Abstract:
:Clinical use of camptothecin (CPT) is hindered due to its poor water and oil solubility, active lactone ring instability and non-targeted toxicity. Recently we reported formulation of camptothecin microemulsions with increased solubility for the improved treatment of breast cancer. In this research chitosan stabilized camptothecin nanoemulsions (CHI-CPT-NEs) were formulated improve the cancer targeting efficiency of CPT. The developed NEs were characterized for their droplet size distribution, stability in plasma and evaluated for in-vitro drug release, in-vivo targeting potential, in-vitro hemolytic potential, cytotoxicity, genotoxicity and in-vivo biodistribution. The CHI-CPT-NEs showed uniform droplet size distribution, extended drug release (61.65±1.57% at 24h), tolerable hemolytic potential (16.4±1.4%), significant cytotoxicity (178±4.3ng/ml) against MCF-7 cancer cells and low DNA damage to lymphocytes. In-vivo biodistribution study conducted in 4T1-breast tumor xenograft BALB/c mice showed that 2495.22±174.66ng/gm of camptothecin was passively targeted to breast cancer by CHI-CPT-NEs compared to the non-stabilized nanoemulsion (1677.58±134.21ng/gm). Thus, passive targeting of developed CHI-CPT-NEs may provide a promising approach for the efficient breast cancer therapy.
journal_name
Int J Biol Macromoljournal_title
International journal of biological macromoleculesauthors
Natesan S,Sugumaran A,Ponnusamy C,Thiagarajan V,Palanichamy R,Kandasamy Rdoi
10.1016/j.ijbiomac.2017.05.127subject
Has Abstractpub_date
2017-11-01 00:00:00pages
1846-1852issue
Pt Beissn
0141-8130issn
1879-0003pii
S0141-8130(16)32673-3journal_volume
104pub_type
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