Sustained Release Solid Lipid Nanoparticles Formulation of Lumefantrine and Ciprofloxacin

Abstract

In the present study, optimized binary lipid matrices of Tallow fat- Transcutol and Precirol-Transcutol were used to formulate sustained release solid lipid nanoparticles loaded lumefantrine and ciprofloxacin. The homolipid (tallow fat from Bos indicus was extracted and purified following standard methods. Abinitio selection of lipid matrices was done by formulation of binary (3:1) and ternary lipid matrices with different ratios, (1:1:1, 1:2:2 and 2:1:1). Single, binary and ternary lipid matrices were characterized by differential scanning calorimetry (DSC) after which the binary lipid matrices of Precirol- Transcutol and Tallow fat- Transcutol of 3:1 ratio with the least enthalpy were optimized. The optimized lipid matrices were the employed to prepare solid lipid nanoparticles using Poloxamer 188 (2%), Tween 80 (1%) and Solutol HS (3%) as the surfactants by the hot homogenization technique. The following parameters were evaluated on the formulated solid lipid nanoparticles (SLN) –thermal properties, particle size, zeta potential, polydispersity index, particle morphology, encapsulation efficiency ,compatibility/interaction study using FT-IR and in vitro drug release as well as in vivo release using animal model. Solid lipid nanoparticle (SLN)- loaded lumefantrine was directly compressed with artemether to form liquisolid tablets/compacts which were characterized as by weight uniformity, hardness, friability and disintegration time tests. In-vitro release study was performed in simulated gastric fluid (SGF) of pH 1.2 and simulated Intestine fluid (SIF) of pH 7.2 and release data were fitted into zero order, first order, Higuchi and Ritger-Peppas mathematical release models to determine kinetics and mechanism of release. Peter’s 4-day days curative test was carried out in mice with liquisolid compacts lumefantrine –artemether tablets using a chloroquine-sensitive strain of Plasmodium berghei berghei. In-vitro antimicrobial activity was carried out on SLN loaded ciprofloxacin.