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Iranian Journal of Basic Medical Sciences، جلد ۲۴، شماره ۳، صفحات ۳۳۱-۳۴۰
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عنوان انگلیسی Sustained release of linezolid in ocular insert based on lipophilic modified structure of sodium alginate
چکیده انگلیسی مقاله Objective(s): Ocular inserts are usually polymeric thin films with increased ocular residence time and sustained drug release capacity. Sodium alginate is a biocompatible and biodegradable carrier; however, initial burst release of encapsulated drug within it, is recognized as a challenge. Grafting –addition of functional moieties to a polymer– is a technique to modify polymers’ physicochemical properties, including higher ability to control drug release. Linezolid (LNZ) solution is used in consecutive doses in treatment of antibiotic-resistant Gram-positive bacterial infections especially induced by methicillin resistant Staphylococcus aureus (MRSA). Materials and Methods: Grafted alginate copolymers were synthesized using butyl methacrylate (BMC) and lauryl methacrylate (LMC) at two different reaction times (12 hr and 24 hr). Copolymerization was evaluated by 1H-NMR, Ft-IR, and TGA. Copolymer safety was examined by cytotoxicity test against HEK-293 cell. Linezolid inserts were prepared using optimized copolymers and characterized.Results: 1H-NMR, Ft-IR, and TGA confirmed the successful grafting of alginate copolymers. ALG-B24 and ALG-L12 showed the highest safety against HEK-293 cell line comparing with intact alginate. Linezolid insert characterization results indicated a slower linezolid release profile related to creation of a lipophilic structure. A better strength property for linezolid loaded ALG-B24 and ALG-L12 inserts was obtained while ALG-L12 showed a stronger adhesive force compared with intact alginate. Antibacterial efficacy on clinical isolated MRSA after 24 hr was similar to linezolid solution.Conclusion: Lipophilic alginate copolymer (ALG-L12) showed a sustained release capability while retaining its main feature in strong film forming ability so it seems to be a promising safe carrier.
کلیدواژه‌های انگلیسی مقاله Copolymer, Grafting, Linezolid, Ocular insert, Sodium alginate
نویسندگان مقاله | Ashkan Mohammad Sadeghi
Department of Quality Control, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran


| Fatemeh Farjadian
Pharmaceutical Sciences Research Center, Shiraz University of Medical Sciences, Shiraz, Iran


| Shohreh Alipour
Department of Quality Control, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran|Pharmaceutical Sciences Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
نشانی اینترنتی https://ijbms.mums.ac.ir/article_17456.html
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زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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