{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,30]],"date-time":"2026-07-30T05:22:40Z","timestamp":1785388960025,"version":"3.55.0"},"reference-count":38,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2023,11,28]],"date-time":"2023-11-28T00:00:00Z","timestamp":1701129600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Thailand Science Research and Innovation Fund Chulalongkorn University","award":["RES_67_000_3300_000"],"award-info":[{"award-number":["RES_67_000_3300_000"]}]},{"name":"Thailand Science Research and Innovation Fund Chulalongkorn University","award":["6305001"],"award-info":[{"award-number":["6305001"]}]},{"DOI":"10.13039\/100007684","name":"Asahi Glass Foundation","doi-asserted-by":"publisher","award":["RES_67_000_3300_000"],"award-info":[{"award-number":["RES_67_000_3300_000"]}],"id":[{"id":"10.13039\/100007684","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100007684","name":"Asahi Glass Foundation","doi-asserted-by":"publisher","award":["6305001"],"award-info":[{"award-number":["6305001"]}],"id":[{"id":"10.13039\/100007684","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Thammasat University Research Unit in Drug, Health Product Development and Application (DHP-DA)","award":["RES_67_000_3300_000"],"award-info":[{"award-number":["RES_67_000_3300_000"]}]},{"name":"Thammasat University Research Unit in Drug, Health Product Development and Application (DHP-DA)","award":["6305001"],"award-info":[{"award-number":["6305001"]}]},{"name":"Second Century Fund (C2F) of Chulalongkorn University","award":["RES_67_000_3300_000"],"award-info":[{"award-number":["RES_67_000_3300_000"]}]},{"name":"Second Century Fund (C2F) of Chulalongkorn University","award":["6305001"],"award-info":[{"award-number":["6305001"]}]},{"name":"Office of Academic Affairs, Chulalongkorn University","award":["RES_67_000_3300_000"],"award-info":[{"award-number":["RES_67_000_3300_000"]}]},{"name":"Office of Academic Affairs, Chulalongkorn University","award":["6305001"],"award-info":[{"award-number":["6305001"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>Celecoxib (CCB), a cyclooxygenase-2 inhibitor, is capable of reducing oxidative stress and vascular endothelial growth factor (VEGF) expression in retinal cells and has been shown to be effective in the treatment of diabetic retinopathy and age-related macular degeneration. However, the ocular bioavailability of CCB is hampered due to its very low aqueous solubility. In a previous study, we developed 0.5% (w\/v) aqueous CCB eye drop microsuspensions (MS) containing randomly methylated \u03b2-cyclodextrin (RM\u03b2CD) or \u03b3-cyclodextrin (\u03b3CD) and hyaluronic acid (HA) as ternary CCB\/CD\/HA nanoaggregates. Both formulations exhibited good physicochemical properties. Therefore, we further investigated their cytotoxicity and efficacy in a human retina cell line in this study. At a CCB concentration of 1000 \u03bcg\/mL, both CCB\/RM\u03b2CD and CCB\/\u03b3CD eye drop MS showed low hemolysis activity (11.1 \u00b1 0.3% or 4.9 \u00b1 0.2%, respectively). They revealed no signs of causing irritation and were nontoxic to retinal pigment epithelial cells. Moreover, the CCB eye drop MS exhibited significant anti-VEGF activity by reducing VEGF mRNA and protein levels compared to CCB suspended in phosphate buffer saline. The ex vivo transscleral diffusion demonstrated that a high quantity of CCB (112.47 \u00b1 37.27 \u03bcg\/mL) from CCB\/\u03b3CD eye drop MS was deposited in the porcine sclera. Our new findings suggest that CCB\/CD eye drop MS could be safely delivered to the ocular tissues and demonstrate promising eye drop formulations for retinal disease treatment.<\/jats:p>","DOI":"10.3390\/pharmaceutics15122689","type":"journal-article","created":{"date-parts":[[2023,11,28]],"date-time":"2023-11-28T07:40:01Z","timestamp":1701157201000},"page":"2689","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":12,"title":["Celecoxib\/Cyclodextrin Eye Drop Microsuspensions: Evaluation of In Vitro Cytotoxicity and Anti-VEGF Efficacy for Retinal Diseases"],"prefix":"10.3390","volume":"15","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-7114-8991","authenticated-orcid":false,"given":"Phatsawee","family":"Jansook","sequence":"first","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand"},{"name":"Cyclodextrin Application and Nanotechnology-Based Delivery Systems Research Unit, Chulalongkorn University, Bangkok 10330, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hay Man Saung Hnin","family":"Soe","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rathapon","family":"Asasutjarit","sequence":"additional","affiliation":[{"name":"Thammasat University Research Unit in Drug, Health Product Development and Application (DHP-DA), Department of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Pathum Thani 12120, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Theingi","family":"Tun","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2630-1755","authenticated-orcid":false,"given":"Hay Marn","family":"Hnin","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Phyo Darli","family":"Maw","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4292-4749","authenticated-orcid":false,"given":"Tanapong","family":"Watchararot","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9439-1553","authenticated-orcid":false,"given":"Thorsteinn","family":"Loftsson","sequence":"additional","affiliation":[{"name":"Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2023,11,28]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1753","DOI":"10.1016\/j.ophtha.2017.05.035","article-title":"Prevalence of age-related macular degeneration in europe: The past and the future","volume":"124","author":"Colijn","year":"2017","journal-title":"Ophthalmology"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"428","DOI":"10.4103\/0301-4738.100542","article-title":"The worldwide epidemic of diabetic retinopathy","volume":"60","author":"Zheng","year":"2012","journal-title":"Indian J. 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