PMID- 34578069 OWN - NLM STAT- PubMed-not-MEDLINE LR - 20210930 IS - 2073-4360 (Electronic) IS - 2073-4360 (Linking) VI - 13 IP - 18 DP - 2021 Sep 18 TI - Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells. LID - 10.3390/polym13183169 [doi] LID - 3169 AB - Rosmarinic acid (RA), one of the most important polyphenol-based antioxidants, has drawn increasing attention because of its remarkable bioactive properties, including anti-inflammatory, anticancer and antibacterial activities. The aim of this study was to synthesize and characterize RA-loaded silk fibroin nanoparticles (RA-SFNs) in terms of their physical-chemical features and composition, and to investigate their antitumor activity against human cervical carcinoma and breast cancer cell lines (HeLa and MCF-7). Compared with the free form, RA bioavailability was enhanced when the drug was adsorbed onto the surface of the silk fibroin nanoparticles (SFNs). The resulting particle diameter was 255 nm, with a polydispersity index of 0.187, and the Z-potential was -17 mV. The drug loading content of the RA-SFNs was 9.4 wt.%. Evaluation of the in vitro drug release of RA from RA-SFNs pointed to a rapid release in physiological conditions (50% of the total drug content was released in 0.5 h). Unloaded SFNs exhibited good biocompatibility, with no significant cytotoxicity observed during the first 48 h against HeLa and MCF-7 cancer cells. In contrast, cell death increased in a concentration-dependent manner after treatment with RA-SFNs, reaching an IC(50) value of 1.568 and 1.377 mg/mL on HeLa and MCF-7, respectively. For both cell lines, the IC(50) of free RA was higher. The cellular uptake of the nanoparticles studied was increased when RA was loaded on them. The cell cycle and apoptosis studies revealed that RA-SFNs inhibit cell proliferation and induce apoptosis on HeLa and MCF-7 cell lines. It is concluded, therefore, that the RA delivery platform based on SFNs improves the antitumor potential of RA in the case of the above cancers. FAU - Fuster, Marta G AU - Fuster MG AD - Chemical Engineering Department, Faculty of Chemistry, Regional Campus of International Excellence "Campus Mare Nostrum", University of Murcia, 30071 Murcia, Spain. FAU - Carissimi, Guzman AU - Carissimi G AUID- ORCID: 0000-0001-8808-7654 AD - Chemical Engineering Department, Faculty of Chemistry, Regional Campus of International Excellence "Campus Mare Nostrum", University of Murcia, 30071 Murcia, Spain. FAU - Montalban, Mercedes G AU - Montalban MG AUID- ORCID: 0000-0003-1085-3042 AD - Chemical Engineering Department, Faculty of Chemistry, Regional Campus of International Excellence "Campus Mare Nostrum", University of Murcia, 30071 Murcia, Spain. FAU - Villora, Gloria AU - Villora G AUID- ORCID: 0000-0002-7325-9131 AD - Chemical Engineering Department, Faculty of Chemistry, Regional Campus of International Excellence "Campus Mare Nostrum", University of Murcia, 30071 Murcia, Spain. LA - eng GR - RG2020-002UM/University of Murcia/ GR - CTQ2017-87708-R/Ministerio de Economia y Competitividad/ GR - PID2020-113081RB-I00/Ministerio de Ciencia e Innovacion/ GR - 20977/PI/18/Fundacion Seneca/ GR - PRE2018-086441/Ministerio de Economia y Competitividad/ PT - Journal Article DEP - 20210918 PL - Switzerland TA - Polymers (Basel) JT - Polymers JID - 101545357 PMC - PMC8467615 OTO - NOTNLM OT - antitumor activity OT - apoptosis OT - cell cycle OT - cell viability OT - cellular uptake OT - nanoparticle OT - rosmarinic acid OT - silk fibroin COIS- The authors declare no conflict of interest. EDAT- 2021/09/29 06:00 MHDA- 2021/09/29 06:01 PMCR- 2021/09/18 CRDT- 2021/09/28 01:25 PHST- 2021/08/29 00:00 [received] PHST- 2021/09/15 00:00 [revised] PHST- 2021/09/16 00:00 [accepted] PHST- 2021/09/28 01:25 [entrez] PHST- 2021/09/29 06:00 [pubmed] PHST- 2021/09/29 06:01 [medline] PHST- 2021/09/18 00:00 [pmc-release] AID - polym13183169 [pii] AID - polymers-13-03169 [pii] AID - 10.3390/polym13183169 [doi] PST - epublish SO - Polymers (Basel). 2021 Sep 18;13(18):3169. doi: 10.3390/polym13183169.