ubiquinone and cetyl-palmitate

In this study we prepared solid lipid nanoparticles (SLN), by the phase inversion temperature (PIT) method, using cetyl palmitate as solid lipid and three different non-ionic emulsifiers of the polyoxyethylene ethers family (ceteth-20, isoceteth-20, oleth-20). These SLN were loaded with different amount of idebenone (IDE), an antioxidant drug useful in the treatment of neurodegenerative diseases and skin oxidative damages. The differential scanning calorimetry (DSC) was employed to evaluate the effects of the different emulsifiers and the different amounts of drug loaded on the thermotropic behavior of SLN and to investigate how the drug was arranged into these nanoparticles. The IDE seemed to be located into different regions of the SLN depending on its concentration and on the surfactant used. The results of this study suggest that the calorimetric studies performed on SLN could provide valuable information to optimize SLN design and drug release from these carriers.

Topics: Antioxidants; Calorimetry, Differential Scanning; Drug Carriers; Drug Compounding; Drug Liberation; Drug Stability; Ethers; Microscopy, Electron, Transmission; Molecular Structure; Nanoparticles; Palmitates; Particle Size; Polyethylene Glycols; Surface Properties; Surface-Active Agents; Transition Temperature; Ubiquinone

Solid lipid nanoparticles (SLN) are regarded as interesting drug delivery systems and their preparation techniques have gained a great deal of attention.. To evaluate the feasibility of preparing idebenone (IDE) loaded SLN from O/W microemulsions by the phase-inversion temperature (PIT) method. Since SLN have been proposed to improve drug delivery to the brain, IDE was chosen as model drug due to its activity in the treatment of neurodegenerative diseases.. Cetyl palmitate was used as solid lipid to prepare SLN containing two surfactant/cosurfactant mixtures, isoceteth-20/glyceryl oleate (SLN A) and ceteth-20/glyceryl oleate (SLN B) by the PIT method.. All the formulations tested showed a mean particle diameter ranging from 30 to 95 nm and a single peak in size distribution. Stability tests showed that SLN B were more stable than SLN A. IDE release was dependent both on the type of primary surfactant used and the amount of loaded drug. IDE-loaded SLN were effective in inhibiting 2,2'-azobis-(2-amidinopropane)dihydrochloride (APPH)-induced lactic dehydrogenase (LDH) release and reactive oxygen species (ROS) production in primary cultures of astrocytes obtained from rat cerebral cortex. It is noteworthy that SLN B2 (containing ceteth-20 as primary surfactant and 0.7% w/w IDE) were able to prevent entirely both the LDH release and ROS production induced by APPH.. The PIT method provided SLN with good technological properties. The tested SLN could be regarded as interesting carriers to overcome the blood brain barrier and increase the efficacy of the loaded drug.

Topics: Animals; Antioxidants; Astrocytes; Blood-Brain Barrier; Cerebral Cortex; Cetomacrogol; Drug Delivery Systems; Drug Stability; Emulsions; Ethylene Glycols; Fatty Alcohols; Glycerides; In Vitro Techniques; Nanoparticles; Palmitates; Particle Size; Rats; Rats, Wistar; Reactive Oxygen Species; Surface-Active Agents; Tissue Distribution; Ubiquinone

Solid lipid nanoparticles (SLNs) of coenzyme Q10 (CoQ10) were formulated by a high-pressure homogenization method. The best formulation of SLN dispersion consisted of 13% lipid (cetyl palmitate or stearic acid), 8% surfactant (Tween 80 or Tego Care 450), and water. Stability tests, particle size analysis, differential scanning calorimetry, transmission electron microscopy, and release study were conducted to find the best formulation. A simple cream of CoQ10 and a cream containing CoQ10-loaded SLNs were prepared and compared on volunteers aged 20-30 years. SLNs with particle size between 50 nm and100 nm exhibited the most suitable stability. In vitro release profiles of CoQ10 from simple cream, SLN alone, and CoQ10-loaded SLN cream showed prolonged release for SLNs compared with the simple cream, whereas there was no significant difference between SLN alone and SLN in cream. In vitro release studies also demonstrated that CoQ10-loaded SLN and SLN cream possessed a biphasic release pattern in comparison with simple cream. In vivo skin hydration and elasticity studies on 25 volunteers suggested good dermal penetration and useful activity of Q10 on skin as a hydratant and antiwrinkle cream.

Topics: Calorimetry, Differential Scanning; Drug Stability; Female; Humans; Hydrogen-Ion Concentration; Nanoparticles; Palmitates; Particle Size; Polysorbates; Skin; Statistics, Nonparametric; Stearic Acids; Ubiquinone; Young Adult

In the present study, nanostructured lipid carriers (NLC) composed of cetyl palmitate with various amounts of caprylic/capric triacylglycerols (as liquid lipid) were prepared and Coenzyme Q(10) (Q(10)) has been incorporated in such carriers due to its high lipophilic character. A nanoemulsion composed solely of liquid lipid was prepared for comparison studies. By photon correlation spectroscopy a mean particle size in the range of 180-240nm with a narrow polydispersity index (PI) lower than 0.2 was obtained for all developed formulations. The entrapment efficiency was 100% in all cases. The increase of oil loading did not affect the mean particle size of NLC formulations. NLC and nanoemulsion, stabilized by the same emulsifier, showed zeta potential values in the range -40/-50mV providing a good physical stability of the formulations. Scanning electron microscopy studies revealed NLC of disc-like shape. With respect to lipid polymorphism, a decrease in the ordered structure of NLC was observed with the increase of both oil and Q(10) loadings, allowing therefore high accommodation for Q(10) within the NLC. Using static Franz diffusion cells, the in vitro release studies demonstrated that Q(10)-loaded NLC possessed a biphasic release pattern, in comparison to Q(10)-loaded nanoemulsions comprising similar composition of which a nearly constant release was observed. The NLC release patterns were defined by an initial fast release in comparison to the release of NE followed by a prolonged release, which was dependent on the oil content.

Topics: Administration, Topical; Calorimetry, Differential Scanning; Caprylates; Chemical Phenomena; Chemistry, Physical; Coenzymes; Crystallization; Decanoic Acids; Drug Carriers; Drug Compounding; Electrochemistry; Emulsions; Excipients; Liposomes; Microscopy, Electron, Scanning; Nanoparticles; Oils; Palmitates; Particle Size; Solubility; Ubiquinone; X-Ray Diffraction