Title of article :
Improvement of Ocular Efficacy of Levofloxacin by Bioadhesive Chitosan Coated PLGA Nanoparticles: Box-Behnken Design, In-vitro Characterization, Antibacterial Evaluation and Scintigraphy Study
Author/Authors :
Zafar, Ameeduzzafar Department of Pharmaceutics - College of Pharmacy - Jouf University, Skaka, P.O. Box 2014, Saudi Arabia , Alruwaili, Nabil K Department of Pharmaceutics - College of Pharmacy - Jouf University, Skaka, P.O. Box 2014, Saudi Arabia , Shalaby, khaled Department of Pharmaceutics - College of Pharmacy - Jouf University, Skaka, P.O. Box 2014, Saudi Arabia , Khan, Nazia Department of Pharmaceutics - School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India , Ali, Asgar Department of Pharmaceutics - School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India , Abbas Bukhari, Syed Nasir Department of Pharmaceutical Chemistry - College of Pharmacy - Jouf University, Skaka, P.O. Box 2014, Saudi Arabia , Alsuwayt, Bader Department of Pharmaceutics - Faculty of Pharmacy - Northern Border University, KSA , Afzal, Muhammad Department of Pharmacology - College of Pharmacy - Jouf University - Skaka, P.O. Box 2014, Saudi Arabia , Akhtar, Sana Department of Pharmacology - College of Pharmacy - Jouf University - Skaka, P.O. Box 2014, Saudi Arabia , Yasir, Mohd Department of Pharmacy - College of Health Science - Arsi University, Asella, Ethopia
Abstract :
Conjunctivitis is considered as a common infection of ocular surfaces. Eye drop is most commonly used for treatment of conjunctivitis, but has some drawback like 95% drug eliminated after administration. Administration of levofloxacin to the anterior site in form of chitosan coated poly (lactic-co-glycolic acid) nanoparticles (LFV-CS-PLGA-NPs) expected to overcome these problem and increasing corneal contact time and permeability for effective treatment of bacterial conjunctivitis. TheNanoparticles were developed by single emulsion solvent evaporation technique and optimized for different variables (chitosan, poly (lactide-co-glycolic acid) and polyvinyl alcohol concentration) by employing three factors, three levels Box–Behnken statistical design. The nanoparticles were evaluated for particle size, drug loading, entrapment efficiency, drug release, ex-vivo permeation, ocular tolerance, antimicrobial study, confocal laser microscopy, and Gamma scintigraphy study. The particle size and PdI of the optimized nanoparticles were 169.968 ± 15.23 nm and 0.13 ± 0.03, respectively, where as entrapment efficiency and drug loading is 49.54 ± 2.43% and 11.29 ± 2.13% with extended release profile and strong mucoadhesion. DSC data indicated levofloxacin formed molecular dispersion within coated nanoparticles. Corneal flux showed significantly (P < 0.05) higher permeation as compared to marketed formulation. Formulation was nonirritant and possessed good antibacterial activity. Gamma Scintigraphy showed slow drainage compared to drug solution, indicating reduction in nasolachrymal drainage. The Gamma Scintigraphy study indicated the CS coated PLGA-NPs have high corneal residence time as compared to drug solution. So, it is revealed that LFV-CS-PLGA-NPs increase the drug concentration over ocular tissue and potential usefulness for sustained drug delivery.
Keywords :
Levofloxacin loaded coated PLGA nanoparticles , Box-Behnken , Ocular irritation , Confocal microscopy antimicrobial study , Gamma scintigraphy
