Veerawat Teeranachaideekul

Influence of oil content on physicochemical properties and skin distribution of Nile red-loaded NLC

The aims of this study were to investigate the effect of the oil content on the physicochemical properties of NLC and to elucidate the potential of NLC for skin targeting. The obtained results showed that an increase in the oil content did not affect the mean particle size of NLC but impacted on the zeta potential. The inner structure of NLC was influenced by the increasing proportion of oil towards the less ordered structure as confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD), particularly for the higher medium chain triglycerides (MCT) loading. The data from proton nuclear magnetic resonance (1H NMR) revealed that cetyl palmitate nanoparticles did not completely recrystallize after cooling down to room temperature. 1H NMR and DSC results indicate that MCT molecules were restricted in the NLC as compared to the nanoemulsions (NE). Nile red distribution and penetration into skin from NLC were pronounced as compared to NE and dependent on the MCT loading. The deep penetration and high amount of Nile red were related to the occlusion factor. Moreover, the epidermal targeting was achieved by NLC applications, particularly those containing 5% MCT (NLC-5) depending on the amount of MCT loading.

Development of ascorbyl palmitate nanocrystals applying the nanosuspension technology

Ascorbyl palmitate (AP) is an antioxidant used in both cosmetics and food industry. Owing to its poor solubility and instability caused by oxidation having been observed in several colloidal systems, the aim of this study was to investigate the feasibility of applying the nanosuspension technology by high-pressure homogenization (HPH) (DissoCubes) technology) to enhance the chemical stability of AP, followed by lyophilization. Sodium dodecyl sulfate (SDS) and Tween 80 were chosen as emulsifying agents to stabilize the developed AP nanosuspensions. After 3 months of storage at three different temperatures (4 degrees C, 25 degrees C and 40 degrees C), the photon correlation spectroscopy (PCS) analysis of AP nanosuspensions revealed that the mean particle size of those stabilized with SDS significantly increased compared to those stabilized with Tween 80. The results observed from both atomic force microscopy (AFM) and scanning electron microscopy (SEM) revealed AP nanocrystals of cubic-like shape. The percentage of AP remaining in nanosuspensions stabilized with Tween 80 was higher than 90% after 3 months storage at 4 degrees C, 25 degrees C and 40 degrees C. To increase the chemical stability of AP nanosuspensions, a drug powder was prepared by lyophilization. The effect of the presence of cryoprotectant trehalose on the physical stability was evaluated at different concentrations. After redispersing the lyophilized product, the mean size of AP nanosuspensions without trehalose was significantly higher compared with the system with trehalose. After 3 months of storage at 25 degrees C the mean size of lyophilized AP nanosuspensions remained constant. X-ray diffraction revealed the crystalline character of AP nanocrystals after HPH and lyophilization.

Effect of Charged and Non-ionic Membrane Additives on Physicochemical Properties and Stability of Niosomes

The aim of this study was to investigate an influence of different types of membrane additives including negative charge (dicetylphosphate, DCP), positive charge (stearylamine, STR) and non-ionic molecule (cholesteryl poly-24-oxyethylene ether, SC24) on the physicochemical properties of drug-free and drug-loaded niosomes. Salicylic acid having different proportions of ionized and unionized species at different pH was selected as a model drug. The niosomes were composed of 1:1 mole ratio of Span 60: cholesterol as vesicle forming agents. The results show that incorporation of salicylic acid to the niosomes did not affect zeta potential values; however, addition of the membrane additives changed the zeta potential depending on the type of the additives. Transmission electron microscopy revealed that niosomes had unilamellar structure. The particle sizes of all developed niosomes were between 217 to 360xa0nm. The entrapment efficiency (%E.E.) of all salicylic acid niosomes at pHxa03 was higher than that of niosomes at pHxa05, indicating that salicylic acid in unionized form was preferably incorporated in niosomes. Furthermore, the positively charged niosomes showed the highest %E.E. of salicylic acid owing to electrostatic attraction between STR and salicylic acid. After 3xa0months of storage at 4°C, the particle size of the niosomes remained in the nanosize range except for DCP salicylic acid niosomes at pHxa03 whose size increased due to an instability of DCP at low pH. In addition, all niosomes showed no leakage of the salicylic acid after 3xa0months of storage indicating the good stability.

