Abstract
Purpose: To enhance the aqueous solubility and dissolution rate of elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles (SLNs) using solvent injection method.Methods: EVG-loaded SLNs were prepared by solvent injection method. Four different formulations of SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous phase. The SLNs were characterized for various physical properties, including particle size, zeta potential, polydispersity, release profile and entrapment efficiency.Results: The yield of SLNs was in the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes were observed in mean particle size (nm), Z - potential (mV) and polydispersity index (PDI) of the SLNs by varying the concentration of cryoprotectant. EVG – SLNs demonstrated a 800 – 1030-fold enhancement in aqueous solubility compared with plain EVG. The dissolution efficiency (DE) for SLNs was > 63 % in all cases and increased up to 83 % with increasing lipid load.Conclusion: Successful preparation and characterization of elvitegravir–loaded solid lipid nanoparticles by solvent injection method has been accomplished in this study.Keywords: Elvitegravir, Solid lipid nanoparticles, Cryoprotectant, Lipid load, Entrapment efficiency
Highlights
Solid lipid nanoparticles are colloidal carrier systems for controlled drug release
Solvent injection method was selected for the preparation of EVG loaded solid lipid nanoparticles (SLNs)’s which depends on the rapid diffusion of solvent across the solvent lipid interface with the aqueous phase [15]
The Z potential values did not change notably by increasing the lipid load and the obtained Z potential values indicate the formation of stable suspension and there is no particle aggregation observed which is due to charged particles with high Z - potential due to electric repulsion [17,18]
Summary
Solid lipid nanoparticles are colloidal carrier systems for controlled drug release. The main advantage of SLN’s over liposomes, polymeric nanoparticles and polyester nanoparticles is the lipid matrix which decreases the danger of acute and chronic toxicity and has good tolerability [13]. The present investigation uses solvent injection method to prepare EVG-loaded SLNs which is based on the injection of organic phase containing drug in to continuously stirred aqueous phase containing emulsifier and surfactant [9,10,11]. EVG is characterised with poor aqueous solubility so the main intend of the present study is to prepare EVG-loaded SLNs by solvent injection method with enhanced aqueous solubility and dissolution rate. The equilibrium solubility of the pure drug EVG in water was determined by the traditional shake flask method. In vitro release of the drug and EVG SLN’s was studied in USP-II apparatus using 2 % polysorbate 80 in 0.01N Hydrochloric acid as dissolution medium. Different mathematical models were applied to the dissolution data of EVG - SLN’s to study the drug release kinetics. Statistical assessment of dissolution data of EVG and EVG SLNs was done by ANOVA: single factor and t-test; paired two-sample for means, and differences were set p < 0.05
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