Purpose: To elucidate the intraocular pressure (IOP)-lowering effects and associated characteristics of Y-39983, a selective Rho-associated coiled coil-forming protein kinase (ROCK) inhibitor derived from Y-27632, in animal eyes.
Methods: Y-39983 was compared with Y-27632 for selectivity of ROCK inhibition by biochemical assay. The IOP was monitored by pneumatonometer in albino rabbits and cynomolgus monkeys that were given topically administered Y-39983. The total outflow facility and uveoscleral outflow were measured by two-level constant-pressure perfusion and perfusion technique using fluorescein isothiocyanate-dextran, respectively, at 2 hours after topical administration of Y-39983 in albino rabbits. The ocular toxicologic effects of topical administration of Y-39983 were observed in albino rabbits and cynomolgus monkeys.
Results: A biochemical assay showed that Y-39983 inhibited ROCK more potently than Y-27632. In rabbits, topical administration of Y-39983 significantly increased conventional outflow by 65.5%, followed by significant, dose-dependent reduction in IOP. Maximum IOP reduction was 13.2 +/- 0.6 mm Hg (mean +/- SE) at 0.1% Y-39983 in rabbits. In monkeys, at 3 hours after topical administration of 0.05% Y-39983, maximum reduction of IOP was 2.5 +/- 0.8 mm Hg. No serious side effects were observed in ocular tissues except sporadic punctate subconjunctival hemorrhage during long-term topical administration of Y-39983 four times a day (at 2-hour intervals) in rabbits or monkeys. However, punctate subconjunctival hemorrhage was not observed with administration twice daily (at a 6-hour interval) or three times a day (at 5-hour intervals).
Conclusions: Y-39983 causes increased outflow facility followed by IOP reduction. Y-39983 ophthalmic solution may be a candidate drug for lowering of IOP, since it increases conventional outflow and produces relatively few side effects.
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http://dx.doi.org/10.1167/iovs.05-1617 | DOI Listing |
Arch Dermatol Res
January 2025
Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Universitas Syiah Kuala, Banda Aceh, 23111, Indonesia.
Atopic dermatitis (AD) is a chronic inflammatory skin condition characterized by dry skin, severe itching, redness, and inflammation. Its complex etiology, involving genetic, immunological, and environmental factors, necessitates innovative therapeutic approaches. This study investigates nanostructured lipid carriers (NLCs) formulated with traditional fermented coconut (Cocos nucifera L.
View Article and Find Full Text PDFJ Contemp Dent Pract
October 2024
Department of Public Health Dentistry, Tamil Nadu Government Dental College and Hospital, Chennai, Tamil Nadu, India, Orcid: https://orcid.org/0000-0002-5876-5458.
Aim: This study aimed to evaluate the effectiveness of fenugreek as an adjuvant in managing oral potentially malignant disorders (OPMDs), specifically leukoplakia, lichen planus, and oral submucous fibrosis (OSMF).
Materials And Methods: Twenty-one participants prediagnosed with OPMDs were randomly divided into a study group (SG) and a control group (CG), with 10 participants in SG and 11 in CG, respectively. The SG received 2 gm of fenugreek as an adjuvant with standard systemic treatments tailored to the respective lesions: intralesional injection of vitamin A 1,00,000 IU (Aquasol A) and topical application of triamcinolone acetonide 0.
Pharm Dev Technol
January 2025
Department of Dermatology, Venereology and Andrology, Faculty of Medicine, Alexandria University, Egypt.
Tear trough deformity (TTD) is a significant cosmetic concern, with current treatments relying primarily on invasive injectable fillers, which are costly and carry risks of complications. Despite the widespread use of hyaluronic acid (HA) in cosmetic applications, its poor dermal permeation has limited the development of effective topical fillers for TTD.This study aim to develop and evaluate a novel hyaluronic acid nanogel (nanofiller, NF) as a non-invasive topical filler for TTD.
View Article and Find Full Text PDFJ Dent Sci
January 2025
Department of Oral and Maxillofacial Surgery, Nagasaki University Graduate School of Biomedical Sciences, Nagasaki, Japan.
Background/purpose: One of the causes of ventilator-associated pneumonia (VAP) is aspiration of oropharyngeal fluid containing pathogenic microorganisms into the lower respiratory tract. In this study, we aimed to investigate whether antibiotic ointment applied to the oral cavity can reduce the number of bacteria in the fluid on the cuff of a tracheal cannula.
Materials And Methods: Tetracycline ointment was applied intraorally once to a patient under endotracheal intubation by postoperative tracheostomy for oral cancer.
Front Bioeng Biotechnol
January 2025
Guangxi Key Laboratory of Oral and Maxillofacial Rehabilitation and Reconstruction, College and Hospital of Stomatology, Guangxi Medical University, Nanning, Guangxi, China.
Introduction: Diabetes mellitus often leads to bone metabolism disorders, hindering bone regeneration and delaying the healing of bone defects. β-Ecdysone, a plant-derived hormone known for its wide range of physiological activities, possesses hypoglycemic effects and promotes osteogenic differentiation. This study developed a composite PLGA slow-release scaffold loaded with β-ecdysone to enhance its bioavailability through topical administration and to investigate its potential to heal diabetic bone defects.
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