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access icon free Efavirenz oral delivery via lipid nanocapsules: formulation, optimisation, and ex-vivo gut permeation study

© The Institution of Engineering and Technology
Received 12/01/2018, Accepted 21/03/2018, Revised 06/03/2018, Published 23/03/2018

Present investigation aimed to prepare, optimise, and characterise lipid nanocapsules (LNCs) for improving the solubility and bioavailability of efavirenz (EFV). EFV-loaded LNCs were prepared by the phase-inversion temperature method and the influence of various formulation variables was assessed using Box–Behnken design. The prepared formulations were characterised for particle size, polydispersity index (PdI), zeta potential, encapsulation efficiency (EE), and release efficiency (RE). The biocompatibility of optimised formulation on Caco-2 cells was determined using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Then, it was subjected to ex-vivo permeation using rat intestine. EFV-loaded LNCs were found to be spherical shape in the range of 20–100 nm with EE of 82–97%. The best results obtained from LNCs prepared by 17.5% labrafac and 10% solutol HS15 when the volume ratio of the diluting aqueous phase to the initial emulsion was 3.5. The mean particle size, zeta potential, PdI, EE, drug loading%, and RE during 144 h of optimised formulation were confirmed to 60.71 nm, −35.93 mV, 0.09, 92.60, 7.39 and 55.96%, respectively. Optimised LNCs increased the ex vivo intestinal permeation of EFV when compared with drug suspension. Thus, LNCs could be promising for improved oral delivery of EFV.

Inspec keywords: nanoparticles; molecular biophysics; biomedical materials; particle size; solubility; cellular biophysics; nanomedicine; drugs; encapsulation; drug delivery systems; nanofabrication; emulsions; suspensions; lipid bilayers; toxicology; electrokinetic effects

Other keywords: size 60.71 nm; ex vivo intestinal permeation; EFV-loaded LNC; improved oral delivery; ex-vivo permeation; Caco-2 cells; drug loading; solubility; phase-inversion temperature method; ex-vivo gut permeation study; time 144.0 hour; mean particle size; zeta potential; encapsulation efficiency; size 20.0 nm to 100.0 nm; voltage -35.93 mV; optimisation; Box–Behnken design; 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay; polydispersity index; diluting aqueous phase; optimised formulation; formulation variables; lipid nanocapsules; drug suspension; bioavailability; efavirenz oral delivery

Subjects: Other methods of nanofabrication; Solubility, segregation, and mixing; Emulsions and suspensions; Patient care and treatment; Nanotechnology applications in biomedicine; Cellular biophysics; Patient care and treatment; Membrane biophysics; Structure of solid clusters, nanoparticles, nanotubes and nanostructured materials; Electrochemistry and electrophoresis; Biomedical materials

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