title: Studying the influence of formulation and process variables on Vancomycin-loaded polymeric nanoparticles as potential carrier for enhanced ophthalmic delivery.
abstract: Ocular topically applied Vancomycin (VCM) suffers poor bioavailability due to its high molecular weight and hydrophilicity. In the present investigation, VCM-loaded polymeric nanoparticles (PNPs) were developed aiming to enhance its ocular bioavailability through prolonging its release pattern and ophthalmic residence. PNPs were prepared utilizing double emulsion (W/O/O), solvent evaporation technique. 23×41full factorial design was applied to evaluate individual and combined influences of polymer type, Eudragit® RS100, sonication time, and Span®80 concentration on PNPs particle size, encapsulation efficiency, and zeta potential. Further, the optimized formulae were incorporated in 1% Carbopol®-based gel. In-vivo evaluation of the optimized formulae was performed via Draize test followed by microbiological susceptibility testing on albino rabbits. Results revealed successful formulation of VCM-loaded PNPs was achieved with particle sizes reaching 155nm and up to 88% encapsulation. Draize test confirmed the optimized formulae as non-irritating and safe for ophthalmic administration. Microbiological susceptibility testing confirmed prolonged residence, higher Cmax.with more than two folds increment in the AUC(0.25-24)of VCM-PNPs over control groups. Thus, VCM-loaded PNPs represent promising carriers with superior achievements for enhanced Vancomycin ophthalmic delivery over the traditional use of commercially available VCM parenteral powder after constitution into a solution by the ophthalmologists.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini St., Cairo, Egypt.
authors.forename: Carol
authors.initials: C
authors.lastname: Yousry
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt.
authors.forename: Seham A
authors.initials: SA
authors.lastname: Elkheshen
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini St., Cairo, Egypt; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, University of Modern Science and Art, Cairo, Egypt.
authors.forename: Hanan M
authors.initials: HM
authors.lastname: El-Laithy
authors.affiliation: Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Kasr El-Aini St., Cairo, Egypt.
authors.forename: Tamer
authors.initials: T
authors.lastname: Essam
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini St., Cairo, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, Ahram Canadian University, 6th of October City, Cairo, Egypt. Electronic address: raniafahmy@gmail.com.
authors.forename: Rania H
authors.initials: RH
authors.lastname: Fahmy
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D060433:Administration, Ophthalmic; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity; D004339:Drug Compounding; D065546:Drug Liberation; D005782:Gels; D006863:Hydrogen-Ion Concentration; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity; D011817:Rabbits; D013211:Staphylococcus aureus / Q000187:drug effects; D014640:Vancomycin / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity
chemical_list: D000180:Acrylic Resins; D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D005782:Gels; C006912:carboxypolymethylene; C050528:Eudragit RS; D014640:Vancomycin
keywords: Draize test; Microbiological susceptibility testing; Ocular infection; Poly (d,l-lactide- coglycolide) (PLGA); Polycaprolactone (PCL); Vancomycin