Journal of Bioequivalence & Bioavailability

Targeted delivery of diethylcarbamazine citrate to the lymphatics using solid lipid nanoparticles

5^th World Congress on Bioavailability and Bioequivalence Pharmaceutical R&D Summit

September 29-October 01, 2014 DoubleTree by Hilton Baltimore-BWI Airport, USA

Siram Karthik

Accepted Abstracts: J Bioequiv Availab

Abstract:

L ymphatic filariasis is a parasitic disease characterized by the presence of adult filarial worms in the lymphatics. Diethylcarbamazine citrate (DEC), because of its hydrophilic nature has poor availability in the lymphatics, which allows the adult worms to reside in the lymphatics. Hence, to target DEC to the lymphatics and to increase its retention time, solid lipid nanoparticles (SLNs) of DEC were prepared by ultrasonication method by varying the proportions of compritol 888 ATO, poloxamer 188 and soya lecithin. The prepared SLNs were evaluated for size, shape, texture, surface charge, physical nature of the entrapped drug and entrapment efficiency. The size of the particles were in the range of 27.25?3.43 nm to 179?3.08 nm and were found to have a spherical morphology. The entrapment efficiencies of the formulations were low and a maximum entrapment efficiency of 68.63?1.53 % was observed. In vitro drug release studies carried out in pH 7.4 PBS displayed a rapid release and the maximum time taken for the complete loaded drug to release was 150 minutes. In vivo studies were carried out in male Sprague Dawley rats to quantify the concentration of DEC in blood and lymph. The results indicated a 4.5 fold increase in the amount of drug that has reached lymphatics when administered through solid lipid nanoparticles. This increased availability of DEC in the lymphatics will help in eradicating the macrofilariae in the lymphatics