FABRICATION AND CHARACTERIZATION OF CHITOSAN NANOPARTICLES FOR EFFICIENT DELIVERY OF KAEMPFEROL IN BREAST AND CERVICAL CANCER TREATMENT
DOI:
https://doi.org/10.22159/ajpcr.2025v18i8.54428Keywords:
Kaempferol,, Chitosan, Nanoparticles, Box–Behnken design, MTT assayAbstract
Objectives: The goal of the present study was to use factorial design to prepare and optimize chitosan nanoparticles loaded with kaempferol for targeted drug delivery. A systematic investigation was conducted into the effects of major preparation variables, polymer amount, sodium tripolyphosphate (TPP) quantity, and stirring speed on drug content, encapsulation efficiency, and cumulative drug release (CDR).
Methods: Using TPP as a cross-linker and chitosan as a biodegradable polymer, kaempferol-loaded chitosan nanoparticles were created through an altered ionic gelation process. The formulation parameters were optimized using a factorial design. A number of nanoparticle characteristics, such as CDR, encapsulation effectiveness, and particle size, were described. A scanning electron microscope was used to investigate the prepared nanoparticles morphology. In addition, the MTT assay was used to evaluate cytotoxicity on the MCF-7 and HeLa human cancer cell line for breast and cervical cancer.
Results: Particle size of 112.5 nm, drug content of 96.63±0.531%, encapsulation efficiency of 89.45±0.311%, cumulative drug release (CDR) of 94.63±0.03%, zeta potential of −24.2 mV, and polydispersity index of 0.192 are all characteristics of the optimal formulation. The nanoparticles’ spherical shape was revealed by the scanning electron microscope results. Studies on in vitro cytotoxicity revealed that the chitosan nanoparticles loaded with kaempferol demonstrated strong anticancer properties, with IC50 values of 68.00 μg/mL for HeLa cell lines and 55.00 μg/mL for MCF-7. The significant p-values were found to be 0.0480, 0.0191, and 0.0372 for all responses. The formulations were included based on chitosan (≥85% deacetylation), kaempferol (≥98% purity), and nanoparticle formulations with size <200 nm, PDI ≤0.3, drug content ≥80%, and encapsulation efficiency ≥70%. Only actively growing, uncontaminated HeLa, and MCF-7 cells (≥95% viability, passages 3–10) were used for cytotoxicity studies.
Conclusion: Therefore, it is possible that the newly discovered nanoparticles for the treatment of breast and cervical cancer represent a ground-breaking approach. These findings significantly support the possibility of using these nanoparticles as a therapeutic treatment for breast and cervical cancer patients undergoing or following resection of malignant lesions.
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References
1. Hosseini A, Alipour A, Baradaran Rahimi V, Askari VR. A comprehensive and mechanistic review on protective effects of kaempferol against natural and chemical toxins: role of NF‐κB inhibition and Nrf2 activation. BioFactors. 2023;49(2):322-50. doi: 10.1002/biof.1923, PMID 36471898
2. Wang X, Zhao Y, Liu L, Li J, Li X. Anti-inflammatory mechanisms of kaempferol in chronic diseases. Int Immunopharmacol. 2023;113:109417. doi: 10.1016/j.intimp.2023.109417
3. Kumar S, Kaempferol PA. A dietary flavonoid with promising anticancer properties. Pharmacol Res. 2023;190:106682. doi: 10.1016/j. phrs.2023.106682
4. Kamisah Y, Jalil J, Yunos NM, Zainalabidin S. Cardioprotective properties of kaempferol: A review. Plants (Basel). 2023;12(11):2096. doi: 10.3390/plants12112096, PMID 37299076
5. Zhang W, Liu Q, Zhao M, Xu L, Huang R. Neuroprotective effects of kaempferol in models of neurodegenerative diseases. Neurochem Int. 2023;160:105420. doi: 10.1016/j.neuint.2023.105420
6. Singh D, Patel M, Rana A. Kaempferol as a potential therapeutic agent for diabetes management. J Ethnopharmacol. 2023;310:116345. doi: 10.1016/j.jep.2023.116345
7. Xu Y, Zhang J, Zhang R, Hu X, Lu X. In vitro antibacterial activity of kaempferol and its synergistic effect with colistin against colistin-resistant Gram-negative bacteria. J Appl Microbiol. 2021;131(3):1158-70. doi: 10.1111/jam.14991
8. Tang SM, Deng XT, Zhou J, Li QP, Ge XX, Miao L. Pharmacological basis and new insights of quercetin action in respect to its anti-cancer effects. Biomed Pharmacother. 2020;121:109604. doi: 10.1016/j. biopha.2019.109604, PMID 31733570
9. Imran M, Salehi B, Sharifi-Rad J, Aslam Gondal T, Saeed F, Imran A, et al. Kaempferol: A key emphasis to its anticancer potential. Molecules. 2019;24(12):2277. doi: 10.3390/molecules24122277, PMID 31248102
10. Srinivas Murthy BR, Yelavarthi PR, Devanna N. Process of orlistat-loaded chitosan nanoparticles using Box-Behnken design - an evaluation study. Asian J Pharm Clin Res. 2021;14(5):103-11. doi: 10.22159/ajpcr.2021.v14i5.41441
11. Jomy S, Muddasir S. Formulation, optimization, and characterization of biocompatible inhalable D-cycloserine-loaded alginate-chitosan nanoparticles for pulmonary drug delivery. Asian J Pharm Clin Res. 2016;9 Suppl 2:82-95.
