title: Design and evaluation of proniosomes as a carrier for ocular delivery of lomefloxacin HCl.
abstract: The current investigation aims to develop and evaluate novel ocular proniosomal gels of lomefloxacin HCl (LXN); in order to improve its ocular bioavailability for the management of bacterial conjunctivitis. Proniosomes were prepared using different types of nonionic surfactants solely and as mixtures with Span 60. The formed gels were characterized for entrapment efficiency, vesicle size, and in vitro drug release. Only Span 60 was able to form stable LXN-proniosomal gel when used individually while the other surfactants formed gels only in combination with Span 60 at different ratios. The optimum proniosomal gel; P-LXN 7 (Span 60:Tween 60, 9:1) appeared as spherical shaped vesicles having high entrapment efficiency (>80%), appropriate vesicle size (187 nm) as well as controlled drug release over 12 h. Differential scanning calorimetry confirmed the amorphous nature of LXN within the vesicles. Stability study did not show any significant changes in entrapment efficiency or vesicle size after storage for 3 months at 4 °C. P-LXN 7 was found to be safe and suitable for ocular delivery as proven by the irritancy test. The antibacterial activity of P-LXN 7 evaluated using the susceptibility test and topical therapy of induced ocular conjunctivitis confirmed the enhanced antibacterial therapeutic efficacy of the LXN-proniosomal gel compared to the commercially available LXN eye drops.
authors.affiliation: a Department of Pharmaceutical Technology , National Research Centre , Cairo , Egypt.
authors.forename: Rawia M
authors.initials: RM
authors.lastname: Khalil
authors.affiliation: b Department of Pharmaceutics , Faculty of Pharmacy, Cairo University , Cairo , Egypt , and.
authors.forename: Ghada A
authors.initials: GA
authors.lastname: Abdelbary
authors.affiliation: a Department of Pharmaceutical Technology , National Research Centre , Cairo , Egypt.
authors.forename: Mona
authors.initials: M
authors.lastname: Basha
authors.affiliation: c Chemistry of Natural and Microbial Product Department, National Research Centre , Cairo , Egypt.
authors.forename: Ghada E A
authors.initials: GE
authors.lastname: Awad
authors.affiliation: a Department of Pharmaceutical Technology , National Research Centre , Cairo , Egypt.
authors.forename: Hadeer A
authors.initials: HA
authors.lastname: El-Hashemy
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D015195:Drug Design; D005123:Eye / Q000187:drug effects* / Q000382:microbiology; D005128:Eye Diseases / Q000188:drug therapy*; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D005782:Gels / Q000138:chemical synthesis / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000138:chemical synthesis / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D011817:Rabbits; D013203:Staphylococcal Infections / Q000188:drug therapy*; D013211:Staphylococcus aureus / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D024841:Fluoroquinolones; D005782:Gels; D008081:Liposomes; C053091:lomefloxacin
keywords: Conjunctivitis; lomefloxacin HCl; microbiological evaluation; ocular delivery; proniosomes