 |
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