Abstract：
:In the present work, we designed and synthesized a novel mono-guanidine heterolipid (MGH) and confirmed its structure by NMR and ESI-MS. The MGH was used as cationic lipid in developing etoposide loaded cationic self-microemulsifying drug delivery system (ECS) intended to be delivered by intratumoral route. The ECS exhibited size <50 nm and zeta potential +32.6 mV on dilution with various isotonic vehicles with no phase separation or drug precipitation. The ECS could be easily sterilized by membrane filtration method and showed excellent stability for 6 months. The ECS demonstrated excellent in vitro antiproliferative activity against B16F10 cells which is attributed to its high transfection efficiency and capability to cause prolonged drug release in cytosolic space. In vivo antitumor activity of ECS was conducted in B16F10 induced melanoma tumor model. ECS at 12 mg/kg dose showed superior tumor suppression ability and exhibited 100% survival compared to other formulations. Mice treated with ECS by intratumoral route, showed neither systemic side effect nor any evidences of hepatotoxicity and nephrotoxicity. In contrast, etoposide administered by intravenous route showed remarkable systemic toxicity, hepatotoxicity and nephrotoxicity.
journal_name
Biomaterialsjournal_title
Biomaterialsauthors
Shete H,Sable S,Tidke P,Selkar N,Pawar Y,Chakraborty A,De A,Vanage G,Patravale Vdoi
10.1016/j.biomaterials.2015.03.040subject
Has Abstractpub_date
2015-07-01 00:00:00pages
116-32eissn
0142-9612issn
1878-5905pii
S0142-9612(15)00318-Xjournal_volume
57pub_type
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