Self-assembled nanomicelles of amphiphilic clotrimazole glycyl-glycine analogue augmented drug delivery, apoptosis and restrained melanoma tumour progression

Materials Science & Engineering. C, Materials for Biological Applications
Amanpreet KaurJitender Madan

Abstract

In present investigation, self-assembled nanomicelles of amphiphilic clotrimazole glycyl-glycine (CLT-GG-SANMs) analogue were customized for augmenting drug delivery, permeability and apoptosis in B16F1 mouse melanoma cancer cells both in vitro and in vivo following intratumoral (i.t.) route of administration. The mean particle size of CLT-GG-SANMs was measured to be 35.9 ± 3.4 nm in addition to zeta-potential of -17.1 ± 3.5 mV. The shape of CLT-GG-SANMs was visualized to be smooth and spherical as like nanoparticles. The critical micellar concentration (CMC) of CLT-GG-SANMs was estimated to be 17 μg/ml using DPH (1,6-diphenyl-1,3,5-hexatriene) as a UV probe. Modification of CLT to CLT-GG-SANMs induced the amorphization in therapeutic moiety. Next, CLT suspension released only 9.7% of the drug within 1 h under dissolution testing and further analysis up to 48 h did not display any remarkable effect on the drug release. On the other hand, CLT-GG-SANMs released 46.2% of the drug significantly (P < 0.01) higher than CLT suspension at 4 h. The IC50 of CLT-GG-SANMs was measured to be 15.1-μM significantly (P < 0.05) lower than CLT suspension (IC50 > 20 μM) in B16F1 cells. Western blotting and histopathological analysis also supporte...Continue Reading

Citations

Nov 2, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Christin DurchscheinNadine Kretschmer

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