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1.
Drug Des Devel Ther ; 15: 399-418, 2021.
Article in English | MEDLINE | ID: mdl-33584095

ABSTRACT

AIM: Norfloxacin (NFX) has low ocular bioavailability. The current work aimed to develop NFX-loaded nanoparticle (NP)-laden hydrogels to improve the ocular potential of NFX, minimize the need for frequent instillations and lower undesirable side effects. METHODS: NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 21.41 full factorial design, using two types of polylactic-co-glycolic acid (PLGA) polymer and four (drug: polymer) ratios. NPs were evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), drug entrapment efficiency percentage (EE%), drug percentage released after 30 min (Q30min) and 12 hours (Q12h), drug percentage permeated through goat corneas after 30 min (P30min) and 12 hours (P12h) and morphology. Two formulae were statistically selected and incorporated into hydroxypropyl methylcellulose (HPMC)-based hydrogels; G1 - G4. The latter systems were evaluated for appearance, clarity, pH, spreadability, rheology, drug percentages released, drug percentages permeated, antimicrobial activity against Pseudomonas aeruginosa, and histopathological changes. RESULTS: The selected NPs (NP2 and NP6) were spherical in shape and possessed suitable PS (392.02 nm and 190.51 nm) and PDI (0.17 and 0.18), high magnitude of ZP (-30.43 mV and -33.62 mV), high EE% (79.24% and 91.72%), low Q30min (10.96% and 16.65%) and P30min (17.39% and 21.05%) and promising Q12h (58.23% and 71.20%) and P12h (53.31% and 65.01%), respectively. Clear, spreadable, tolerable, pseudoplastic, and thixotropic HPMC-based hydrogels were developed. They showed more prolonged drug release and drug permeation profiles. NP2- and NP6-laden hydrogels (G3 and G4 systems, respectively) had promising antibacterial activity, and reasonable histopathological safety. CONCLUSION: G3 and G4 are potential ocular delivery systems for NFX.


Subject(s)
Anti-Bacterial Agents/pharmacology , Hydrogels/chemistry , Nanoparticles/chemistry , Norfloxacin/pharmacology , Polylactic Acid-Polyglycolic Acid Copolymer/chemistry , Pseudomonas/drug effects , Anti-Bacterial Agents/chemistry , Dose-Response Relationship, Drug , Drug Carriers/chemistry , Drug Development , Microbial Sensitivity Tests , Molecular Structure , Norfloxacin/chemistry , Pseudomonas aeruginosa/drug effects , Structure-Activity Relationship
2.
Clin Ophthalmol ; 14: 1833-1837, 2020.
Article in English | MEDLINE | ID: mdl-32636611

ABSTRACT

PURPOSE: To evaluate corneal biomechanical parameters with an ocular response analyzer (ORA) in patients with psoriasis and compare these parameters with age-matched control subjects. STUDY DESIGN: This was a cross-sectional observational case-control study. METHODS: Thirty eyes of 15 psoriasis patients were included in the study and compared with 30 eyes of 15 control subjects. Corneal biomechanical properties were calculated by ORA. Central corneal thickness (CCT) was measured by anterior-segment optical coherence tomography. The main outcome measures were corneal hysteresis (CH), corneal resistance factor (CRF), corneal-compensated intraocular pressure (IOPcc), and Goldmann-correlated IOP (IOPg). For dry-eye evaluation, Schirmer's test was used. RESULTS: Mean CH in the psoriasis group was 10.20±1.55 mmHg and in the control group 10.66±1.36 mmHg (p=0.215). Mean CRF in the psoriasis group was 9.76±1.60 mmHg and in the control group 10.97±1.42 mmHg (p=0.003). Mean IOPcc in the psoriasis group was 14.84±3.43 mmHg and in the control group 16.67±3.17 mmHg (p=0.035). Mean IOPg in the psoriasis group was 13.92±3.35 mmHg and in the control group 16.62±3.10 mmHg (p=0.002). Mean CCT in the psoriasis group was 543.90±37.27 µm and in the control group 551.23±28.63 µm (p=0.392). Schirmer's test results in the psoriasis group were 11.4±1.57 mm/5 min and in the control group 17.5±1.52 mm/5 min (p<0.001). CONCLUSION: Psoriasis affects corneal biomechanical properties with statistically significantly lower corneal biomechanics than normal. CH correlates negatively with disease activity. These corneal biomechanical changes should be considered when determining IOP values and during corneal evaluation for keratoconus-suspected patients.

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