12. Jacob V, Rajiv P. In vitro analysis: The antimicrobial and antioxidant activity of zinc oxide nanoparticles from Curcuma longa. Asian J Pharm Clin Res. 2019;12(1):200-4. doi: 10.22159/ajpcr.2019.v12i1.28808
13. Wikantyasning ER, Mazidah Z, Da’i M, Kusumawati IT, Suprapto S. Anticancer studies of zerumbone-loaded chitosan-oleic acid nanoparticles against T47D breast cancer cells. Int J App Pharm. 2024;16(6):66-71. doi: 10.22159/ijap.2024.v16s6.TY2036
14. Gomes AS, Simplicio SS, Gonsalves JK. Chitosan nanoparticles as a potential drug delivery system in the skin: A systematic review based on in vivo studies. Chem Select. 2024;9:e202402058. doi: 10.1002/ slct.202402058
15. Radhakrishnan J, Suma S, Nair AS, Ramachandran R. Curcumin-loaded chitosan-coated 5-fluorouracil encapsulated nanozeolitic imidazolate framework for combination cancer therapy. J Pharm Innov. 2023;18:2043-53. doi: 10.1007/s12247-023-09770-1
16. Sangnim T, Dheer D, Jangra N, Huanbutta K, Puri V, Sharma A. Chitosan in oral drug delivery formulations: A review. Pharmaceutics. 2023;15(9):2361. doi: 10.3390/pharmaceutics15092361
17. Liu X, Zhang H, Chen Y, Xu L, Yang S, Feng Y. Kaempferol role in modulating oxidative stress in metabolic disorders. Free Radic Biol Med. 2023;193:123-32. doi: 10.1016/j.freeradbiomed.2023.01.012
18. Zhou Y, Zhang X, Wang L, Chen J, Liu Y, Huang Q, et al. Kaempferol inhibits cancer cell proliferation by targeting the PI3K/Akt pathway. Mol Cancer Ther. 2023;22(1):45-55. doi: 10.1158/1535-7163.MCT-22- 0456
19. Zhang L, Huang Q, Li Y. Kaempferol attenuates liver fibrosis via TGF-β1/Smad signaling pathway inhibition. Phytol Med. 2023;115:154789. doi: 10.1016/j.phymed.2023.154789
20. Gao Y, Zhang T, Li M. Kaempferol suppresses tumor angiogenesis by down regulating VEGF expression. Cancer Lett. 2023;560:215-23. doi: 10.1016/j.canlet.2023.01.012
21. Mehta A, Hanini A, Shah A, Bhatt P, Pathak Y. Advancements in chitosan-based nanoparticles for targeted drug delivery. Carbohydr Poly. 2023;301:120123. doi: 10.1016/j.carbpol.2023.120123
22. Verma S, Gupta M, Sharma P, Mishra V, Jain K. Chitosan nanoparticles: A versatile platform for drug delivery. J Control Release. 2023;355:123- 36. doi: 10.1016/j.jconrel.2023.01.045
23. Chen X, Liu J, Zhang Q, Xu T, Huang Y. Chitosan-based nanocarriers for cancer therapy: Recent advances and challenges. Colloids Surf B Biointerfaces. 2023;218:112743.
24. Chen L, Huang M, Zhao Q, Feng Y, Li T. Chitosan nanoparticles for mucosal drug delivery. Inter Pharma. 2023;628:122345. doi: 10.1016/j. ijpharm.2023.122345
25. Li Q, Zhang W, Huang R, Zhao M, Feng L, Xu T, Yang L. Chitosan nanoparticles in cancer therapy: A review. J Biomed Mater Res A. 2023;111(3):567-78. doi: 10.1002/jbm.a.37480
26. Verma R, Kumar A, Patel M, Joshi R, Chauhan D. Kaempferol-loaded chitosan nanoparticles: A promising strategy for cancer therapy. J Drug Deliv Sci Technol. 2023;81:104123. doi: 10.1016/j.jddst.2022.104123
27. Kumar V, Patel A, Joshi M, Chauhan R, Gupta P. Kaempferol-loaded chitosan nanoparticles: Formulation, characterization and in vitro evaluation for cancer treatment. J Mol Liq. 2023;384:122003. doi: 10.1016/j.molliq.2023.122003
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