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OJVRTM

 

Online Journal of Veterinary Research©

(Including Medical and Laboratory Research)

Established 1994

ISSN 1328-925X

 

Volume 28 (7): 434-444, 2024.

          Disposition of  flutamide with or without liposomes in male Wistar rats.

                                                                                            

Umrethia ML, Ghosh PK, Majithiya RJ, Murthy RSR.

 

Pharmacy, M.S. University of Baroda, Vadodara, India

 

ABSTRACT

 

Umrethia ML, Ghosh PK, Majithiya RJ, Murthy RSR., Disposition of  flutamide with or without liposomes in male Wistar rats, Onl J Vet Res., Volume 28 (7): 434-444, 2024. Flutamide is a non-steroidal anti-androgenic for prostate cancer. We encapsulated flutamide within standard liposomes (CL) or phosphotidylcholine, cholesterol and glycol lipids (SL)  by thin film hydration yielding ~99% 136nm in CL and ~98% 158nm in SL.  Flutamide in lyophilized CL and SL was stable 3 months at 2-8°C retained 90% but leakage from CL by 24h only 48% compared with SL ~66% both gone by 48h. Flutamide per se was retained only 3.6% by 4hr. In CL liposome flutamide peaked at 15μg/ml, 1.9 μg/ml by 24h and half life of 17.4h but with SL only 7.9 μg/ml, 0.13 μg/ ml by 24h with half-life of 6.5h whereas flutamide controls only 1.4h. Flutamide in lipid lyposomes was cleared by 24h. Liver and spleen uptake of SL was 82% and 75% less than those of CL. Clearance of control flutamide was 6 and 16X compared with CL and SL, respectively. Microscopy revealed marked hepatic necrosis, fatty degeneration and eccentrically situated nuclei with bile duct proliferation in rats given pure flutamide whereas those given CL cloudy degeneration and patchy necrosis and SL liposomes no pathology. Flutamide boosted alanine transaminase to 453U/L and  CL to 213.3U/L. Our results suggest that 200nm liposomes can be fabricated by thin film hydration and high-pressure homogenization and lyophilized to retain flutamide 24h in human plasma.

 

Keywords: Flutamide, liposomes, pharmacokinetics, biodistribution, histopathology.

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