Volume : 13, Issue : 06, June – 2026
Title:
OPTIMIZATION AND CHARACTERIZATION OF KAEMPFEROL PHYTOSOMES VIA QUALITY BY DESIGN APPROACH
Authors :
Shaik Bajula, Srikala Kamireddy*
Abstract :
Background: A plant-derived flavonoid called Kaempferol has a lot of potential as an antidiabetic medication. Its therapeutic effectiveness is, however, restricted by its low water solubility and limited absorption. The pharmacological efficacy and absorption of Kaempferol can be improved by the creation of phytosomes.
Aim: The major goal of this effort is to improve the bioavailability of Kaempferol phytosomes by developing and optimizing them utilizing QBD technology.
Materials and Methods: L-α phosphatidylcholine was used as the lipid carrier in the rotary evaporation process to create phytosomes. To find out how the molar ratio, reaction duration and reaction temperature affected the system’s performance, the formulation was refined using a Box-Behnken experimental design. The optimal formulation was determined by evaluating the generated phytosomes based on Zeta potential, drug loading, particle size, and entrapment efficiency.
Results: The new formulation exhibited strong drug encapsulation, nanoscale size, high colloidal stability and uniformity, with an entrapment deficiency of 84.03%, particles size of 195 nm, zeta potential -29.09 MV, and drug loading of 19.39%. In vitro drug release test revealed that the phytosomal formulation produced a more dramatic, increased and sustained release profile of Kaempferol than the pure drug. The optimal formulation parameters were obtained at a 2:1 molar ratio, a reaction time of 67.45 minutes, and an operating temperature of 49.78°C and they are confirmed using overlay plot analysis.
Conclusion: These results demonstrate the potential of this strategy to enhance the administration of poorly soluble phytoconstituents, including Kaempferol, for anti-diabetic treatment and validate the effective use of BBD in modifying phytosomal formulations.
key words: QbD, BBD, entrapment efficiency, Kaempferol, diabetic.
Cite This Article:
Please cite this article in press Srikala kamireddy et al., Optimization And Characterization Of Kaempferol Phytosomes Via Quality By Design Approach, Indo Am. J. P. Sci, 2026; 13(06).
REFERENCES:
1. Den Hartogh DJ, Tsiani E. Antidiabetic properties of Kaempferol: A citrus fruit polyphenol. Biomolecules. 2019 Mar;9(3):99.
2. Bhia M, Motallebi M, Abadi B, Zarepour A, Pereira-Silva M, Saremnejad F, Santos AC, Zarrabi A, Melero A, Jafari SM, Shakibaei M. Kaempferol nano-delivery systems and their therapeutic applications. Pharmaceutics. 2021 Feb 23;13(2):291.
3. Barani M, Sangiovanni E, Angarano M, Rajizadeh MA, Mehrabani M, Piazza S, Gangadharappa HV, Pardakhty A, Mehrbani M, Dell’Agli M, Nematollahi MH. Phytosomes as innovative delivery systems for phytochemicals: A comprehensive review of literature. International journal of nanomedicine. 2021 Oct 15:6983-7022.
4. Metkari V, Shah R, Salunkhe N, Gurav S. QBD approach for the design, optimization, development, and characterization of Kaempferol-loaded phytosomes to enhance solubility and oral bioavailability. Journal of Pharmaceutical Innovation. 2023 Dec;18(4):2083-97.
5. Mirzaei H, Shakeri A, Rashidi B, Jalili A, Banikazemi Z, Sahebkar A. Phytosomal curcumin: A review of pharmacokinetic, experimental and clinical studies. Biomedicine & Pharmacotherapy. 2017 Jan 1;85:102-12.
6. Toma L, Deleanu M, Sanda GM, Barbălată T, Niculescu LŞ, Sima AV, Stancu CS. Bioactive compounds formulated in phytosomes administered as complementary therapy for metabolic disorders. International journal of molecular sciences. 2024 Apr 9;25(8):4162.
7. Namjoshi S, Dabbaghi M, Roberts MS, Grice JE, Mohammed Y. Quality by design: Development of the quality target product profile (QTPP) for semisolid topical products. Pharmaceutics. 2020 Mar 23;12(3):287.
8. Naman S, Baldi A. Quality-by-Design Perspectives of Phytosomes for Pharmaceutical Benefits. InAdvances in Novel Phytopharmaceuticals 2024 Dec 19 (pp. 230-245). CRC Press.
