{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,17]],"date-time":"2026-04-17T00:56:44Z","timestamp":1776387404070,"version":"3.51.2"},"reference-count":59,"publisher":"Bentham Science Publishers Ltd.","issue":"9","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["CDD"],"published-print":{"date-parts":[[2023,11]]},"abstract":"<jats:sec>\n<jats:title>Background:<\/jats:title>\n<jats:p>Diacerein, an osteoarthiritis drug, experiences slow topical permeation due to\nlimited solubility. Additionally, it shows a laxative effect due to acid\/base hydrolysis of the drug in the\ncolon.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Objective:<\/jats:title>\n<jats:p>Diacerein solubility was improved to increase percutaneous drug delivery.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Methods:<\/jats:title>\n<jats:p>To improve saturation solubility of the drug, Diacerein was pre-treated with Polysorbate 80\naqueous solution (1% v\/v) to obtain lyophilized powder after wet milling or formulated as solid dispersion\nusing PEG 4000 by fusion method. The lyophilized Diacerein in hydroxypropyl methylcellulose\n(HPMC 8% w\/w) and polyvinyl pyrrolidone (PVP 30% w\/w) matrix, with PEG 400 as co-solvent, provided\nan optimized array. The solid dispersion was loaded in the CMC based gel for subsequent administration\non dissolving microneedle-treated skin.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p>The addition of PEG 400 increased Diacerein loading in microneedles to 390.35\u00b14.28 \u03bcg per\narray. The lyophilized drug displayed amorphous characteristics in the dissolving microneedles as per\nXRD analysis. SEM photographs showed uniformity in the surface topology of microneedles. The needles\nshowed rapid polymer dissolution within 5 minutes, whereas methylene-blue distribution confirmed\nthe formation of microcavities in excised rat skin. The drug-loaded arrays showed better permeation\n(74.39%) and skin deposition (15.75%) after 24 hours, however, \u205312% of Diacerein remained in the\nbaseplate. This led to the tailoring of CMC-based gel (3% w\/v) containing 0.4% solid dispersion of\nDiacerein. When compared to untreated skin, the gel improved permeation rate by 2.43 folds through\naqueous microchannels generated by dissolving microneedle pre-treatment and allowed 98% drug permeation.\nThe quasi-Fickian diffusion mechanism was found to drive ex vivo release kinetics, with a\nshorter lag time (0.88 h) and higher flux (26.65 \u03bcg\/sq.cm.h). Microneedle-assisted Diacerein gel showed\na positive anti-inflammatory effect in the paw edema model and reduced diarrheal episodes in comparison\nto the marketed oral formulation. The gel showed desired characteristics at 5\u00b0C\u00b12\u00b0C when tested\nunder accelerated stability conditions.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p>The present study reports for the first time the verification of efficacy and safety to advocate\nthe suitability of Diacerein for percutaneous delivery through dissolving microneedle-treated skin.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1567201819666220629123058","type":"journal-article","created":{"date-parts":[[2022,6,30]],"date-time":"2022-06-30T07:24:23Z","timestamp":1656573863000},"page":"1351-1367","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Development of a Novel Self-Dissolving Microneedle-Assisted Percutaneous\nDelivery System of Diacerein through Solid Dispersion Gel: Solubility\nEnhancement, Proof of Anti-inflammatory Activity and Safety"],"prefix":"10.2174","volume":"20","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9308-5175","authenticated-orcid":true,"given":"Maryam","family":"Shabbir","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, University of Lahore, Lahore, Punjab, Pakistan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4038-6035","authenticated-orcid":true,"given":"Kashif","family":"Barkat","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, University of Lahore, Lahore, Punjab, Pakistan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Muhammad Umer","family":"Ashraf","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, University of Lahore, Lahore, Punjab, Pakistan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7549-8195","authenticated-orcid":true,"given":"Uzair","family":"Nagra","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, University of Lahore, Lahore, Punjab, Pakistan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"965","reference":[{"key":"ref=1","doi-asserted-by":"publisher","first-page":"478","DOI":"10.1016\/j.joca.2010.09.013","volume":"19","author":"Lane N.E.","year":"2011","unstructured":"Lane N.E.; Brandt K.; Hawker G.; Peeva E.; Schreyer E.; Tsuji W.; Hochberg M.C.; OARSI-FDA initiative: Defining the disease state of osteoarthritis. 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