Enhancement of in vitro anti-inflammatory activity of aqueous leaf extract of Xanthium strumarium L. through encapsulation in chitosan nanoparticles
Abstract
Xanthium strumarium L. (Asteraceae) is a medicinally important plant widely documented for its anti-inflammatory, antirheumatic and anti-rhinitis activities. Chitosan is a noteworthy versatile, biopolymer in drug delivery due to its biocompatibility and efficacy in controlled drug release. The aim of the present investigation was to encapsulate aqueous leaf extract of X. strumarium (XS-ALE) using chitosan nanoparticles (CSNPs), determine the in vitro drug release kinetics and to evaluate the anti-inflammatory activity using various in vitro assays. The XS-ALE encapsulated CSNPs (XS-ALE CSNPs) were synthesized and their entrapment efficiency, drug release percentage, drug release kinetics, various characterization studies such as UV-Vis spectroscopy, FTIR, SEM, zetapotential and anti-inflammatory activity were assessed. The concentration (5µg/mL) with maximum entrapment efficiency percentage (64.80%) was selected for further drug release, characterization and anti-inflammatory assays. In vitro drug release studies demonstrated a controlled and sustained drug release of 70.96% within 3.5 hours. The drug release kinetics fit in to the Higuchi model, exhibiting a high correlation coefficient (R² = 0.97), which suggests a diffusion-regulated release mechanism. Fourier transform infrared (FTIR) spectral analysis confirmed the presence of characteristic functional groups accountable to both chitosan and the plant extract. XS-ALE CSNPs showed irregular morphology with a positive charge of +32.7 mV. XS-ALE CSNPs showed the highest percentage inhibition for both protein denaturation (79%) and proteinase inhibitory (82.46%) compared to CSNPs and the reference drugs. The outcomes of the study suggested the efficacy of using XS-ALE CSNPs at minimal concentrations as a potent biocompatible and eco-friendly anti-inflammatory agent.
Keywords: Xanthium strumarium, chitosan nanoparticles, anti-inflammatory activity, drug release kinetics
Keywords:
Xanthium strumarium, chitosan nanoparticles, drug release kineticsDOI
https://doi.org/10.22270/jddt.v16i6.7681References
1. Nel A, Xia T, Madler L, Li N, Toxic potential of materials at the nano level. Science, 2006; 311(5761): 622-627. DOI: https://doi.org/10.1126/science.1114397.
2. Gadad AP, Kumar SV, Dandagi PM, Bolmol UB, Pallavi NP, Nanoparticles and their therapeutic applications in pharmacy. Int. J. Pharm. Sci. Nanotechnol, 2014;7: 2509-2519. DOI: https://doi.org/10.37285/ijpsn.2014.7.3.2 .
3. Venkatesan J, Kim SK, Chitosan composites for bone tissue engineering-an overview. Marine drugs, 2010;8(8): 2252-2266. DOI: https://doi.org/10.3390/md8082252.
4. Kumar MR, Muzzarelli, R, Muzzarelli, C, Sashiva H, Domb AJ, Chitosan chemistry and pharmaceutical perspectives. Chemical Reviews, 2004; 104:6017-6084. DOI: https://doi.org/10.1021/cr030441b .
5. Alex A, Millan DS, Perez M, Wakenhut F, Whitlock GA, Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space. MedChemComm, 2011; 2(7): 669-674. DOI: https://doi.org/10.1039/C1MD00093D .
6. Ćirić A, Krajišnik D, Čalija B, Đekić L, Biocompatible non-covalent complexes of chitosan and different polymers: Characteristics and application in drug delivery. Arhiv za farmaciju, 2020; 70(4): 173-197. DOI: https://doi.org/10.5937/arhfarm2004173Q .
7. Ricciotti E, FitzGerald GA, Prostaglandins and inflammation. Arteriosclerosis, thrombosis, and vascular biology, 2011; 31(5): 986-1000. DOI: https://doi.org/10.1161/atvbaha.110.207449 .
8. Velnar T, Bailey T, Smrkolj V, The wound healing process: an overview of the cellular and molecular mechanisms. Journal of international medical research, 2009;37(5):1528-1542. DOI: https://doi.org/10.1177/147323000903700531 .
9. Singh G, Recent considerations in nonsteroidal anti-inflammatory drug gastropathy. The American journal of medicine, 1998;105(1):31S-38S. DOI: https://doi.org/10.1016/s0002-9343(98)00072-2 .
