piperidines and glyceryl-behenate

Oral squamous cellular carcinoma (OSCC) is considered a life-threatening disease with detection in late stages, which forces us to opt for dangerous treatment with a combination of chemotherapy and radiotherapy. Herbal components such as piperine and quercetin are derived from edible sources, proving their anticancer potential against oral cancer cells in vitro. Encapsulation into lipid matrix-mediated nanostructured lipid carriers (NLCs) can make both drugs bio-accessible. NLCs were synthesised using the high shear homogenisation method and characterised for their physicochemical properties, followed by in vitro cellular evaluation in FaDu oral cancer cells. NLCs showed negatively charged particles smaller than 180 nm with a polydispersity index (PDI) of <0.3. Both drugs were found to encapsulate sufficiently, with >85% entrapment efficiency and an improved drug release profile compared to their pristine counterparts. Differential scanning calorimetry (DSC) thermograms showed conversion into an amorphous matrix in lyophilized NLCs, which was supported by X-ray diffraction (XRD) analysis. The cytotoxicity assay showed the IC

Topics: Alkaloids; Animals; Apoptosis; Benzodioxoles; Drug Liberation; Drug Screening Assays, Antitumor; Fatty Acids; Humans; Membrane Potential, Mitochondrial; Mouth Neoplasms; Nanoparticle Drug Delivery System; Nanostructures; Particle Size; Piperidines; Polyunsaturated Alkamides; Quercetin; Rats; Squamous Cell Carcinoma of Head and Neck; Tissue Distribution

To study the effect of different types of lipid on the entrapment efficiency (EE) and physical stability of repaglinide (RG)-loaded solid lipid nanoparticles (SLNs). RG-loaded SLNs were prepared by modified solvent injection method using stearic acid (RSA), glycerol monosteratae (RGM), glyceryl behenate (RGB) and tristearin (RTS). Poloxamer F68 was used as a stabilizer.. SLNs were characterized by particle size, zeta-potential, EE, in vitro release, solid-state properties (differential scanning calorimetry, transmission electron microscopy and electron diffraction) and stability at 30 degrees C/65% relative humidity for 3 months. The mean particle size and zeta-potential of RG-loaded SLNs prepared with different lipids in varying concentrations ranged from 150 to 355 nm and -21.04 +/- 3.10 to -30.54 +/- 2.76 mV, respectively.. EE was found to vary with lipids in the following order: RSA < RGM < RGB < RTS. Tristearin-prepared SLNs showed a significant prolonged drug release up to 24 h. Differential scanning calorimetry and electron diffraction microphotograph results indicated that RG entrapped in the SLNs existed in an amorphous or molecular state. SLNs prepared with stearic acid, glycerol monostearate and glyceryl behenate after storage showed significant increases in particle size, polydispersity index and EE. The SLNs prepared with tristearin were stable.

Topics: Administration, Oral; Calorimetry, Differential Scanning; Carbamates; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Carriers; Drug Compounding; Drug Stability; Excipients; Fatty Acids; Glycerides; Humidity; Hypoglycemic Agents; Kinetics; Lipids; Microscopy, Electron, Transmission; Nanoparticles; Nanotechnology; Piperidines; Poloxamer; Solubility; Stearic Acids; Technology, Pharmaceutical; Temperature; Triglycerides