title: Preclinical evaluation of a ricinoleic acid poloxamer gel system for transdermal eyelid delivery.
abstract: Our previous study has shown that pluronic lecithin organogel (PLO gel) made of ricinoleic acid has the potential for use as a transdermal eyelid delivery system. The present study deals with the evaluation of ocular tissue concentrations of dexamethasone in a rabbit model following topical application of the gel formulation onto the eyelids. The PLO gel formulation containing dexamethasone was applied to the outside of the eyelid skin. Rabbits were sacrificed at regular time intervals of 2, 4, 8, 12, 20 and 24h. Maxidex(®) eye drops were used as a control. Rabbits were sacrificed and dexamethasone concentrations were analyzed in anterior segment tissues such as the cornea, conjunctiva, aqueous humor, lens, and iris-ciliary body by liquid chromatography tandem mass spectrometry (LC-MS/MS). Rabbit eyes were also examined for ocular irritation and scored using the modified Draize scoring system. No significant irritation or redness was observed in the eyes as compared to the control rabbit eyes. PLO gel formulation resulted in constant dexamethasone concentrations in the anterior segment tissues for up to 24h, which was equivalent or higher than Maxidex(®) eye drops. The findings of this investigation indicate that the ricinoleic acid PLO gel formulation may be clinically effective as a new treatment modality for anterior segment diseases.
authors.affiliation: Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, Ohio 43614, USA. Electronic address: sboddu@utnet.utoledo.edu.
authors.forename: Sai H S
authors.initials: SH
authors.lastname: Boddu
authors.affiliation: Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, Ohio 43614, USA.
authors.forename: Himanshu
authors.initials: H
authors.lastname: Gupta
authors.affiliation: Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, Ohio 43614, USA.
authors.forename: Sindhu Prabha
authors.initials: SP
authors.lastname: Bonam
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D003907:Dexamethasone / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D005123:Eye / Q000378:metabolism*; D005782:Gels; D008297:Male; D020442:Poloxamer / Q000737:chemistry*; D011817:Rabbits; D012277:Ricinoleic Acids / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D005782:Gels; D012277:Ricinoleic Acids; D020442:Poloxamer; D003907:Dexamethasone; C030521:ricinoleic acid
keywords: Lecithin; Pluronic F127; Pluronic lecithin organogel; Rabbit eyelids; Ricinoleic acid; Transdermal