title: Tri/tetra-block co-polymeric nanocarriers as a potential ocular delivery system of lornoxicam: in-vitro characterization, and in-vivo estimation of corneal permeation.
abstract: Polymeric micelles that can deliver drug to intended sites of the eye have attracted much scientific attention recently. The aim of this study was to evaluate the aqueous-based formulation of drug-loaded polymeric micelles that hold significant promise for ophthalmic drug delivery. This study investigated the synergistic performance of mixed polymeric micelles made of linear and branched poly(ethylene oxide)-poly(propylene oxide) for the more effective encapsulation of lornoxicam (LX) as a hydrophobic model drug. The co-micellization process of 10% binary systems combining different weight ratios of the highly hydrophilic poloxamers; Synperonic(®) PE/P84, and Synperonic(®) PE/F127 and the hydrophobic poloxamine counterpart (Tetronic(®) T701) was investigated by means of photon correlation spectroscopy and cloud point. The drug-loaded micelles were tested for their solubilizing capacity towards LX. Results showed a sharp solubility increase from 0.0318 mg/mL up to more than 2.34 mg/mL, representing about 73-fold increase. Optimized formulation was selected to achieve maximum drug solubilizing power and clarity with lowest possible particle size, and was characterized by (1)HNMR analysis which revealed complete encapsulation of the drug within the micelles. Further investigations by histopathological and confocal laser studies revealed the non-irritant nature and good corneal penetrating power of the proposed nano-formulation.
authors.affiliation: Department of Pharmaceutical Technology, National Research Center, Cairo, Egypt.
authors.forename: Alaa Hamed
authors.initials: AH
authors.lastname: Salama
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, Egypt. Electronic address: rehab.shamma@pharma.cu.edu.eg.
authors.forename: Rehab Nabil
authors.initials: RN
authors.lastname: Shamma
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry* / Q000633:toxicity; D003315:Cornea / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D065546:Drug Liberation; D005029:Ethylenediamines / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry* / Q000633:toxicity; D010316:Particle Size; D010894:Piroxicam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000633:toxicity; D011092:Polyethylene Glycols / Q000737:chemistry*; D011095:Polyethylenes / Q000737:chemistry*; D011126:Polypropylenes / Q000737:chemistry*; D011817:Rabbits; D012235:Rhodamines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D012995:Solubility
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005029:Ethylenediamines; D005456:Fluorescent Dyes; D011095:Polyethylenes; D011126:Polypropylenes; D012235:Rhodamines; D010894:Piroxicam; C012571:tetronic 701; D011092:Polyethylene Glycols; C078661:UCON 50-HB-5100; C059451:lornoxicam; C029773:rhodamine B
keywords: Confocal laser scanning microscopy; Histopathological studies; Lornoxicam; Ocular drug delivery; Single and mixed nanomicellar systems