title: Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties.
abstract: The main purpose of this work was to optimize the rheological properties of docetaxel (DCT)-loaded thermosensitive liquid suppositories for rectal administration. DCT-loaded liquid suppositories were prepared by a cold method and characterized in terms of physicochemical and viscoelastic properties. Major formulation parameters including poloxamer (P407) and Tween 80 were optimized to adjust the thermogelling and mucoadhesive properties for rectal administration. Notably, the gel strength and mucoadhesive force significantly increased with the increase in these variables. Furthermore, DCT incorporation did not alter the viscoelastic behavior, and the mean particle size of nanomicelles in it was approximately 16 nm with a distinct spherical shape. The formulation existed as liquid at room temperature and transformed into gel at physiological temperature through the reverse gelation phenomenon. Thus, DCT-loaded thermosensitive liquid suppositories [DCT/P407/P188/Tween 80 (0.25/11/15/10 %)] with optimal gel properties were easy to prepare and administer rectally, and might enable the gel to stay in the rectum without getting out from rectum.
authors.affiliation: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan, 712-749, South Korea.
authors.forename: Woo Hyun
authors.initials: WH
authors.lastname: Yeo
authors.forename: Thiruganesh
authors.initials: T
authors.lastname: Ramasamy
authors.forename: Dong-Wuk
authors.initials: DW
authors.lastname: Kim
authors.forename: Hyuk Jun
authors.initials: HJ
authors.lastname: Cho
authors.forename: Yong-Il
authors.initials: YI
authors.lastname: Kim
authors.forename: Kwan Hyung
authors.initials: KH
authors.lastname: Cho
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
authors.forename: Han-Gon
authors.initials: HG
authors.lastname: Choi
mesh_terms: D000268:Adhesiveness / Q000187:drug effects; D000285:Administration, Rectal; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D000077143:Docetaxel; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry*; D005260:Female; D011817:Rabbits; D012212:Rheology / Q000379:methods*; D013488:Suppositories; D043823:Taxoids / Q000008:administration & dosage* / Q000737:chemistry*; D013696:Temperature; D014783:Viscosity / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D013488:Suppositories; D043823:Taxoids; D000077143:Docetaxel