Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine
The goal of this study was to optimize and formulate apigenin (APG)-loaded pegylated chitosan nanoparticles (PEGylated-CNPs) via ionic gelation techniques using the Box–Behnken design (BBD). Three individual variables, X<sub>1</sub>(chitosan: TPP concentration), X<sub>2</sub>...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-10-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/20/4344 |
| _version_ | 1811153722860896256 |
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| author | Md Ali Mujtaba Nawaf M. Alotaibi Sultan M. Alshehri Mohammad Yusuf Md Khalid Anwer Mohammad Akhlaquer Rahman Arshiya Parveen |
| author_facet | Md Ali Mujtaba Nawaf M. Alotaibi Sultan M. Alshehri Mohammad Yusuf Md Khalid Anwer Mohammad Akhlaquer Rahman Arshiya Parveen |
| author_sort | Md Ali Mujtaba |
| collection | DOAJ |
| description | The goal of this study was to optimize and formulate apigenin (APG)-loaded pegylated chitosan nanoparticles (PEGylated-CNPs) via ionic gelation techniques using the Box–Behnken design (BBD). Three individual variables, X<sub>1</sub>(chitosan: TPP concentration), X<sub>2</sub> (PEG-400 concentration), and X<sub>3</sub> (sonication time), were investigated for their influence on response variables (Y<sub>1</sub>—particle size (PS); Y<sub>2</sub>—drug entrapment efficiency (DEE); and Y<sub>3</sub>—zeta potential (ZP). The optimized formula of APG-PEGylated CNPs was picked from the statistical design and was then examined for physical, morphological, release characterization, anti-oxidant, and anti-tumor potential. The average PS, PDI, %DEE, and ZP were found to be 139.63 ± 5.67 nm, 0.296 ± 0.014, 79.55 ± 3.12%, and 24.68 ± 1.84 mV, respectively. The optimized APG formulation was chosen and reformulated based on the desirability function. Results of the observed and predicted values of responses through the BBD process were found to be nearly identical. The resulting APG-PEGylated CNPs were spherical and smooth, according to surface morphology studies. The release study revealed that PEGylated-CNPs exhibited biphasic release patterns distinguished by an initial burst release of APG only at early phases accompanied by a delayed release near 24 h. Furthermore, APG-PEGylated CNPs demonstrated statistically increased antioxidant activities and cytotoxicity against MCF-7 cells compared to pure APG. Based on the findings, it is possible to conclude that BBD was efficient in optimizing the PEGylated CNPs formulation and recognizing the impacts of formulation variables. In conclusion, the developed formulation has a significant potential for anticancer therapy. |
| first_indexed | 2024-03-09T19:33:07Z |
| format | Article |
| id | doaj.art-e17921a391bb4614b3f8590e625afd24 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T19:33:07Z |
| publishDate | 2022-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-e17921a391bb4614b3f8590e625afd242023-11-24T02:07:34ZengMDPI AGPolymers2073-43602022-10-011420434410.3390/polym14204344Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral NanomedicineMd Ali Mujtaba0Nawaf M. Alotaibi1Sultan M. Alshehri2Mohammad Yusuf3Md Khalid Anwer4Mohammad Akhlaquer Rahman5Arshiya Parveen6Department of Pharmaceutics, Faculty of Pharmacy, Northern Border University, Rafhaa 73213, Saudi ArabiaDepartment of Clinical Pharmacy, Faculty of Pharmacy, Northern Border University, Rafhaa 73213, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi ArabiaDepartment of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi ArabiaDepartment of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaThe goal of this study was to optimize and formulate apigenin (APG)-loaded pegylated chitosan nanoparticles (PEGylated-CNPs) via ionic gelation techniques using the Box–Behnken design (BBD). Three individual variables, X<sub>1</sub>(chitosan: TPP concentration), X<sub>2</sub> (PEG-400 concentration), and X<sub>3</sub> (sonication time), were investigated for their influence on response variables (Y<sub>1</sub>—particle size (PS); Y<sub>2</sub>—drug entrapment efficiency (DEE); and Y<sub>3</sub>—zeta potential (ZP). The optimized formula of APG-PEGylated CNPs was picked from the statistical design and was then examined for physical, morphological, release characterization, anti-oxidant, and anti-tumor potential. The average PS, PDI, %DEE, and ZP were found to be 139.63 ± 5.67 nm, 0.296 ± 0.014, 79.55 ± 3.12%, and 24.68 ± 1.84 mV, respectively. The optimized APG formulation was chosen and reformulated based on the desirability function. Results of the observed and predicted values of responses through the BBD process were found to be nearly identical. The resulting APG-PEGylated CNPs were spherical and smooth, according to surface morphology studies. The release study revealed that PEGylated-CNPs exhibited biphasic release patterns distinguished by an initial burst release of APG only at early phases accompanied by a delayed release near 24 h. Furthermore, APG-PEGylated CNPs demonstrated statistically increased antioxidant activities and cytotoxicity against MCF-7 cells compared to pure APG. Based on the findings, it is possible to conclude that BBD was efficient in optimizing the PEGylated CNPs formulation and recognizing the impacts of formulation variables. In conclusion, the developed formulation has a significant potential for anticancer therapy.https://www.mdpi.com/2073-4360/14/20/4344apigeninBox–Behnken designantioxidantchitosannanoparticles |
| spellingShingle | Md Ali Mujtaba Nawaf M. Alotaibi Sultan M. Alshehri Mohammad Yusuf Md Khalid Anwer Mohammad Akhlaquer Rahman Arshiya Parveen Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine Polymers apigenin Box–Behnken design antioxidant chitosan nanoparticles |
| title | Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine |
| title_full | Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine |
| title_fullStr | Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine |
| title_full_unstemmed | Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine |
| title_short | Novel Therapeutic Approach in PEGylated Chitosan Nanoparticles of Apigenin for the Treatment of Cancer via Oral Nanomedicine |
| title_sort | novel therapeutic approach in pegylated chitosan nanoparticles of apigenin for the treatment of cancer via oral nanomedicine |
| topic | apigenin Box–Behnken design antioxidant chitosan nanoparticles |
| url | https://www.mdpi.com/2073-4360/14/20/4344 |
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