Development and Evaluation of Chitosan Nanoparticles for Ocular Delivery of Tedizolid Phosphate
被引:23
作者:
Abul Kalam, Mohd
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King Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi ArabiaKing Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
Abul Kalam, Mohd
[1
,2
]
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Iqbal, Muzaffar
[3
,4
]
Alshememry, Abdullah
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机构:
King Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi ArabiaKing Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
Alshememry, Abdullah
[1
,2
]
Alkholief, Musaed
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机构:
King Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi ArabiaKing Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
Alkholief, Musaed
[1
,2
]
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Alshamsan, Aws
[1
,2
]
机构:
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, Nanobiotechnol Unit, Riyadh 11451, Saudi Arabia
[2] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi Arabia
[3] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
[4] King Saud Univ, Coll Pharm, Bioavailabil Unit, Cent Lab, Riyadh 11451, Saudi Arabia
This study investigates the development of topically applied non-invasive chitosan-nanoparticles (CSNPs) for ocular delivery of tedizolid phosphate (TZP) for the treatment of MRSA-related ocular and orbital infections. An ionic-gelation method was used to prepare TZP-encapsulated CSNPs using tripolyphosphate-sodium (TPP) as cross-linker. Particle characterization was performed by the DLS technique (Zeta-Sizer), structural morphology was observed by SEM. The drug encapsulation and loading were determined by the indirect method. In-vitro release was conducted through dialysis bags in simulated tear fluid (pH 7) with 0.25% Tween-80. Physicochemical characterizations were performed for ocular suitability of CSNPS. An antimicrobial assay was conducted on different strains of Gram-positive bacteria. Eye-irritation from CSNPs was checked in rabbits. Transcorneal flux and apparent permeability of TZP from CSNPs was estimated through excised rabbit cornea. Ionic interaction between the anionic and cationic functional groups of TPP and CS, respectively, resulted in the formation of CSNPs at varying weight ratios of CS/TPP with magnetic stirring (700 rpm) for 4 h. The CS/TPP weight ratio of 3.11:1 with 10 mg of TZP resulted in optimal-sized CSNPs (129.13 nm) with high encapsulation (82%) and better drug loading (7%). Release profiles indicated 82% of the drug was released from the TZP aqueous suspension (TZP-AqS) within 1 h, while it took 12 h from F2 to release 78% of the drug. Sustained release of TZP from F2 was confirmed by applying different release kinetics models. Linearity in the profile (suggested by Higuchi's model) indicated the sustained release property CSNPs. F2 has shown significantly increased (p < 0.05) antibacterial activity against some Gram-positive strains including one MRSA strain (SA-6538). F2 exhibited a 2.4-fold increased transcorneal flux and apparent permeation of TZP as compared to TZP-AqS, indicating the better corneal retention. No sign or symptoms of discomfort in the rabbits' eyes were noted during the irritation test with F2 and blank CSNPs, indicating the non-irritant property of the TZP-CSNPs. Thus, the TZP-loaded CSNPs have strong potential for topical use in the treatment of ocular MRSA infections and related inflammatory conditions.
机构:
King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
King Abdulaziz Univ, Dept Chem, Polymer Res Lab, Fac Sci, Jeddah, Saudi ArabiaKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Kurakula, Mallesh
Ahmed, Osama A. A.
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King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Menia Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm, Al Minya, EgyptKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Ahmed, Osama A. A.
Fahmy, Usama A.
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King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi ArabiaKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Fahmy, Usama A.
Ahmed, Tarek A.
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King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Al Azhar Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm, Cairo, EgyptKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
机构:
King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
King Abdulaziz Univ, Dept Chem, Polymer Res Lab, Fac Sci, Jeddah, Saudi ArabiaKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Kurakula, Mallesh
Ahmed, Osama A. A.
论文数: 0引用数: 0
h-index: 0
机构:
King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Menia Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm, Al Minya, EgyptKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Ahmed, Osama A. A.
Fahmy, Usama A.
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机构:
King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi ArabiaKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Fahmy, Usama A.
Ahmed, Tarek A.
论文数: 0引用数: 0
h-index: 0
机构:
King Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia
Al Azhar Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm, Cairo, EgyptKing Abdulaziz Univ, Dept Pharmaceut & Ind Pharm, Adv Pharmaceut & Nanotechnol Lab, Fac Pharm, Jeddah, Saudi Arabia