Oestrogen receptor-mediated liposomal drug delivery for treating melanoma. (28th May 2018)

• Record Type: Journal Article
• Authors: Ganguly, Anirban; Rachamalla, Hari Krishna Reddy; Bhattacharya, Dwaipayan; Bhamidipati, Keerti; Pal, Abhishek; Gora Ravuri, Halley; Chakravarty, Sumana; Adhikari, Susanta Sekhar; Banerjee, Rajkumar
• Is Part Of: Journal of drug targeting. Volume 26:Number 5/6(2018)
• Page Start: 481
• Page End: 493
• Publication Date: 2018-05-28
• Subjects: Oestrogen receptor -- drug delivery -- docetaxel -- liposome -- melanoma; Drug delivery systems -- Periodicals; Drug Delivery Systems; Vehicles; Drug Administration Routes; Drug Evaluation; 615.7
• DOI: 10.1080/1061186X.2018.1433679
• Languages: English
• ISSNs: 1061-186X

Abstract

Abstract: Function of steroid hormone oestrogen that transactivates oestrogen receptor (ER) is expressed in multiple organs. Except for malignancies of gynaecological organs, ER remains largely unutilised as a target to treat cancers of ER-expressing brain, prostate, skin etc. We have previously developed oestrogen targeting cationic lipid molecule (ES-C10), which showed targeted killing of ER + breast and skin cancer cells. In this study, we explored the targeting ability of ES-C10 as a ligand as well as its additive killing effect (if any), when incorporated in two different liposomes (DCME and DCDE), carrying two anticancer molecules MCIS3 and Docetaxel™, respectively. DCME and DCDE exhibited higher cytotoxicity in ER + cancer cells than in ER − cancer or in non-cancer cells. Both liposomes induced ER-mediated cytotoxicity and caspase 3-induced apoptosis in ER + melanoma cells. Further, decreased levels of pAkt, and increased levels of PTEN and p53 were also observed. Both the targeted liposomes were least haemolytic. These selectively delivered drug-cargoes to tumour mass over other vital organs and induced better anti-tumour effect, which led to increased survivability than their respective controls. In conclusion, we demonstrated the development of two independent liposomal drug-delivery systems associated with an anticancer, oestrogen-structure based ligand for efficient, ER-mediated anti-melanoma effect.