Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Nanoscaled devices have great potential for drug delivery applications due to their small size. In the present study, we report for the first time the preparation and evaluation of antitumor efficacy of 5-fluorouracil (5-FU)-entrapped poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles with dependence on the lactide/glycolide combination of PLGA. 5-FU-loaded PLGA nanoparticles with two different monomer combinations, 50-50 and 90-10 were synthesized using a modified double emulsion method, and their biological evaluation was done in glioma (U87MG) and breast adenocarcinoma (MCF7) cell lines. 5-FU-entrapped PLGA 50-50 nanoparticles showed smaller size with a high encapsulation efficiency of 66%, which was equivalent to that of PLGA 90-10 nanoparticles. Physicochemical characterization of nanoparticles using differential scanning calorimetry and X-ray diffraction suggested the presence of 5-FU in molecular dispersion form. In vitro release studies showed the prolonged and sustained release of 5-FU from nanoparticles with both the PLGA combinations, where PLGA 50-50 nanoparticles showed faster release. Nanoparticles with PLGA 50-50 combination exhibited better cytotoxicity than free drug in a dose- and time-dependent manner against both the tumor cell lines. The enhanced efficiency of PLGA 50-50 nanoparticles to induce apoptosis was indicated by acridine orange/ethidium bromide staining. Cell cycle perturbations studied using flow cytometer showed better S-phase arrest by nanoparticles in comparison with free 5-FU. All the results indicate that PLGA 50-50 nanoparticles possess better antitumor efficacy than PLGA 90-10 nanoparticles and free 5-FU. Since, studies have shown that long-term exposure of ailing tissues to moderate drug concentrations is more favorable than regular administration of higher concentration of the drug; our results clearly indicate the potential of 5-FU-loaded PLGA nanoparticles with dependence on carrier combination as controlled release formulation to multiplex the therapeutic effect of cancer chemotherapy

Pharmacognostic Investigation and HPTLC Fingerprinting of a Siddha Polyherbal Drug, Padai chankaran

The present study aims to establish the quality and purity of a Siddha formulation, Padai chankaran by laying down various pharmacognostic parameters, physico-chemical constants and HPTLC fingerprint profiles. Padai chankaran is a Siddha polyherbal preparation comprised of Catunaregum spinosa – root bark, C. spinosa – seed and Alangium salvifolium – root bark as the ingredients. The formulation is used as an external application, having astringent, anthelmintic and antiseptic activities that supports in healing of ulcers and dermatological diseases. Powder microscopy studies and physico-chemical analysis were carried out. Also, an attempt has been made to develop a HPTLC method for phytochemical fingerprinting and the mobile phase Toluene: Ethyl acetate: Formic acid (5: 2: 0.1) gave the best resolution for various components. Hence, the aforesaid analyses confirmed the purity and quality of the Siddha formulation for their future applications. Keywords: Padai chankaran, powder microscopy, physico-chemical, HPTLC studie