10. Griffin MR, Yared A, Ray WA, Nonsteroidal anti-inflammatory drugs and acute renal failure in elderly persons. American journal of epidemiology, 2000;151(5): 488-496. DOI: https://pubmed.ncbi.nlm.nih.gov/10707917/ .
11. Hossain MM, Ahamed SK, Dewan SMR, Hassan MM, Istiaq A, Islam MS, Moghal MMR, In vivo antipyretic, antiemetic, in vitro membrane stabilization, antimicrobial, and cytotoxic activities of different extracts from Spilanthes paniculata leaves. Biological Research, 2014; 47(1): 45. DOI :https://doi.org/10.1186/0717-6287-47-45 .
12. Chopra RN, Nayar SL, (1956). Glossary of Indian medicinal plants. Council of scientific and Industrial Research.
13. Kim IT, Park YM, Won JH, Jung HJ, Park HJ, Choi JW, Lee KT, Methanol extract of Xanthium strumarium L. possesses anti-inflammatory and anti-nociceptive activities. Biological and Pharmaceutical Bulletin, 2005; 28(1): 94-100. DOI: https://doi.org/10.1248/bpb.28.94 .
14. Menon GS, Kuchroo K, Dasgupta D, Interaction of microtubules with active principles of Xanthium strumarium. Physiological Chemistry and Physics and Medical NMR, 2001; 33(2):153-162. DOI: https://pubmed.ncbi.nlm.nih.gov/12002689/
15. Jiménez Nieves L, León Padilla MDC, Herrera Rodríguez R, García Simón G, Cadenas Freixas JL, Efecto diurético del Xanthium strumarium L.(guizazo de caballo). Revista Cubana de Plantas Medicinales, 1999;4(1): 22-25. https://www.researchgate.net/publication/262739814_Evaluacion_del_efecto_genotoxico_del_Xhantium_strumarium_L_Guisazo_de_Caballo .
16. ÇETİNSOY S, TAMER A, AYDEMİR M, Investigations on Repellent and Insecticidal Effects of Xanthium strumarium L. on Colorado Potato Beetle Leptinotrasa decemlineata Say (Col: Chrysomelidae). Turkish Journal of Agriculture and Forestry, 1998; 22(6): 543-552. https://journals.tubitak.gov.tr/cgi/viewcontent.cgi?article=2702&context=agriculture
17. Kim HS, Lee IS, Yeo SH, Seong LS, Yu TS, Isolation and characterization of antitumor agents from Xanthium strumarium L. Korean Journal of Biotechnology and Bioengineering, 2003;18(4).DOI:https://agris.fao.org/search/en/providers/122646/records/647243102c1d629bc9794120 .
18. Fouché G, Cragg GM, Pillay P, Kolesnikova N, Maharaj VJ, Senabe J, In vitro anticancer screening of South African plants. Journal of Ethnopharmacology, 2008;119 (3):455-461. DOI: https://doi.org/10.1016/j.jep.2008.07.005 .
19. Jawad AL, Mahmould MJ, Al-Naib A, Antimicrobial activity of Xanthium strumarium extract. Fitoterapia, 1988;59(3): 220-221.
20. Kishore N, Dubey NK, Tripathi RD, Singh SK. Fungi toxicity of the leaf extracts of some higher plants against Fusarium moniliforme. 1982;5(2) 43-45. DOI: https://www.cabidigitallibrary.org/doi/full/10.5555/19831389099 .
21. Talakal TS, Dwivedi SK, Sharma SR, In vitro and in vivo antitrypanosomal activity of Xanthium strumarium leaves. Journal of Ethnopharmacology, 1995;49(3):141-145. DOI: https://doi.org/10.1016/0378-8741(95)01313-x .
22. Anjoo Kamboj, AK, Pooja Atri PA, Saluja AK, Phytochemical screening, in-vitro evaluation of antioxidant and free radical scavenging activity of leaves, stems and roots of Xanthium strumarium L., (Compositae). Journal of Pharmaceutical Research International, 2013;1-22. DOI: https://doi.org/10.9734/BJPR/2014/3667 .
23. Kupiecki FP, Ogzewalla CD, Schell FM. Isolation and characterization of a hypoglycemic agent from Xanthium strumarium. Journal of Pharmaceutical Sciences, 1974; 63(7):1166-1167. DOI: https://doi.org/10.1002/jps.2600630736 .
