{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,22]],"date-time":"2026-07-22T23:23:01Z","timestamp":1784762581999,"version":"3.55.0"},"reference-count":58,"publisher":"MDPI AG","issue":"14","license":[{"start":{"date-parts":[[2022,7,20]],"date-time":"2022-07-20T00:00:00Z","timestamp":1658275200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Researchers Supporting Project","award":["RSP-2022-R490"],"award-info":[{"award-number":["RSP-2022-R490"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>The aim of this study was the successful utilization of the positively charged nanocrystals (NCs) of Tedizolid Phosphate (TZP) (0.1% w\/v) for topical ocular applications. TZP belongs to the 1, 3-oxazolidine-2-one class of antibiotics and has therapeutic potential for the treatment of many drug-resistant bacterial infections, including eye infections caused by MRSA, penicillin-resistant Streptococcus pneumonia and vancomycin-resistant Enterococcus faecium. However, its therapeutic usage is restricted due to its poor aqueous solubility and limited ocular availability. It is a prodrug and gets converted to Tedizolid (TDZ) by phosphatases in vivo. The sterilized NC1 was subjected to antimicrobial testing on Gram-positive bacteria. Ocular irritation and pharmacokinetics were performed in rabbits. Around a 1.29 to 1.53-fold increase in antibacterial activity was noted for NC1 against the B. subtilis, S. pneumonia, S. aureus and MRSA (SA-6538) as compared to the TZP-pure. The NC1-AqS was \u201cpractically non-irritating\u201d to rabbit eyes. There was around a 1.67- and 1.43 fold increase in t1\/2 (h) and Cmax (ngmL\u22121) while there were 1.96-, 1.91-, 2.69- and 1.41-times increases in AUC0\u201324h,AUC0\u2013\u221e,AUMC0\u2013\u221e and MRT0\u2013\u221e, respectively, which were found by NC1 as compared to TZP-AqS in the ocular pharmacokinetic study. The clearance of TDZ was faster (11.43 mLh\u22121) from TZP-AqS as compared to NC1 (5.88 mLh\u22121). Relatively, an extended half-life (t1\/2; 4.45 h) of TDZ and the prolonged ocular retention (MRT0\u2013\u221e; 7.13 h) of NC1 was found, while a shorter half-life (t1\/2; 2.66 h) of TDZ and MRT0\u2013\u221e(t1\/2; 5.05 h)was noted for TZP-AqS, respectively. Cationic TZP-NC1 could offer increased transcorneal permeation, which could mimic the improved ocular bioavailability of the drug in vivo. Conclusively, NC1 of TZP was identified as a promising substitute for the ocular delivery of TZP, with better performance as compared to its conventional AqS.<\/jats:p>","DOI":"10.3390\/molecules27144619","type":"journal-article","created":{"date-parts":[[2022,7,21]],"date-time":"2022-07-21T03:34:40Z","timestamp":1658374480000},"page":"4619","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["Perspectives of Positively Charged Nanocrystals of Tedizolid Phosphate as a Topical Ocular Application in Rabbits"],"prefix":"10.3390","volume":"27","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1306-1625","authenticated-orcid":false,"given":"Abdullah","family":"Alshememry","sequence":"first","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Musaed","family":"Alkholief","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5713-8858","authenticated-orcid":false,"given":"Mohd","family":"Abul Kalam","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6015-6125","authenticated-orcid":false,"given":"Mohammad","family":"Raish","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9892-2158","authenticated-orcid":false,"given":"Raisuddin","family":"Ali","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8418-9311","authenticated-orcid":false,"given":"Sulaiman S.","family":"Alhudaithi","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5821-5600","authenticated-orcid":false,"given":"Muzaffar","family":"Iqbal","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8950-6571","authenticated-orcid":false,"given":"Aws","family":"Alshamsan","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,7,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"184","DOI":"10.1007\/s00347-017-0596-6","article-title":"Nanoparticles as drug delivery systems in ophthalmology","volume":"115","author":"Loscher","year":"2018","journal-title":"Ophthalmologe"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"3","DOI":"10.2174\/1389201053167158","article-title":"The impact of nanobiotechnology on the development of new drug delivery systems","volume":"6","author":"Kayser","year":"2005","journal-title":"Curr. 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