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Novel Formulation of Eye Drops Containing Choline Salicylate and Hyaluronic Acid: Stability, Permeability, and Cytotoxicity Studies Using Alternative Ex Vivo and In Vitro Models.

ABSTRACT: This work investigated the potential of a novel formulation of eye drops containing a non-steroidal anti-inflammatory drug-choline salicylate (CS)-and hyaluronic acid (HA). Thus, these drops may exert both anti-inflammatory and regenerative activity. The experiment was conducted through the careful characterization of physicochemical properties, stability, and quality of eye drops. Moreover, microbiological analysis, as well as penetration and cytotoxic studies, were performed. The UV, HPLC-UV, and HPLC-MS/MS methods were used to determine the purity and stability of CS. The penetration rate of CS was assessed using a hydrophilic membrane and ex vivo porcine cornea model. Additionally, the cytotoxic effects were evaluated using the SIRC cell line. The interaction between HA and CS was tested using size-exclusion chromatography and IR spectrophotometry. As a result, HA increased the viscosity of the drops, which prolonged their contact with the ocular surface, thus ensuring more effective penetration of CS into the corneal structure. After long-term storage, an interaction in the pharmaceutical phase between CS and HA was observed. However, this interaction did not affect the viability of rabbit corneal cells. Our findings showed that eye drops with CS and HA, stored at 2-8 °C in light-protected conditions, met the criteria of stability and safety.

SUBMITTER: Wroblewska KB

PROVIDER: S-EPMC8465216 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:BACKGROUND:Dry eye may be caused or exacerbated by deficient lipid secretion. Recently, lipid-containing artificial tears have been developed to alleviate this deficiency. Our study compared the efficacy, safety, and acceptability of lipid-containing eye drops with that of aqueous eye drops. METHODS:A non-inferiority, randomized, parallel-group, investigator-masked multicenter trial was conducted. Subjects with signs and symptoms of dry eye were randomized to use one of two lipid-containing artificial tears, or one of two aqueous artificial tears. Subjects instilled assigned drops in each eye at least twice daily for 30 days. The primary efficacy analysis tested non-inferiority of a preservative-free lipid tear formulation (LT UD) to a preservative-free aqueous tear formulation (AqT UD) for change in Ocular Surface Disease Index (OSDI) score from baseline at day 30. Secondary measures included OSDI at day 7, tear break-up time (TBUT), corneal and conjunctival staining, Schirmer's test, acceptability and usage questionnaires, and safety assessments. RESULTS:A total of 315 subjects were randomized and included in the analyses. Subjects reported instilling a median of three doses of study eye drops per day in all groups. At days 7 and 30, all groups showed statistically significant improvements from baseline in OSDI (P<0.001) and TBUT (P?0.005). LT UD was non-inferior to AqT UD for mean change from baseline in OSDI score at day 30. No consistent or clinically relevant differences for the other efficacy variables were observed. Acceptability was generally similar across the groups and there was a low incidence of adverse events. CONCLUSION:In this heterogeneous population of dry eye subjects, there were no clinically significant differences in safety, effectiveness, and acceptability between lipid-containing artificial tears and aqueous eye drops. The results suggest that lipid-containing artificial tears can be used to counteract lipid deficiency that is common in dry eye, without compromising overall acceptability.

Project description:Dry eye disease (DED) is a chronic ocular surface disorder often characterized by decreased tear production and rapid tear evaporation that affect tear film stability and homeostasis. The common symptoms of DED include ocular discomfort, visual disturbances, dryness, and itching. Artificial tears are the mainstay of DED management and supplement one or more layers of the tear film. Artificial tear drops are available as a combination of viscosity-enhancing agents (demulcents/lubricants), humectants, and buffers either with or without preservatives. Artificial tears, as a combination of components (polymers/demulcents/viscosity-enhancing agents), can provide synergistic action compared with a single component for the management of multifactorial signs and symptoms of DED. This review describes the formulation components, physicochemical properties, mechanism of action, and summary of preclinical and clinical evidence on the hydroxypropyl guar-hyaluronic acid (HPG-HA) dual-polymer lubricant eye drops (SYSTANE™ HYDRATION). The dual-polymer eye drops consist of dual demulcents (propylene glycol and polyethylene glycol 400) and the polymers hydroxypropyl guar (HPG) and hyaluronic acid (HA). When instilled on the ocular surface, HPG forms a cross-linked gel matrix with borate ions that prolongs the retention of demulcents, thus providing long-lasting lubrication and ocular surface protection. Additionally, HA stabilizes the tear film, increases corneal wettability, and reduces friction during blinks due to its hygroscopic and viscoelastic properties. Preclinical evidence demonstrates that HPG HA dual-polymer lubricant eye drops provide protection against desiccation by cell hydration and surface retention, cell barrier protection, prolonged lubrication, and promotion of corneal re-epithelialization. Clinical scientific evidence demonstrates that HPG HA dual-polymer lubricant eye drops are safe and effective in the management of DED. Specifically, they reduce the signs and symptoms of DED, reduce dry eye symptoms post-cataract surgery, and improve tear film quality in healthy eyes.

Project description:PurposeThe purpose of this study was to evaluate the intraocular pressure (IOP) reduction efficiency of hyaluronic acid-chitosan-latanoprost link nanoparticle (HA-CS-latanoprost link NP) formulated eye drops.MethodsThe IOP reduction study was performed in 24 normotensive albino rabbits. The test animals were randomized and grouped accordingly to treatment namely, HA-CS-latanoprost link NP, plain latanoprost, and the commercially available Xalatan eye drop, all were formulated with 0.005% latanoprost. The 9 days of the experiment were divided into baseline period (days 1-2), treatment period (days 3-6), and recovery period (days 7-9). A wireless noncontact tonometer was used to measure IOP at a time interval of 2 hours for 12 hours per day with 5 readings each.ResultsThe highest mean daily IOP reduction during the treatment period was 24% for plain latanoprost, 23% for Xalatan, and 29% for HA-CS-latanoprost link NP. The maximum reduction in IOP for plain latanoprost and Xalatan all occurred at the sixth hour with the peak effects of 4.85 mm Hg (37%) and 4.8 mm Hg (36%), respectively. Although HA-CS-latanoprost link NP had peak effects of 5.75 mm Hg (43%) at the sixth hour and 5.22 mm Hg (39%) at the eighth hour. Daily mean IOP measurements of each treatment group showed that HA-CS-latanoprost link NP has a greater IOP reduction effect compared with the other two treatments (P < 0.001).ConclusionsThe results showed that the formulation of latanoprost with CS and HA is more effective in reducing the IOP than by drug alone.Translational relevanceThe results provide evidence from animal experiment that HA-CS-latanoprost link NP formulation could improve and sustain drug concentration in the anterior segment of the eye. The improved reduction in IOP with that HA-CS-latanoprost link NP formulation can serve as a basis that latanoprost eye drops can be formulated with decreased concentration of benzalkonium HCl, an irritant preservative and penetration enhancer.

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Novel Formulation of Eye Drops Containing Choline Salicylate and Hyaluronic Acid: Stability, Permeability, and Cytotoxicity Studies Using Alternative Ex Vivo and In Vitro Models.

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