Development And Characterization Of Diacerin Loaded Niosomes For Improved Transdermal Delivery In Osteoarthritis
- Authors
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Ghada Hamid Naji
Department of Pharmaceutics, College of Pharmacy, University of Babylon, Babylon, Iraq.
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- Keywords:
- Diacerein, Niosomes, Transdermal Drug Delivery, Osteoarthritis, Nanovesicles
- Abstract
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General Background: Osteoarthritis is a chronic degenerative joint disease, while oral diacerein has limited dissolution and low bioavailability. Specific Background: Niosomes may provide a vesicular approach for transdermal diacerein delivery while addressing limitations associated with oral administration. Knowledge Gap: An optimized diacerein niosomal formulation requires appropriate surfactant, cholesterol ratio, and sonication conditions. Aims: This study aimed to develop and optimize diacerein-loaded niosomes using the thin film hydration method. Results: Formulation F8 showed a vesicle size of 164.92±0.41 nm, entrapment efficiency of 91.52±1.0%, PDI of 0.16±0.015, and zeta potential of −33.94 mV. Increasing Span 60 reduced vesicle size and increased entrapment efficiency, whereas higher cholesterol increased vesicle size and reduced entrapment efficiency. Longer sonication reduced vesicle size but decreased entrapment efficiency. Novelty: F8 combined favorable vesicle characteristics with high drug entrapment. Implications: F8 may serve as a candidate for further transdermal development, requiring ex vivo permeation and in vivo anti-inflammatory studies.
Key Findings Highlights
Span 60 increased drug entrapment while reducing vesicle size.
Higher cholesterol produced larger vesicles with lower entrapment.
Extended sonication reduced vesicle size but lowered drug entrapment.
Keywords : Diacerein, Niosomes, Transdermal Drug Delivery, Osteoarthritis, Nanovesicles
- References
-
González-Rodríguez, F. J. De Toro, A. Jorge-Mora, P. Fernandez-Pernas, C. P. Rivadulla, M. Fraga, J. A. Fafián-Labora, and M. C. Arufe, “Targeting Osteoarthritis With Small Extracellular Vesicle Therapy: Potential and Perspectives,” Frontiers in Bioengineering and Biotechnology, vol. 13, p. 1570526, 2025.
N. Rashidi, C. Liu, P. V. Guillot, and M. Tamaddon, “Isolation, Characterization, and In Vitro Cell Studies of Plant-Based Exosome-Like Nanovesicles for Treatment of Early Osteoarthritis,” International Journal of Molecular Sciences, vol. 26, no. 5, p. 2211, 2025.
Q. Weng, S. L. Goh, J. Wu, M. S. Persson, J. Wei, A. Sarmanova, X. Li, M. Hall, M. Doherty, T. Jiang, and C. Zeng, “Comparative Efficacy of Exercise Therapy and Oral Non-Steroidal Anti-Inflammatory Drugs and Paracetamol for Knee or Hip Osteoarthritis: A Network Meta-Analysis of Randomised Controlled Trials,” British Journal of Sports Medicine, vol. 57, no. 15, pp. 990–996, 2023.
N. Y. Fareed and H. J. Kassab, “A Comparative Study of Oral Diacerein and Transdermal Diacerein as Novasomal Gel in a Model of MIA-Induced Osteoarthritis in Rats,” Pharmacia, vol. 70, no. 4, pp. 1363–1371, 2023.
T. Ayesha, A. Erum, N. Shahid, U. R. Tulain, and U. Saleem, “An Effective Approach in Osteoarthritis: Diacerein-Loaded Solid Lipid Nanoparticles, Preparation and Evaluation for Targeted Therapy,” Journal of Drug Delivery Science and Technology, vol. 108, p. 106856, 2025.
K. Singh, R. Sharma, and J. Rai, “Diacerein as Adjuvant to Diclofenac Sodium in Osteoarthritis Knee,” International Journal of Rheumatic Diseases, vol. 15, no. 1, pp. 69–77, 2012.
