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Various alternatives have been developed for improving the physicochemical properties (i.e., solubility) of the AZM without much success. To overcome the problems associated with AZM, an inclusion complex employing a modified cyclodextrin, i.e., sulfobutylether-\u03b2-cyclodextrin (SBE-\u03b2-CD), was prepared and characterized by phase solubility studies and PXRD techniques. The results portrayed the formation of an inclusion complex of AZM with SBE-\u03b2-CD in 1:2 molar stoichiometric ratios. This inclusion complex was later incorporated into a polymer matrix to prepare an in situ gel. Various combinations of Carbopol 934P and hydroxypropyl methylcellulose (HPMC K4M) polymers were used and evaluated by rheological and in vitro drug release studies. The optimized formulation (F4) containing Carbopol 934P (0.2% w\/v) and HPMC K4M (0.2% w\/v) was evaluated for clarity, pH, gelling capacity, drug content, rheological properties, in vitro drug release pattern, ocular irritation test, and antimicrobial efficacy. Finally, owing to the improved antimicrobial efficacy and increased residence time, the AZM:SBE-\u03b2-CD in situ gel was found to be a promising formulation for the efficient treatment of bacterial ocular disease.<\/jats:p>","DOI":"10.1021\/acsomega.1c07218","type":"journal-article","created":{"date-parts":[[2022,6,24]],"date-time":"2022-06-24T13:39:46Z","timestamp":1656077986000},"page":"23050-23060","source":"Crossref","is-referenced-by-count":10,"title":["Cyclodextrin Derivative Enhances the Ophthalmic Delivery\nof Poorly Soluble Azithromycin"],"prefix":"10.1021","volume":"7","author":[{"given":"Anil","family":"Thakur","sequence":"first","affiliation":[{"name":"Lachoo Memorial College of Science and Technology , ,","place":["Jodhpur, India, 342001"]},{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sourabh","family":"Jain","sequence":"additional","affiliation":[{"name":"Lachoo Memorial College of Science and Technology , ,","place":["Jodhpur, India, 342001"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anjali","family":"Pant","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Akanksha","family":"Sharma","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]},{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rajiv","family":"Kumar","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Neha","family":"Singla","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ashish","family":"Suttee","sequence":"additional","affiliation":[{"name":"Lovely Professional University , , ,","place":["Phagwara, Panjab, India, 144411"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Santosh","family":"Kumar","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]},{"name":"S. P. Pune University Campus , , Ganeshkhind , , ,","place":["Pune, Maharashtra, India, 411007"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3156-5357","authenticated-orcid":true,"given":"Ravi P.","family":"Barnwal","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Om Prakash","family":"Katare","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1665-145X","authenticated-orcid":true,"given":"Gurpal","family":"Singh","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2022,6,24]]},"reference":[{"key":"2026081710132669700_cit1","doi-asserted-by":"publisher","first-page":"569","DOI":"10.1002\/prot.22905","article-title":"Temperature-dependent\noligomerization in M-crystallin: lead or lag toward cataract, an NMR\nperspective","volume":"79","author":"Barnwal","year":"2011","journal-title":"Proteins"},{"key":"2026081710132669700_cit2","doi-asserted-by":"publisher","first-page":"675","DOI":"10.1016\/j.jmb.2008.12.058","article-title":"Solution\nStructure and Calcium-Binding Properties of M-Crystallin, A Primordial\n\u03b2\u03b3-Crystallin from Archaea","volume":"386","author":"Barnwal","year":"2009","journal-title":"J. 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Ophthalmol."},{"key":"2026081710132669700_cit7","doi-asserted-by":"publisher","first-page":"1190","DOI":"10.1902\/jop.2015.150024","article-title":"Comparison of Azithromycin\nand Amoxicillin Before Dental Implant Placement: An Exploratory Study\nof Bioavailability and Resolution of Postoperative Inflammation","volume":"86","author":"Escalante","year":"2015","journal-title":"J. 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Sci."},{"key":"2026081710132669700_cit24","doi-asserted-by":"publisher","first-page":"500","DOI":"10.3109\/10717544.2010.483255","article-title":"New method for ophthalmic delivery\nof azithromycin by poloxamer\/carbopol-based in situ gelling system","volume":"17","author":"Cao","year":"2010","journal-title":"Drug Delivery"},{"key":"2026081710132669700_cit25","doi-asserted-by":"publisher","first-page":"887","DOI":"10.1080\/03639040802680271","article-title":"Lipid emulsions\nas a potential delivery system for\nocular use of azithromycin","volume":"35","author":"Liu","year":"2009","journal-title":"Drug Dev. Ind. Pharm."},{"key":"2026081710132669700_cit26","doi-asserted-by":"publisher","first-page":"4862","DOI":"10.1021\/acs.molpharmaceut.8b00516","article-title":"Encapsulation\nof azithromycin ion pair in liposome for enhancing ocular delivery\nand therapeutic efficacy on dry eye","volume":"15","author":"Ren","year":"2018","journal-title":"Mol. 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Ba\u0301sica.\nApl."},{"key":"2026081710132669700_cit45","doi-asserted-by":"publisher","first-page":"1371","DOI":"10.1023\/A:1016290127371","article-title":"Hydroxypropyl-\u03b2-cyclodextrin\nincreases the aqueous solubility and stability of pilocarpine prodrugs","volume":"12","author":"Jarho","year":"1995","journal-title":"J. Pharm. Res."},{"key":"2026081710132669700_cit46","doi-asserted-by":"publisher","first-page":"165","DOI":"10.1016\/S0378-5173(03)00181-9","article-title":"Poly (acrylic acid) micro gels (carbopol\n934)\/surfactant interactions in aqueous media. Part 1: nonionic surfactants","volume":"258","author":"Iglesias","year":"2003","journal-title":"Int. J. Pharm."},{"key":"2026081710132669700_cit47","doi-asserted-by":"publisher","first-page":"211","DOI":"10.1016\/0378-5173(91)90363-S","article-title":"Indomethacin\nand cyclodextrin complexes","volume":"69","author":"Lin","year":"1991","journal-title":"Int. J. 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