ABSTRACT
In the preparation of nanoparticles (NPs) by the nanoprecipitation method, emulsifiers play a key role for NPs' characteristics. The present study aimed to investigate the combined emulsifier effect on ibuprofen loaded poly(lactic-co-glycolic acid) (PLGA) NPs' characteristics and anticancer activity. Ibuprofen loaded PLGA NPs were prepared by nanoprecipitation using different concentrations of PVA (poly(vinyl alcohol)) or PVA-TPGS (d-α-tocopherol polyethylene glycol 1000 succinate) combination as emulsifier. It was found that encapsulation efficiencies of NPs varied between 17.9 and 41.9 % and the highest encapsulation efficiency was obtained with 0.5% PVA + 0.1% TPGS (coded as PLGA PVA/TPGS NPs). PLGA PVA/TPGS NPs were characterized and compared with PLGA PVA NPs, which was obtained by 0.5% PVA alone. Polydispersity index of PLGA PVA/TPGS and PLGA PVA NPs were found to be 0.08 and 0.15, respectively. Incorporation of TPGS with PVA slightly decreased the initial ibuprofen release. Transmission electron microscopy analyses demonstrated a nearly uniform particle size distribution and spherical particle shape of the PLGA PVA/TPGS NPs. Additionally, PLGA PVA/TPGS NPs were significantly more cytotoxic than PLGA PVA NPs on the MCF-7 (human breast adenocarcinoma cells) and Caco-2 (human epithelial colorectal adenocarcinoma) cells (p<0.05). Also PLGA PVA/TPGS NPs were not cytotoxic on normal cells (L929, mouse healthy fibroblast cells) (p>0.05). In conclusion, these results indicated that using a combination of TPGS and PVA as an emulsifier in nanoprecipitation could be a promising approach for preparing ibuprofen loaded PLGA NPs because of their improved characteristics and anticancer activity.
Subject(s)
Antineoplastic Agents/administration & dosage , Emulsifying Agents/chemistry , Ibuprofen/administration & dosage , Nanoparticles , Adenocarcinoma/drug therapy , Adenocarcinoma/pathology , Animals , Antineoplastic Agents/pharmacology , Breast Neoplasms/drug therapy , Breast Neoplasms/pathology , Caco-2 Cells , Chemistry, Pharmaceutical/methods , Colorectal Neoplasms/drug therapy , Colorectal Neoplasms/pathology , Drug Liberation , Female , Humans , Ibuprofen/pharmacology , Lactic Acid/chemistry , MCF-7 Cells , Mice , Microscopy, Electron, Transmission/methods , Particle Size , Polyglycolic Acid/chemistry , Polylactic Acid-Polyglycolic Acid Copolymer , Polyvinyl Alcohol/chemistry , Vitamin E/chemistryABSTRACT
Skin biopsies from three patients with Sézary Syndrome have been labeled in vitro with H-3Thymidine. Labeled cells have been counted in semithin Epon embedded sections and characterized by electron microscopic autoradiography. The ratio of labeled Sézary cells to total lymphocytes was two to four times higher in the epidermis than in the dermis. It is concluded that Sézary cells replicate in the skin and that epidermal cells seem to possess new blastogenic properties in Sézary Syndrome.
