title: Diacerein niosomal gel for topical delivery: development, in vitro and in vivo assessment.
abstract: The purpose of this study was to load diacerein (DCR) in niosomes by applying response surface methodology and incorporate these niosomes in gel base for topical delivery. Box-Behnken design was used to investigate the effect of charge-inducing agent (X1), surfactant HLB (X2) and sonication time (X3) on the vesicle size (Y1), entrapment efficiency (Y2) and cumulative drug released (Y3). DCR niosomal formulations were prepared by thin film hydration method. The optimized formula was incorporated in different gel bases. DCR niosomal gels were evaluated for homogeneity, rheological behavior; in vitro release and pharmacodynamic activity by carrageenan-induced hind paw edema method in the rat compared with DCR commercial gel. The results revealed that the mean vesicle sizes of the prepared niosomes ranged from 7.33 to 23.72 µm and the entrapment efficiency ranged from 9.52% to 58.43% with controlled release pattern over 8 h. DCR niosomal gels exhibited pseudoplastic flow with thixotropic behavior. The pharmacodynamic activity of DCR niosomal gel in 3% HPMC showed significant, 37.66%, maximum inhibition of edema size in comparison with 20.83% for the commercial gel (p < 0.05). These results recommended the incorporation of DCR niosomes in 3% HPMC for topical application as a potent anti-inflammatory drug for the treatment of osteoarthritis.
authors: a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , King Abdulaziz University , Jeddah , Saudi Arabia and.|b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Al-Azhar University , Cairo , Egypt.
authors: Khalid M
authors: KM
authors: El-Say
authors: b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Al-Azhar University , Cairo , Egypt.
authors: Fathy I
authors: FI
authors: Abd-Allah
authors: b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Al-Azhar University , Cairo , Egypt.
authors: Ahmed E
authors: AE
authors: Lila
authors: b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Al-Azhar University , Cairo , Egypt.
authors: Abd El-Saboor A
authors: Ael-S
authors: Hassan
authors: b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Al-Azhar University , Cairo , Egypt.
authors: Alaa Eldin A
authors: AE
authors: Kassem
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000880:Anthraquinones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002351:Carrageenan; D016503:Drug Delivery Systems; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005782:Gels; D008081:Liposomes; D008297:Male; D010003:Osteoarthritis / Q000188:drug therapy*; D051381:Rats
chemical_list: D000880:Anthraquinones; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005782:Gels; D008081:Liposomes; C025292:diacerein; D002351:Carrageenan
keywords: Anti-inflammatory activity; Box–Behnken design; osteoarthritis; response surface methodology; thin film hydration