S. A. Fouad, F. A. Malaak, M. A. El-Nabarawi, K. Abu Zeid, and A. M. Ghoneim, “Preparation of Solid Dispersion Systems for Enhanced Dissolution of Poorly Water-Soluble Diacerein: In Vitro Evaluation, Optimization and Physiologically Based Pharmacokinetic Modeling,” PLoS One, vol. 16, no. 1, p. e0245482, 2021.
S. Maitra, S. K. Das, D. Sinha, M. Mukherjee, L. Kumari, and T. Roy, “Recent Advancements and Future Perspectives in Diacerein Delivery Systems for Rheumatoid Arthritis: Novel Strategies and Emerging Technologies,” Palestinian Medical and Pharmaceutical Journal, vol. 11, no. 1, 2025.
M. Shabbir, K. Barkat, M. U. Ashraf, U. Nagra, and S. N. Shah, “Assessment of Formulation Variables of Poor Water-Soluble Diacerein for Its Improved Loading and Anti-Inflammatory Activity,” Drug Delivery and Translational Research, vol. 13, no. 6, pp. 1780–1798, 2023.
N. Y. Albassam and H. J. Kassab, “Diacerein Loaded Novasome for Transdermal Delivery: Preparation, In Vitro Characterization and Factors Affecting Formulation,” Iraqi Journal of Pharmaceutical Sciences, vol. 32, Suppl., pp. 214–224, 2023.
H. A. Benson, J. E. Grice, Y. Mohammed, S. Namjoshi, and M. S. Roberts, “Topical and Transdermal Drug Delivery: From Simple Potions to Smart Technologies,” Current Drug Delivery, vol. 16, no. 5, pp. 444–460, 2019.
L. Antonara, E. Triantafyllopoulou, M. Chountoulesi, N. Pippa, N. Lagopati, P. P. Dallas, D. M. Rekkas, and M. Gazouli, “Recent Advances in Niosome-Based Transdermal Drug Delivery Systems,” Current Opinion in Biomedical Engineering, vol. 35, p. 100603, 2025.
N. Ala’a and N. A. Rajab, “Formulation and Characterization of Niosomes for Controlled Delivery of Tolmetin,” Journal of Pharmaceutical Negative Results, vol. 13, no. 4, pp. 159–169, 2022.
Akbarzadeh, M. Shayan, M. Bourbour, M. Moghtaderi, H. Noorbazargan, F. E. Yeganeh, S. Saffar, and M. Tahriri, “Preparation, Optimization and In Vitro Evaluation of Curcumin-Loaded Niosome@Calcium Alginate Nanocarrier as a New Approach for Breast Cancer Treatment,” Biology, vol. 10, no. 3, p. 173, 2021.
F. D. Moghaddam, I. Akbarzadeh, E. Marzbankia, M. Farid, L. Khaledi, A. H. Reihani, M. Javidfar, and P. Mortazavi, “Delivery of Melittin-Loaded Niosomes for Breast Cancer Treatment: An In Vitro and In Vivo Evaluation of Anti-Cancer Effect,” Cancer Nanotechnology, vol. 12, no. 1, p. 14, 2021.
M. I. Al-Shadedi and F. J. Al-Gawhari, “Formulation of Risperidone Nano Niosomal Vesicular System by Ecofriendly Direct Ultrasonication Method,” Iraqi Journal of Pharmaceutical Sciences, vol. 34, no. 2, pp. 250–258, 2025.
K. Thamer and A. N. Abood, “Preparation and In Vitro Characterization of Aceclofenac Nanosuspension (ACNS) for Enhancement of Percutaneous Absorption Using Hydrogel Dosage Form,” Iraqi Journal of Pharmaceutical Sciences, vol. 30, no. 2, pp. 86–98, 2021.