24. Mandal SC, Boominathan R, Devi BP, Panda S, Studies on anti-tussive activity of Xanthium strumarium L. extract. In III WOCMAP Congress on Medicinal and Aromatic Plants-Volume 4: Targeted Screening of Medicinal and Aromatic Plants, Economics, 2003; 678: 149-152. DOI: https://doi.org/10.17660/ActaHortic.2005.678.20 .
25. Sultana A, Wahab A, Perveen R, Haider SS, FARHEEN R, ANWAR A, A brief review on phytochemistry and pharmacological activity of Xanthium strumarium L. FUUAST Journal of Biology, 2019;9(2): 271-276. DOI: https://doi.org/10.64793/fuuastjb.v9i2.421 .
26. Shivangi K, Kumari GD, Kumar GM, In-vitro evaluation of drug release and antioxidant activity of aloe loaded chitosan nanoparticles. Journal of Drug Delivery & Therapeutics, 2019;9(4). DOI: https://doi.org/10.22270/jddt.v9i4.2979 .
27. Bagyalakshmi J, Haritha H, Green synthesis and characterization of silver nanoparticles using Pterocarpus marsupium and assessment of its in vitro Antidiabetic activity. Am. J. Adv. Drug Deliv, 2017; 5(3):1-13. DOI https://www.primescholars.com/articles/green-synthesis-and-characterization-of-silver-nanoparticles-using-pterocarpus-marsupium-and-assessment-of-its-in-vitro-antidiabet.pdf .
28. Sultan MH, Moni SS, Madkhali OA, Bakkari MA, Alshahrani S, Alqahtani SS, Alshamrani M, Characterization of cisplatin-loaded chitosan nanoparticles and rituximab-linked surfaces as target-specific injectable nano-formulations for combating cancer. Scientific reports, 2022;12(1):468. DOI: https://www.nature.com/articles/s41598-021-04427-w .
29. Dash TK, Konkimalla VB, Poly-є-caprolactone based formulations for drug delivery and tissue engineering: A review. Journal of Controlled Release, 2012;158(1):15-33. DOI: https://doi.org/10.1016/j.jconrel.2011.09.064 .
30. Paarakh MP, Jose PA, Setty CM, Peterchristoper GV, Release kinetics-concepts and applications. International Journal of Pharmacy Research & Technology (IJPRT), 2018;8(1):12-20. DOI: https://doi.org/10.31838/ijprt/08.01.02 .
31. Gunathilake KDPP, Ranaweera KKDS, Rupasinghe HPV, Influence of boiling, steaming and frying of selected leafy vegetables on the in vitro anti-inflammation associated biological activities. Plants, 2018; 7(1):22. DOI: https://doi.org/10.3390/plants7010022 .
32. Sakat S, Tupe P, Juvekar A, Gastroprotective effect of methanol extract of Oxalis corniculata Linn (whole plant) experimental animals. Planta Medica, 2010;76(12):P090. DOI: https://doi.org/10.4103/0250-474x.102543 .
33. Mishra SS, Sharma A, Preparation and characterization of chitosan nanoparticles of insulin for nasal delivery. J. Drug Deliv. Ther, 2018; 8:400-406.DOI: https://doi.org/10.22270/jddt.v8i5-s.2002 .
34. Manne AA, Kumar A, Mangamuri U, Podha S, Pterocarpus marsupium Roxb. heartwood extract synthesized chitosan nanoparticles and its biomedical applications. Journal of Genetic Engineering and Biotechnology, 2020; 18(1):19. DOI: https://doi.org/10.1186/s43141-020-00033-x .
35. Youssef FS, El-Banna HA, Elzorba HY, Galal AM, Application of some nanoparticles in the field of veterinary medicine. International journal of veterinary science and medicine, 2019;7(1): 78-93. DOI: https://doi.org/10.1080/23144599.2019.1691379 .
36. Hariharan, CJACAG, Photocatalytic degradation of organic contaminants in water by ZnO nanoparticles: Revisited. Applied Catalysis A: General, 2006;304:55-61. DOI: https://doi.org/10.1016/j.apcata.2006.02.020 .
37. Arafa MG, Mousa HA, Afifi NN, Preparation of PLGA-chitosan based nanocarriers for enhancing antibacterial effect of ciprofloxacin in root canal infection. Drug Delivery, 2020;27(1), 26-39. DOI: https://doi.org/10.1080/10717544.2019.1701140
38. Mohamadpour H, Azadi A, Rostamizadeh K, Andalib S, Saghatchi Zanjani MR, Hamidi M, Preparation, optimization, and evaluation of methoxy poly (ethylene glycol)-co-poly (ε-caprolactone) nanoparticles loaded by rivastigmine for brain delivery. ACS chemical neuroscience, 2020;11(5): 783-795. DOI: https://doi.org/10.1021/acschemneuro.9b00691 .
