Formulation and evaluation of spray dried liposomes of lopinavir for topical application

Abstract: The anti-HIV therapy is the most capable disease management approach for HIV-AIDS, but its purpose could not fulfill to get maximum bioavailability. In this study, an attempt has been made to develop lopinavir–loaded phospholipid vesicles by using the spray-drying method. Lopinavir loaded spray-dried powder (L-SDP) has been transformed into the vesicles and characterized for physico-chemical properties. Penetration enhancers (PEs) containing cream have been formulated to deliver L-SDP through the skin. Vesicle showed globular shape, 270 nm particle size, polydispersity index (PDI) 0.239, − 34.34 mV zeta potential with 56.38 ± 1.24% entrapment efficiency. In-vitro drug release (%) study through a cellophane membrane showed extended drug release of drug from liposomal formulations in contrast to hydro-alcoholic drug solution (HAS), which released most of the drug within 3–4 h and higher drug release than drug cream. The penetration enhancers (PEs) were selected after investigating their ability to enhance membrane fluidity by FTIR, which showed encouraging outcomes. L-SDP cream with PEs subjected for ex-vivo drug release and skin deposition study using goat facial skins. The cream showed superior drug deposition as well as drug release. The cream containing peppermint oil showed tenfold higher (57.2%) than drug cream (5.91%) and olive oil showed 44.9% drug release. Graphical abstract: [Figure not available: see fulltext.]. © 2018, The Korean Society of Pharmaceutical Sciences and Technology.