H. Abdelkader, S. Ismail, A. Kamal, and R. G. Alany, “Preparation of Niosomes as an Ocular Delivery System for Naltrexone Hydrochloride: Physicochemical Characterization,” Die Pharmazie—An International Journal of Pharmaceutical Sciences, vol. 65, no. 11, pp. 811–817, 2010.
G. A. Abdelbary and M. H. Aburahma, “Oro-Dental Mucoadhesive Proniosomal Gel Formulation Loaded With Lornoxicam for Management of Dental Pain,” Journal of Liposome Research, vol. 25, no. 2, pp. 107–121, 2015.
M. Al-Mahallawi, A. A. Abdelbary, and M. H. Aburahma, “Investigating the Potential of Employing Bilosomes as a Novel Vesicular Carrier for Transdermal Delivery of Tenoxicam,” International Journal of Pharmaceutics, vol. 485, no. 1–2, pp. 329–340, 2015.
G. H. Al-Edhari and F. J. Al-Gawhari, “Study the Effect of Formulation Variables on Preparation of Nisoldipine Loaded Nano Bilosomes,” Iraqi Journal of Pharmaceutical Sciences, vol. 32, Suppl., pp. 271–282, 2023.
N. K. Alruwaili, A. Zafar, O. A. Alsaidan, M. Yasir, E. M. Mostafa, S. F. Alnomasy, A. Rawaf, A. Alquraini, and F. A. Alomar, “Development of Surface Modified Bilosomes for the Oral Delivery of Quercetin: Optimization, Characterization In Vitro, Antioxidant, Antimicrobial, and Cytotoxicity Study,” Drug Delivery, vol. 29, no. 1, pp. 3035–3050, 2022.
M. A. El-Nabarawi, R. N. Shamma, F. Farouk, and S. M. Nasralla, “Bilosomes as a Novel Carrier for the Cutaneous Delivery of Dapsone as a Potential Treatment of Acne: Preparation, Characterization and In Vivo Skin Deposition Assay,” Journal of Liposome Research, vol. 30, no. 1, pp. 1–1, 2020.
Ameeduzzafar, N. K. Alruwaili, S. S. Imam, N. H. Alotaibi, N. A. Alhakamy, K. S. Alharbi, S. Alshehri, M. Afzal, S. K. Alenezi, and S. N. Bukhari, “Formulation of Chitosan Polymeric Vesicles of Ciprofloxacin for Ocular Delivery: Box-Behnken Optimization, In Vitro Characterization, HET-CAM Irritation, and Antimicrobial Assessment,” AAPS PharmSciTech, vol. 21, no. 5, p. 167, 2020.
G. A. Abdelbary, M. M. Amin, and M. Y. Zakaria, “Ocular Ketoconazole-Loaded Proniosomal Gels: Formulation, Ex Vivo Corneal Permeation and In Vivo Studies,” Drug Delivery, vol. 24, no. 1, pp. 309–319, 2017.
J. Akbari, M. Saeedi, R. Enayatifard, K. Morteza-Semnani, S. M. Hashemi, A. Babaei, S. M. Rahimnia, S. S. Rostamkalaei, and A. Nokhodchi, “Curcumin Niosomes (Curcusomes) as an Alternative to Conventional Vehicles: A Potential for Efficient Dermal Delivery,” Journal of Drug Delivery Science and Technology, vol. 60, p. 102035, 2020.
K. Owodeha-Ashaka, M. O. Ilomuanya, and A. Iyire, “Evaluation of Sonication on Stability-Indicating Properties of Optimized Pilocarpine Hydrochloride-Loaded Niosomes in Ocular Drug Delivery,” Progress in Biomaterials, vol. 10, no. 3, pp. 207–220, 2021.
N. Allam, S. I. Hamdallah, and O. Y. Abdallah, “Chitosan-Coated Diacerein Nanosuspensions as a Platform for Enhancing Bioavailability and Lowering Side Effects: Preparation, Characterization, and Ex Vivo/In Vivo Evaluation,” International Journal of Nanomedicine, pp. 4733–4745, 2017.
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