Subcutaneous Implants of a Cholesterol-Triglyceride-Buprenorphine Suspension in Rats. (9th April 2017)

• Record Type: Journal Article
• Authors: Guarnieri, M.; Brayton, C.; Sarabia-Estrada, R.; Tyler, B.; McKnight, P.; DeTolla, L.
• Other Names: Laudadio Vito Academic Editor.
• Is Part Of: Journal of veterinary medicine. Volume 2017(2017)
• Publication Date: 2017-04-09
• Subjects: Veterinary medicine -- Periodicals; 636.08905
• DOI: 10.1155/2017/3102567
• Languages: English
• ISSNs: 2356-7708

Abstract

Abstract : A Target Animal Safety protocol was used to examine adverse events in male and female Fischer F344/NTac rats treated with increasing doses of a subcutaneous implant of a lipid suspension of buprenorphine. A single injection of 0.65 mg/kg afforded clinically significant blood levels of drug for 3 days. Chemistry, hematology, coagulation, and urinalysis values with 2- to 10-fold excess doses of the drug-lipid suspension were within normal limits. Histopathology findings were unremarkable. The skin and underlying tissue surrounding the drug injection were unremarkable. Approximately 25% of a cohort of rats given the excess doses of 1.3, 3.9, and 6.5 mg/kg displayed nausea-related behavior consisting of intermittent and limited excess grooming and self-gnawing. These results confirm the safety of cholesterol-triglyceride carrier systems for subcutaneous drug delivery of buprenorphine in laboratory animals and further demonstrate the utility of lipid-based carriers as scaffolds for subcutaneous, long-acting drug therapy.