cis-Dichlorodiamminoplatinum (II) glyconanoparticles by drug-induced ionic gelation technique targeted to prostate cancer: preparation, optimization and in vitro characterization.

BACKGROUND: Cancer stem cells (CSC) have been proposed as the reason of cancer relapse which are characterized mainly based on CD44+ phenotype with other supplementary markers. The aim of the present study is to fabricate cis-dichlorodiamminoplatinum (II) (CDDP) loaded glyconanoparticles using hyaluronic acid (HA) which is also known as the endogenous substrate for CD44 in vivo. METHODS: For this purpose, a drug-induced ionic gelation technique has been used to prepare CDDP-incorporated nanoparticles. To optimize the fabrication technique, stirring rate, stirring time, and HA/CDDP ratio have been selected as the main factors from other factors and subjected to face-centered central composite design for optimization purposes. The optimized nanoparticles were further characterized using different complementary methods including FTIR, SEM, AFM and DSC. To evaluate the biological effectiveness of CDDP nanoparticles release study, MTS assay, tumor cell clonogenicity and sphere formation assay have been performed as well. RESULTS: Spherical CDDP nanoparticles with Z-average approx. 150nm with low PdI were prepared by adjusting the selected variables. FTIR results indicated the presence of inclusion complexes between CDDP and HA which lead to preparing nanoparticles with high entrapment efficiency and drug content of 87.4 and 43.74 percentage respectively. In vitro release study showed a sustained release of CDDP up to 4 days, and cellular studies confirmed that nanoparticles formation keeps the anticancer activity of formulated CDDP while moderate increase in cancer stem cell suppression. CONCLUSION: It seems hyaluronic acid could be successfully exploited as carrier in cancer-targeted drug delivery with a look at targeting the CSCs.

Effect of Roasting Process on Total Phenolic Compounds and γ-tocopherol Contents of Iranian Sesame Seeds (Sesamum indicum).

Sesame (Sesamum indicum L.) seed and oil have long been used widely as healthy foods to supply energy and prevent aging. Some of the main active anti-oxidative constituents in sesame seeds are γ-tocopherol and phenols. The purpose of this study was to investigate the relationship between roasting temperature and time with γ-tocopherol and total phenolic compounds (TPC) of sesame seeds when roasted in a domestic electric oven. Eight cultivars of sesame seeds in this study were Darab, Dezful, Karaj, Moghan, Naz- Branching, Naz-NonBranching, Siah and Varamin. Each cultivar was divided into ten group based on the roasting time (10, 15 and 20 min) and temperatures (180, 200 and 220 °C)andunroasted one. The high-performance liquid chromatography (HPLC) and spectrophotometeric methods were used for γ-tocopherol (n = 80) and TPC (n = 80) analysis, respectively. The γ-tocopherol content ranged from 329 ± 5 mg/L in Naz-Branching sesame oil to 1114±7 mg/L in Siah sesame oil and 169±6 to 577±1 mg/kg in sesame seed respectively. γ-tocopherol content of six cultivars increased significantly (p < 0.05) as the roasting temperature and time; until 200 °C for 10 min, but they were decreased by roasting at 220 °C in longer time. Also TPC increased significantly as the roasting temperature. The amount of TPC varied in different sesame cultivars from 20.109 ± 3.967 µM to 129.300±3.493 in Varamin and Naz- Branching sesame seed cultivars, respectively, also TPC increased from 70.953 ± 5.863 µM in unroasted Naz-Branching sesame seed to 129.300 ± 3.493 µM after roasting in 200 °C for 20 min. The present study showed that Iranian sesame seed can be considered as a good source of natural antioxidant specially after roasting. The optimum temperature and time roasting to obtain the most γ-tocopherol and total phenolic content was 200 °C for 10 and 20 min, respectively.