Objective: HIV protease inhibitors (HIV-PI) are the drugs utilized for the treatment of
HIV. However, their effectiveness is limited due to lack of bioavailability and they need to be coadministered
with another drug. In this study single lopinavir (LPV) loaded phospholipid vesicles
were prepared by the spray-drying method. The LPV-loaded spray-dried powder (L-SDP) was
transformed into vesicles and then entrapped in a cream base with peppermint and olive oil.
Method: It is an Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR) membrane
fluidity study that is used to predict oil’s effect on skin. The central composite design was used to
optimize the L-SDP cream formulation. Ex-vivo drug release, skin deposition study, and cell proliferation
assays were carried out using cancer cell lines of breast, lung, and skin melanoma.
Analysis of DNA by flow cytometry on human breast cancer cell line MDA-MB-231 was carried
out. The fluorescence microscopy, histopathological study, and in-vivo bioavailability studies
were performed to measure the penetration and inertness of cream in animals.
Results: A membrane fluidity study revealed the effectiveness of oils as penetration enhancers.
The L-SDP cream showed comparatively superior (%) drug deposition and permeability . Fluorescence
images further confirm the penetration ability of the L-SDP cream which showed promising
antiproliferative action on breast and lung cancer cells. The histopathological study demonstrates
the inertness of cream while in-vivo bioavailability studies showed the many-fold increase
in bioavailability of LPV.
Conclusions: The liposomal drug delivery system of LPV has the potential to expose skin to systemic
circulation and is useful for treating cancer.