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Research in Pharmaceutical Sciences، جلد ۲۰، شماره ۳، صفحات ۳۱۶-۳۴۲
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| عنوان فارسی |
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| چکیده فارسی مقاله |
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| کلیدواژه‌های فارسی مقاله |
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| عنوان انگلیسی |
Synthesis and in vitro evaluation of novel pH-triggered biocompatible folate-chondroitin sulfate-dexamethasone copolymers for delivery of tofacitinib in rheumatoid arthritis |
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| چکیده انگلیسی مقاله |
Background and purpose : Rheumatoid arthritis (RA) is a chronic inflammatory disease associated with systemic complications and progressive disability. Systemic side effects and poor drug delivery to joints limit current treatments. This study aimed to enhance the efficacy of tofacitinib (Tofa) by synthesizing novel pH-triggered biocompatible polymers, both folate-targeted and non-folate-targeted. Experimental approach: First-generation polymers were synthesized and characterized using FT-IR and 1 H-NMR spectroscopy. The critical micelle concentration of the copolymers was evaluated, and Tofa-loaded micelles were prepared using the dialysis method. The physical properties of the micelles were assessed using FE-SEM and dynamic light scattering. Cytotoxicity of Tofa/ chondroitin sulfate-maleic-dexamethasone (Tofa/CHS-Mal-DEX) and Tofa/folic acid-polyethylene glycol-chondroitin sulfate-maleic-dexamethasone (Tofa/FA-PEG-CHS-Mal-DEX) micelles was evaluated on the fibroblastic L929 and RAW264.7. The cellular uptake and anti-inflammatory effects were investigated in the activated Raw 264.7 cell line. Findings/Results : Tofa/CHS-Mal-DEX and Tofa/FA-PEG-CHS-Mal-DEX micelles exhibited particle sizes of 188 nm and 173.06 nm, respectively, with entrapment efficiencies of 51% and 72.76%. The release profiles exhibited that about 40% of Tofa was released from micelles over 62 h in physiological pH, whereas in acidic conditions, this significantly decreased to 2 h. Micelles demonstrated improved uptake efficiency, resulting in a significant reduction in IL-6 levels compared to free Tofa. None of the micelle formulations indicated cytotoxic effects on fibroblastic L929 and Raw 264.7 macrophage cell lines. Conclusion and implications : The developed folate and non-folate-targeted micelles were not toxic and biocompatible for enhancing the therapeutic potential of Tofa in RA and improving drug delivery. |
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| کلیدواژه‌های انگلیسی مقاله |
Chondroitin sulfate, Dexamethasone, Folic acid, Tofacitinib, pH-sensitive copolymers, Rheumatoid arthritis. |
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| نویسندگان مقاله |
| Zahra Ansarypour
Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, Isfahan, University of Medical Sciences, Isfahan, I.R. Iran.
| Jaber Emami
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, I.R. Iran.
| Farshid Hassanzadeh
Department of Clinical Biochemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.
| Mahmoud Aghaei
Department of Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.
| Mohsen Minaiyan
Faculty of Pharmacy and Pharmaceutical Sciences, Katz Centre for Pharmacy and Health Research, University of Alberta, Edmonton, AB, T6G 2E1, Canada.
| Neal M. Davies
Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, Isfahan, University of Medical Sciences, Isfahan, I.R. Iran.
| Mahboubeh Rezazadeh
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| نشانی اینترنتی |
http://rps.mui.ac.ir/index.php/jrps/article/view/2310 |
| فایل مقاله |
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| کد مقاله (doi) |
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| زبان مقاله منتشر شده |
en |
| موضوعات مقاله منتشر شده |
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| نوع مقاله منتشر شده |
Original Article |
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