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Abstract

Oral administration of anti-cancer drugs is an effective alternative to improve their efficacy and reduce undesired toxicity. Bromelain (BL) is known as an effective anti-cancer phyto-therapeutic agent; however, its activity is reduced upon oral administration. As a result, BL was encapsulated in Poly lactic-co-glycolic acid to formulate nanoparticles (NPs), which were further coated with Eudragit L30D polymer in order to provide stability against the gastric acidic conditions upon oral delivery of NPs. NPs were characterized for BL entrapment, proteolytic activity and mean particle size. The stability and release pattern of NPs was also evaluated under simulated gastrointestinal tract pH conditions. Cytotoxicity studies, carried out in human cell lines of diverse origin showed a significant dose advantage (~7-10 folds) with NPs in reducing the IC50 values as compared to free BL. The cellular uptake of NPs in MCF-7, HeLa cells and Caco-2 cell monolayer was significantly enhanced several folds as compared to free BL. Altered expression of marker proteins associated with apoptosis and cell death (P53, P21, Bcl2, Bax) also confirmed the enhanced anti-carcinogenic potential of formulated NPs. Oral administration of NPs reduced the tumor burden on mice and also increased their life-span when compared with the free BL. The generation of reactive oxygen species, induction of apoptosis and impaired mitochondrial membrane potential in tumor cells treated with NPs confirmed the suitability of NPs as a promising candidate for oral chemotherapy.

Biography

Email: priyankab.chem@gmail.com