• MADHAVI M. GITAM School of Pharmacy, GITAM Deemed to be University, Hyderabad 502329, Telangana, India
  • SHIVA KUMAR G. GITAM School of Pharmacy, GITAM Deemed to be University, Hyderabad 502329, Telangana, India



Iguratimod, Rheumatoid arthritis, Cyclodextrin-based nanosponges, Box-Behnken design


Objective: Cyclodextrin nanosponges have unfolded themselves as budding delivery aids for intractable molecules that face difficulty in formulation.

Methods: The present research aimed at the preparation of cyclodextrin-based nanosponges employing diphenyl carbonate crosslinker as reported elsewhere. Box-Behnken design was adopted to evaluate the effects of factors (reaction temperature, reaction time and stirring speed) on practical yield and particle size. Based on a numerical optimization technique, five batches of nanosponge formulations with varying molar ratios (1:2, 1:4, 1:6, 1:8 and 1:10) were formulated and evaluated.

Results: The drug loading into optimized β–CD (NS14, NS16) was carried out by by freeze-drying method with a maximum drug loading of 32% displayed by IGNS14. The particle sizes of Iguratimod-loaded nanosponges range between 178 to 181 nm with lower polydispersity indices. The formulation IGNS14 and IGNS16 displayed optimal zetapotential of-27 and-26 mV, which is sufficient to stabilize the colloidal nanosuspension. The dissolution of both nanosponges was significantly higher (>98%) and controlled when compared to pure drug (34%). Retention of the drug in the optimized nanosponges was observed, which was released slowly over time. The PXRD confirm the formation of paracrystalline nanosponges that are spherical in shape with no interaction amongst the drug and excipients.

Conclusion: The cyclodextrin-based NS of Iguratimod were a probable alternative for drug delivery with improved physicochemical properties and therapeutic efficacy.


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Trotta F, Zanetti M, Cavalli R. Cyclodextrin-based nanosponges as drug carriers. Beilstein J Org Chem. 2012;8:2091-9. doi: 10.3762/bjoc.8.235, PMID 23243470.

Bhowmik, Himangshu, Venkatesh D, Kuila, Anuttam, Kumar, Kammari. Nanosponges: a review. Int J Appl Pharm. 2018;10:1-10.

Venuti V, Rossi B, Mele A, Melone L, Punta C, Majolino D. Tuning structural parameters for the optimization of drug delivery performance of cyclodextrin-based nanosponges. Opi: Expert Verlag. Drug Deliv. 2017;14(3):331-40.

Simranjot Kaur, Sandeep Kumar. The nanosponges: an innovative drug delivery system. Asian J Pharm Clin Res. 2019:60-7. doi: 10.22159/ajpcr.2019.v12i7.33879.

Trotta F, Cavalli R. Characterization and applications of new hyper-cross-linked cyclodextrins. Compos Interfaces. 2009;16(1):39-48. doi: 10.1163/156855408X379388.

Swaminathan S, Vavia PR, Trotta F, Cavalli R, Tumbiolo S, Bertinetti L. Structural evidence of differential forms of nanosponges of beta-cyclodextrin and its effect on solubilization of a model drug. J Incl Phenom Macrocycl Chem. 2013;76(1-2):201-11. doi: 10.1007/s10847-012-0192-y.

Chilajwar SV, Pednekar PP, Jadhav KR, Gupta GJC, Kadam VJ. Cyclodextrin-based nanosponges: a propitious platform for enhancing drug delivery. Expert Opin Drug Deliv. 2014;11(1):111-20. doi: 10.1517/17425247.2014.865013, PMID 24298891.

Anita Chando, Munira Momin, Mural Q, Shaily L. Topical nanocarriers for management of rheumatoid arthritis: a review. Biomed Pharmacother. 2021;141:111880. doi: 10.1016/j.biopha.2021.111880.

Takeba Y, Suzuki N, Wakisaka S, Nagafuchi H, Mihara S, Kaneko A. Effects of actarit on synovial cell functions in patients with rheumatoid arthritis. J Rheumatol. 1999;26(1):25-33. PMID 9918236.

Janakiraman K, Krishnaswami V, Rajendran V, Natesan S, Kandasamy R. Novel Nano therapeutic materials for the effective treatment of rheumatoid arthritis-recent insights. Mater Today Commun. 2018 Dec;17:200-13. doi: 10.1016/j.mtcomm.2018.09.011, PMID 32289062.

Rangaraj N, Pailla SR, Chowta P, S Nagarjun Rangaraj, Sravanthi Reddy Pailla, Paramesh Chowta. Fabrication of ibrutinib nanosuspension by quality by design approach: intended for enhanced oral bioavailability and diminished fast-fed variability. AAPS PharmSciTech. 2019;20(8):326. doi: 10.1208/s12249-019-1524-7, PMID 31659558.

Bowden GD, Pichler BJ, Maurer A. A design of experiments (DoE) approach accelerates the optimization of copper-mediated 18F-fluorination reactions of Arylstannanes. Sci Rep. 2019;9(1):11370. doi: 10.1038/s41598-019-47846-6, PMID 31388076.

Anandam S, Selvamuthukumar S. Fabrication of cyclodextrin nanosponges for quercetin delivery: physicochemical characterization, photostability, and antioxidant effects. J Mater Sci. 2014;49(23):8140-53. doi: 10.1007/s10853-014-8523-6.

Singireddy A, Subramanian SK. Cyclodextrin nanosponges to enhance the dissolution profile of quercetin by inclusion complex formation. Part Sci Technol. 2016;34(3):341-6. doi: 10.1080/02726351.2015.1081658.

Darandale SS, Vavia PR. Cyclodextrin-based nanosponges of curcumin: formulation and physicochemical characterization. J Incl Phenom Macrocycl Chem. 2013;75(3-4):315-22. doi: 10.1007/s10847-012-0186-9.

Zoppi A, Quevedo MA, Longhi MR. Specific binding capacity of beta-cyclodextrin with cis and trans enalapril: physicochemical characterization and structural studies by molecular modeling. Bioorg Med Chem. 2008;16(18):8403-12. doi: 10.1016/ j.bmc.2008.08.032, PMID 18771929.

Madhuri, Shete, Rajkumar. Formulation and evaluation of gliclazide nanosponges. Solunke, Rahul and Borge, Uday and Murthy, Krishna and Deshmukh. Int J Appl Pharm. 2019;11:181-9.

El-Assal MI. Nano-sponge novel drug delivery system as carrier of an anti-hypertensive drug. Int J Pharm Pharm Sci. 2019:47-63. doi: 10.22159/ijpps.2019v11i10.34812.



How to Cite

M., M., & G., S. K. (2022). PREPARATION AND EVALUATION OF IGURATIMOD ORAL FORMULATION USING CYCLODEXTRIN NANOSPONGES. International Journal of Applied Pharmaceutics, 14(5), 78–87.



Original Article(s)