Lopinavir Loaded Spray Dried Liposomes with Penetration Enhancers for Cytotoxic Activity.

OBJECTIVE: HIV protease inhibitors (HIV-PI) are the drugs utilized for the treatment of HIV. However, its effectiveness is limited due to lack of bioavailability and need to co-administer with another drug. In this study single lopinavir (LPV) loaded phospholipid vesicles were prepared by the spray-drying method. LPV-loaded spray-dried powder (L-SDP) was transformed into vesicles and then entrapped in a cream base with peppermint and olive oil.

METHOD: Attenuated total reflectance Fourier transform infrared (ATR-FTIR) membrane fluidity study 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, 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 its penetration and inertness of cream in animals.

RESULTS: Membrane fluidity study revealed the effectiveness of oils as penetration enhancers. The L-SDP cream showed superior (%) drug deposition and permeability in comparison. Fluorescence images further confirm the penetration ability of the L-SDP cream and cream showed promising anti-proliferative action on breast and lung cancer cells. Histopathological study demonstrates the inertness of cream while in-vivo bioavailability studies showed the many-fold increase in bioavailability of LPV.

CONCLUSIONS: Liposomal drug delivery system of LPV has potential to deliver skin to the systemic circulation and useful for treating cancer.