Preparation and Characterization of Capsaicin Encapsulated Polymeric Micelles and Studies of Synergism with Nicotinic Acids as Potential Anticancer Nanomedicines

Abstract

ABSTRACT Background/Objective/Methods: Capsaicin micelles were prepared by the direct dissolution using the amphiphilic copolymer Pluronic P123 and advanced for substantially novel submicro-nanocytotoxicity. Results: Superior cytotoxicity of capsaicin loaded nanomicelles vs. both the raw capsaicin and reference cisplatin in pancreatic PANC1, breast MCF7, colorectal resistant CACO2, skin A375, lung A549 and prostate PC3 cancer cell lines were delineated. Nicotinic acid (NA) derivative 39 (2-Amino IsoNA) had antiinflammatory potential but consistently lacked antiproliferation in MCF7, PANC1 and CACO2. Besides NA derivatives 8 (5-MethylNA) and 44 (6-AminoNA) exhibited lack of antiinflammation but had comparable antitumorigenesis potency to cisplatin in PANC1 cells. Though capsaicin loaded nanomicelles exerted pronounced antiinflammation (with IC50 value of 510 nM vs. Indomethacin’s) in lipopolysacchride-induced inflammation of RAW247.6 macrophages; they lacked DPPH scavenging propensities. Free capsaicin proved more efficacious vs. its loaded nanocarriers to chemosensitize cytotoxicity of combinations with NAs 1(6-Hexyloxy Nicotinic Acid), 5(6-OctyloxyNA), 8(5-MethylNA), 12(6-Thien-2yl-NA), 13(5,6-DichloroNA) and 44(6-AminoNA) in CACO2, PANC1 and prostate PC3. Conclusion: Capsaicin loaded nanomicelles proved more efficacious vs. free capsaicin to chemo-sensitize antiproliferation of cotreatments with NA derivatives, 1, 5, 8, 12, 13 and 44 (in skin A375), 1, 5, 8 and 12 (in breast MCF7), and 1, 5, 12 and 44 (in lung A549).