Q10-loaded NLC versus nanoemulsions: stability, rheology and in vitro skin permeation.

In this study, nanoemulsions (NE) of medium chain triacylglycerols (MCT) and nanostructured lipid carriers (NLC) of cetyl palmiate/MCT were produced to load coenzyme Q(10) (Q(10)) and characterized for their stability before and after incorporation into xanthan gum hydrogels. After storage at 4, 25 and 40 degrees C, the particles remained in the nanosize range for 12 months, with zeta potential higher than |40 mV|. Similar results were found in xanthan gum-based hydrogels containing NE or NLC. The crystallinity index of Q(10)-loaded NLC increased after being incorporated into hydrogels. The Q(10) entrapped in NLC and NE remained higher than 90% at all temperatures for 12 months but dramatically decreased when exposed to light. From the rheological studies, both NLC and NE dispersions possessed pseudoplastic flow having more liquid characteristics, whereas NLC and NE hydrogels exhibited plastic flow with thixothopy, showing more elastic rather than viscous properties. The occurrence of a spatial arrangement of lipid molecules was observed in the matrix of NLC when entrapped into hydrogels. From in vitro permeation studies, it could be stated that the amount of Q(10) released and occlusiveness were major keys to promote the deep penetration of Q(10) into the skin.

Physicochemical characterization and in vitro release studies of ascorbyl palmitate-loaded semi-solid nanostructured lipid carriers (NLC gels)

The aim of this study was to characterize the physicochemical properties and to study in vitro release of ascorbyl palmitate from semi-solid lipid nanoparticles based on nanostructured lipid carriers (NLC gels) systems with the desired viscosity for dermal delivery. NLC gels were obtained by a one-step production procedure employing a high pressure homogenization technique using different solid lipid matrices. Ascorbyl palmitate (AP) was selected as a lipophilic active ingredient due to its range of cosmetic applications. After the production, particles within the size range 170–250 nm having polydispersity index lower than 0.3 were obtained from all formulations. After the AP incorporation into the NLC gels, the zeta potential increased to values higher than |30 mV|. Almost 100% encapsulation efficiency was observed. The obtained SEM and AFM data revealed non-spherical shaped nanoparticles. From DSC and X-ray diffraction studies, it was shown that the lipid recrystallized in the solid state possessing a less ordered structure as compared to the bulk material. The release study of active-loaded NLC gel formulations using Franz diffusion cells revealed that the type of lipid matrix affects both the rate and the release pattern. The viscoelastic measurements revealed a more elastic than viscous behaviour of NLC formulations indicating a typical gel-like structure.

Preparation and optimization of chlorophene-loaded nanospheres as controlled release antimicrobial delivery systems

Abstract Chlorophene-loaded nanospheres with various formulation parameters were evaluated. The optimal formulation was found at 0.1% w/v of poloxamer 407, 15u2009mL of ethyl acetate and 20% initial chlorophene loading that provided the suitable size (179u2009nm), the highest loading content (19.2%), encapsulation efficiency (88.0%) and yield (91.6%). Moreover, encapsulation of chlorophene in nanospheres was able to prolong and sustain drug release over one month. Chlorophene-loaded nanospheres were effective against Staphylococcus aureus (S. aureus) and Candida albicans (C. albicans), the main cause of hospital-acquired infections. Chlorophene-loaded nanospheres were effective against S. aureus (>46u2009µg/mL) and C. albicans (>184u2009µg/mL). These nanospheres appeared to have profound effect on the time-dependent hemolytic activity due to gradual release of chlorophene. At the concentration of 46u2009µg/mL, nearly no HRBC hemolysis in 24u2009h compared to 80% of hemolysis from free drug. In conclusion, polymeric nanospheres were successfully fabricated to encapsulate chlorophene which can eliminate inherent toxicity of drugs and have potential uses in prolonged release of antimicrobial.

