title: Clear, Aqueous Topical Drop of Triamcinolone Acetonide.
abstract: The objective of this study was to develop a clear aqueous mixed nanomicellar formulation (NMF) of triamcinolone acetonide (TA) with a combination of nonionic surfactant hydrogenated castor oil 60 (HCO-60) and octoxynol-40 (Oc-40). In order to delineate the effects of drug-polymer interactions on entrapment efficiency (EE), loading efficiency (LE), and critical micellar concentration (CMC), a design of experiment (DOE) was performed to optimize the formulation. In this study, full-factorial design has been used with HCO-60 and OC-40 as independent variables. All formulations were prepared following solvent evaporation and film rehydration method, characterized with size, polydispersity, shape, morphology, EE, LE, and CMC. A specific blend of HCO-60 and Oc-40 at a particular wt% ratio (5:1.5) produced highest drug EE, LE, and smallest CMC (0.0216 wt%). Solubility of TA in NMF improved 20 times relative to normal aqueous solubility. Qualitative1H NMR studies confirmed the absence of free drug in the outer aqueous NMF medium. Moreover, TA-loaded NMF appeared to be highly stable and well tolerated on human corneal epithelial cells (HCEC) and human retinal pigment epithelial cells (D407 cells). Overall, these studies suggest that TA in NMF is safe and suitable for human topical ocular drop application.
authors.affiliation: Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 5258 Health Science Building, 2464 Charlotte Street, Kansas City, Missouri, 64108-2718, USA.
authors.forename: Hoang M
authors.initials: HM
authors.lastname: Trinh
authors.affiliation: Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 5258 Health Science Building, 2464 Charlotte Street, Kansas City, Missouri, 64108-2718, USA.|RiconPharma LLC, 100 Ford Road, Suite#9, Denville, New Jersey, 07834, USA.
authors.forename: Kishore
authors.initials: K
authors.lastname: Cholkar
authors.affiliation: Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 5258 Health Science Building, 2464 Charlotte Street, Kansas City, Missouri, 64108-2718, USA.
authors.forename: Mary
authors.initials: M
authors.lastname: Joseph
authors.affiliation: Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 5258 Health Science Building, 2464 Charlotte Street, Kansas City, Missouri, 64108-2718, USA.
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Yang
authors.affiliation: Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 5258 Health Science Building, 2464 Charlotte Street, Kansas City, Missouri, 64108-2718, USA. mitraa@umkc.edu.
authors.forename: Ashim K
authors.initials: AK
authors.lastname: Mitra
mesh_terms: D000287:Administration, Topical; D000818:Animals; D002368:Castor Oil / Q000737:chemistry; D003315:Cornea / Q000166:cytology; D004847:Epithelial Cells / Q000187:drug effects; D006801:Humans; D008823:Micelles; D017830:Octoxynol / Q000737:chemistry; D009883:Ophthalmic Solutions; D055213:Retinal Pigment Epithelium / Q000187:drug effects; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D014222:Triamcinolone Acetonide / Q000008:administration & dosage* / Q000633:toxicity; D014867:Water / Q000737:chemistry
chemical_list: D008823:Micelles; D009883:Ophthalmic Solutions; D013501:Surface-Active Agents; D014867:Water; D002368:Castor Oil; D017830:Octoxynol; D014222:Triamcinolone Acetonide
keywords: aqueous mixed nanomicelles; characterization; critical micellar concentration (CMC); cytotoxicity; experiment design; triamcinolone acetonide