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Mono-guanidine heterolipid based SMEDDS: A promising tool for cytosolic delivery of antineoplastics

Paper ID Volume ID Publish Year Pages File Format Full-Text
5677 412 2015 17 PDF Available
Title
Mono-guanidine heterolipid based SMEDDS: A promising tool for cytosolic delivery of antineoplastics
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.

Keywords
Mono-guanidine heterolipid; Etoposide; Cationic SMEDDS; Intratumoral; Melanoma
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Mono-guanidine heterolipid based SMEDDS: A promising tool for cytosolic delivery of antineoplastics
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 57, July 2015, Pages 116–132
Authors
, , , , , , , , ,
Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us