Effect of binary solid lipid matrix of wax and triglyceride on lipid crystallinity, drug-lipid interaction and drug release of ibuprofen-loaded solid lipid nanoparticles (SLN) for dermal delivery

HYPOTHESISnThe physicochemical properties of solid lipid nanoparticles (SLN) depend on lipid compositions. An addition of secondary solid complex triglycerides (Softisan 378; S378) into solid wax (cetyl palmitate; CP) is expected to influence the properties of obtained SLN compared to SLN prepared from sole CP.nnnEXPERIMENTSnIbuprofen-loaded SLN (IBSLN-TG) composed of different ratios of CP and S378 were prepared and evaluated in term of size, zeta potential (ZP), entrapment efficiency (E.E.), crystallinity, lipid-drug interaction and in vitro drug release.nnnFINDINGSnAfter production, all developed IBSLN-TG prepared from different ratios of CP and S378 had the particle size in the nanometer range (180-200nm) with the ZP values of higher than |-40mV| and possessed approximately 100% E.E. The release of IBSLN-TG demonstrated the biphasic pattern with a fast release followed by sustained release, which was fitted to Higuchis kinetics. The addition of S378 into CP-matrix led to a slight decrease in particle size and surface charge, and distortion of CP crystallization. The results from 1H-NMR indicated the formation of tiny liquid S378 nanocompartments within CP-matrix. The localization of ibuprofen in the S378 nanocompartments and the interaction between ibuprofen and S378 had an impact on the release profiles of IBSLN-TG depending on the ratios of CP and S378.

Fabrication and Evaluation of Eudragit® Polymeric Films for Transdermal Delivery of Piroxicam

Abstract The aims of this work were to develop and characterize the prolonged release piroxicam transdermal patch as a prototype to substitute oral formulations, to reduce side effects and improve patient compliance. The patches were composed of film formers (Eudragit®) as a matrix backbone, with PVC as a backing membrane and PEG200 used as a plasticizer. Results from X-ray diffraction patterns and Fourier transform-infrared spectroscopy indicated that loading piroxicam into films changed the drug crystallinity from needle to an amorphous or dissolved form. Piroxicam films were prepared using Eudragit® RL100 and Eudragit® RS100 as film formers at various ratios from 1:0 to 1:3. Films prepared solely by Eudragit® RL100 showed the toughest and softest film, while other formulations containing Eudragit® RS100 were hard and brittle. Drug release kinetic data from the films fitted with the Higuchi model, and the piroxicam release mechanism was diffusion controlled. Among all formulation tested, Eudragit® RL100 films showed the highest drug release rate and the highest drug permeation flux across human epidermal membrane. Increasing drug loading led to an increase in drug release rate. Eudragit® can be used as a film former for the fabrication of piroxicam films.

Development of γ-Oryzanol Rich Extract from Leum Pua Glutinous Rice Bran Loaded Nanostructured Lipid Carriers for Topical Delivery

Leum Pua is native Thai glutinous rice that contains antioxidants higher than white rice and other colored rice. One of the major antioxidants in rice brans is γ-oryzanol (GO). In this study, Leum Pua glutinous rice bran was extracted by different solvents. Oleic acid (~40 g/100 g extract), linoleic acid (~30 g/100 g extract), and palmitic acid (~20 g/100 g extract) were found to be major lipid components in the extracts. Methanol extract showed less variety of lipid components compared to the others. However, hexane extract showed the highest percent of γ-oryzanol compared to other solvents. Therefore, the hexane extract was selected to prepare nanostructured lipid carriers (NLC). The prepared NLC had small particles in the size range of 142.9 ± 0.4 nm for extract-loaded NLC and 137.1 ± 0.5 nm for GO-loaded NLC with narrow size distribution (PI < 0.1) in both formulations. The release profile of extract-loaded NLC formulation was slightly higher than GO-loaded NLC formulation. However, they did not follow the Higuchi model because of small amounts of γ-oryzanol loaded in NLC particles.