Open AccessEfavirenz oral delivery via lipid nanocapsules: formulation, optimisation, and ex‐vivo gut permeation study
Author(s) -
Varshosaz Jaleh,
Taymouri Somayeh,
JahanianNajafabadi Ali,
Alizadeh Arezoo
Publication year - 2018
Publication title -
iet nanobiotechnology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.366
H-Index - 38
eISSN - 1751-875X
pISSN - 1751-8741
DOI - 10.1049/iet-nbt.2018.0006
Subject(s) - ex vivo , nanocapsules , permeation , efavirenz , in vivo , solid lipid nanoparticle , drug delivery , chemistry , pharmacology , materials science , nanotechnology , nanoparticle , medicine , virology , human immunodeficiency virus (hiv) , biology , microbiology and biotechnology , antiretroviral therapy , viral load , biochemistry , membrane
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.