39. Modi S, Anderson BD, Determination of drug release kinetics from nanoparticles: overcoming pitfalls of the dynamic dialysis method. Molecular pharmaceutics, 2013;10(8): 3076-3089. DOI: https://doi.org/10.1021/mp400154a .
40. D’Addio SM, Bukari AA, Dawoud M, Bunjes H, Rinaldi C, Prud’homme RK, Determining drug release rates of hydrophobic compounds from nanocarriers. Philosophical transactions of the royal society a: mathematical, physical and engineering sciences, 2016; 374(2072): 20150128. DOI: https://doi.org/10.1098/rsta.2015.0128 .
41. D’Souza S, A review of in vitro drug release test methods for nano‐sized dosage forms. Advances in pharmaceutics, 2014;2014(1):304757. DOI: https://doi.org/10.1155/2014/304757 .
42. Sreelatha S, Kumar N, Yin TS, Rajani S, Evaluating the antibacterial activity and mode of action of thymol-loaded chitosan nanoparticles against plant bacterial pathogen Xanthomonas campestris pv. campestris. Frontiers in Microbiology, 2022; 12:792737. DOI: https://doi.org/10.3389/fmicb.2021.792737 .
43. El-Naggar NEA, Eltarahony M, Hafez EE, Bashir SI. Green fabrication of chitosan nanoparticles using Lavendula angustifolia, optimization, characterization and in vitro antibiofilm activity. Scientific Reports, 2023;13(1):11127. DOI: https://doi.org/10.1038/s41598-023-37660-6 .
44. Eid MM, Characterization of Nanoparticles by FTIR and FTIR-Microscopy. In Handbook of consumer nanoproducts 2022; 1-30. Singapore: Springer Singapore. DOI: https://doi.org/10.1007/978-981-15-6453-6_89-1 .
45. Soltanzadeh M, Peighambardoust SH, Ghanbarzadeh B, Mohammadi M, Lorenzo J M, Chitosan nanoparticles as a promising nanomaterial for encapsulation of pomegranate (Punica granatum L.) peel extract as a natural source of antioxidants. Nanomaterials, 2021;11(6): 1439. DOI: https://doi.org/10.3390/nano11061439 .
46. Severino P, da Silva CF, da Silva MA, Santana MH, Souto EB, Chitosan cross-linked pentasodium tripolyphosphate micro/nanoparticles produced by ionotropic gelation. Sugar Tech, 2016;18(1): 49-54. DOI: https://doi.org/10.1007/s12355-014-0360-z .
47. Gobalan K, Sudharsan P, Reshma Devi R, Koperuncholan M, Sumithra D, Prabhu K, Vasanth S, Anti-inflammatory activity of Ocimum tenuiflorum L. leaf extract loaded chitosan nanoparticle as a drug carrier–an in vitro study. Europ. Chem. Bull, 2023;12: 1062-1084. DOI: https://doi.org/10.31838/ecb/2023.12.1.086 .
48. Shafqat O, Rehman Z, Shah MM, Ali SHB, Jabeen Z, Rehman S, Synthesis, structural characterization and in vitro pharmacological properties of betanin-encapsulated chitosan nanoparticles. Chemico-Biological Interactions, 2023;370:110291. DOI: https://doi.org/10.1016/j.cbi.2022.110291 .
49. Soualmia F, El Amri C, Serine protease inhibitors to treat inflammation: a patent review (2011-2016). Expert opinion on therapeutic patents, 2018;28(2):93-110. DOI: https://doi.org/10.1080/13543776.2018.1406478 .
50. Manoharan K, Chitra P, In vitro antioxidant, anti-inflammatory and antibacterial activities of microencapsulated Elaeocarpus tectorius (Lour.) Poir leaf extracts. Asian J. Biol. Life Sci, 2021;10:597.DOI: https://pdfs.semanticscholar.org/260d/2a3c66f8180f810bd1f4ecdee3b9512553a5.pdf
Published
Abstract Display: 0 
PDF Downloads: 0 PDF Downloads: 0 How to Cite
Issue
Section
Copyright (c) 2026 Gunachitra Pannerselvam 1, Sradha Sajeev , Kavimani Thangasamy , Kayalvizhi Duraisamy , Natesan Geetha
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
How to Cite
.