9. Belwal T, Bhatt ID, Rawal RS, Pande V. Microwave-assisted extraction (MAE) conditions using polynomial design for improving antioxidant phytochemicals in Berberis asiatica Roxb. ex DC. leaves. Industrial Crops and Products. 2017 Jan 1;95:393-403.
10. Metkari V, Shah R, Salunkhe N, Gurav S. QBD approach for the design, optimization, development, and characterization of Kaempferol-loaded phytosomes to enhance solubility and oral bioavailability. Journal of Pharmaceutical Innovation. 2023 Dec;18(4):2083-97.
11. Yu Z, Liu X, Chen H, Zhu L. Kaempferol-loaded dipalmitoylphosphatidylcholine phytosome dry powders for inhaled treatment of acute lung injury. Journal of aerosol medicine and pulmonary drug delivery. 2020 Aug 1;33(4):194-204.
12. Pazzi J, Subramaniam AB. Dynamics of giant vesicle assembly from thin lipid films. Journal of Colloid and Interface Science. 2024 May 1;661:1033-45.
13. Telange DR, Sohail NK, Hemke AT, Kharkar PS, Pethe AM. Phospholipid complex-loaded self-assembled phytosomal soft nanoparticles: evidence of enhanced solubility, dissolution rate, ex vivo permeability, oral bioavailability, and antioxidant potential of mangiferin. Drug Delivery and Translational Research. 2021 Jun;11(3):1056-83.
14. Cuadra II RE, Uy MM, Aseniero MI. Sustainable valorization, synthesis, and characterization of nanocellulose from industrial waste abaca fibers (iWAFs). Nano-Structures & Nano-Objects. 2026 Feb 1;45:101612.
15. Cordenonsi LM, Bromberger NG, Raffin RP, Scherman EE. Simultaneous separation and sensitive detection of naringin and Kaempferol in nanoparticles by chromatographic method indicating stability and photodegradation kinetics. Biomedical chromatography. 2016 Feb;30(2):155-62.
16. Decker JE, Hight Walker AR, Bosnick K, Clifford CA, Dai L, Fagan J, Hooker S, Jakubek ZJ, Kingston C, Makar J, Mansfield E. Sample preparation protocols for realization of reproducible characterization of single-wall carbon nanotubes. Metrologia. 2009 Dec 1;46(6):682-92.
17. Nashaat D, Elsabahy M, Hassanein KM, El-Gindy GA, Ibrahim EH. Development and in vivo evaluation of therapeutic phytosomes for alleviation of rheumatoid arthritis. International journal of pharmaceutics. 2023 Sep 25;644:123332.
18. Human C, Aucamp M, de Beer D, van Der Rijst M, Joubert E. Food‐grade phytosome vesicles for nanoencapsulation of labile C‐glucosylated xanthones and dihydrochalcones present in a plant extract matrix—Effect of process conditions and stability assessment. Food Science & Nutrition. 2023 Dec;11(12):8093-111.
19. Wan X, Wang W, Liu J, Tong T. Estimating the sample mean and standard deviation from the sample size, median, range and/or interquartile range. BMC medical research methodology. 2014 Dec 19;14(1):135.
20. Peanparkdee M, Yooying R. Enhancement of solubility, thermal stability and bioaccessibility of vitexin using phosphatidylcholine-based phytosome. NFS Journal. 2023 Jun 1;31:28-38.
21. Matias D, Rijo P, Pinto Reis C. Phytosomes as biocompatible carriers of natural drugs. Current Medicinal Chemistry. 2017 Feb 1;24(6):568-89.
22. Omidfar F, Gheybi F, Davoodi J, Amirinejad M, Badiee A. Nanophytosomes of hesperidin and of hesperetin: Preparation, characterization, and in vivo evaluation. Biotechnology and Applied Biochemistry. 2023 Apr;70(2):846-56.
23. Huang W, Yang C, Miao N, Lin C, Xu W, Marcelli A, Wei H. A novel temperature-dependent electrochemical system for electrode materials for time resolved X-ray diffraction. Scripta Materialia. 2022 Apr 1;211:114529.
24. Singh RP, Gangadharappa HV, Mruthunjaya K. Phytosome complexed with chitosan for gingerol delivery in the treatment of respiratory infection: In vitro and in vivo evaluation. European Journal of Pharmaceutical Sciences. 2018 Sep 15;122:214-29.
25. Mneimneh AT, Hayar B, Al Hadeethi S, Darwiche N, Mehanna MM. Application of Box-Behnken design in the optimization and development of albendazole-loaded zein nanoparticles as a drug repurposing approach for colorectal cancer management. International Journal of Biological Macromolecules. 2024 Nov 1;281:136437.