Dissolution and antioxidant potential of apigenin self nanoemulsifying drug delivery system (SNEDDS) for oral delivery.

Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as SNEDDS to solve its dissolution problem and enhance oral bioavailability and antioxidant potential. SNEDDS were prepared by mixing Gelucire 44/14, Tween 80, and PEG 400 under controlled conditions.

Controlled Sublimation Rate of Guest Drug from Polymorphic Forms of a Cyclodextrin-Based Polypseudorotaxane Complex and Its Correlation with Molecular Dynamics as Probed by Solid-State NMR.

Encapsulation of active pharmaceutical ingredients (APIs) in confined spaces has been extensively explored as it dramatically alters the molecular dynamics and physical properties of the API. Herein, we explored the effect of encapsulation on the molecular dynamics and physical stability of a guest drug, salicylic acid (SA), confined in the intermolecular spaces of γ-cyclodextrin (γ-CD) and poly(ethylene glycol) (PEG)-based polypseudorotaxane (PPRX) structure. The sublimation tendency of SA encapsulated in three polymorphic forms of the γ-CD/PEG-based PPRX complex, monoclinic columnar (MC), hexagonal columnar (HC), and tetragonal columnar (TC), was investigated.

Analysis of Lutein Content in Microencapsulated Marigold Flower Extract ( L.) Using UHPLC-Q-Orbitrap-HRMS and Its Cytotoxicity in ARPE-19 Cells.

Organic solvents are commonly used to extract lutein. However, they are toxic and are not environmental-friendly. There are only a few reports on the quantification of lutein.

Effects of Wall Material on Medium-Chain Triglyceride (MCT) Oil Microcapsules Prepared by Spray Drying.

A medium-chain triglyceride (MCT) oil microcapsule was prepared by spray drying. The effects of the wall-material parameters of wall-to-oil ratio (1:1 to 3:1) and type of wall material (gum arabic (GA), whey protein isolate (WPI), and octenyl succinic anhydride (OSA) starch) on the microcapsules were evaluated. The droplet size, size distribution, viscosity, zeta potential, and stability of the emulsions were measured.

Non-Destructive Analysis of Chlorpheniramine Maleate Tablets and Granules by Chemometrics-Assisted Attenuated Total Reflectance Infrared Spectroscopy.

Non-destructive analysis of chlorpheniramine maleate (CPM), pharmaceutical tablets, and granules was conducted by chemometrics-assisted attenuated total reflectance infrared spectroscopy (ATR-IR). For tablets, an optimum PLSR model with eight latent factors was obtained from area-normalized and standard normal variate (SNV) pretreated ATR-IR spectral data with correlation coefficients (R) of calibration and cross-validation of 0.9716 and 0.

The nanostructure of rod-like ascorbyl dipalmitate nanoparticles stabilized by a small amount of DSPE-PEG.

Previously, we reported the formation of 100-200 nm disk- and tube-like nanoparticles by hydration of -ascorbyl 2,6-dipalmitate (ASC-DP) and distearoylphosphatidylethanolamine polyethylene glycol 2000 (DSPE-PEG) films prepared at an initial molar ratio of 2:1. This study investigated the feasibility of nanoparticle formation with higher ASC-DP loading. Although particle size distribution determined by dynamic light scattering showed a multimodal pattern including micro-sized particles at a molar ratio of 3:1, the mean particle size gradually decreased with a further increased molar ratio.

Size Reduction Efficiency of Alpha-Mangostin Suspension Using High-Pressure Homogenization.

In this study, we aimed to investigate the effects of stabilizers and processing parameters on the size reduction of alpha-mangostin (AMG) using high-pressure homogenization (HPH). The solubility of AMG in various stabilizers was studied. Selected stabilizers were used to prepare AMG suspensions by HPH under different conditions.

Composition-dependent structural changes and antitumor activity of ASC-DP/DSPE-PEG nanoparticles.

Ascorbyl 2,6-dipalmitate (ASC-DP) and distearoyl phosphatidylethanolamine polyethylene glycol 2000 (DSPE-PEG) formed stable nanoparticles at a molar ratio of less than or equal to 2:1 after dispersing the solvent-evaporated film in water. The mean particle sizes measured by dynamic light scattering were within the range of ca. 100-160nm.

Design of one-dimensional power spectrum using two-dimensional fast Fourier transform for discrimination of paper-based kraft tapes.

A novel type of spectrum, the one-dimensional power spectrum (1D-PS), was designed for the discrimination of adhesive packing tapes, i.e., kraft tapes.

Mechanistic insight into the dramatic improvement of probucol dissolution in neutral solutions by solid dispersion in Eudragit E PO with saccharin.

Objectives: Solid dispersion using Eudragit E PO (EPO) improves the dissolution of poorly water-soluble drugs in acidic solutions; however, the dissolution extremely decreases in neutral solutions. In this report, ternary solid dispersions containing probucol (PBC), EPO, and saccharin (SAC) were prepared to enable high drug dissolution at neutral pH.

Methods: Cryogenic-grinding was used to obtain ternary solid dispersions.

Encapsulation of poorly water-soluble drugs into organic nanotubes for improving drug dissolution.

Hydrocortisone (HC), a poorly water-soluble drug, was encapsulated within organic nanotubes (ONTs), which were formed via the self-assembly of N-{12-[(2-α,β-d-glucopyranosyl) carbamoyl]dodecanyl}-glycylglycylglycine acid. The stability of the ONTs was evaluated in ten organic solvents, of differing polarities, by field emission transmission electron microscopy. The ONTs maintained their stable tubular structure in the highly polar solvents, such as ethanol and acetone.

Drug solubilization mechanism of α-glucosyl stevia by NMR spectroscopy.

We investigated the drug solubilization mechanism of α-glucosyl stevia (Stevia-G) which was synthesized from stevia (rebaudioside-A) by transglycosylation. (1)H and (13)C NMR peaks of Stevia-G in water were assigned by two-dimensional (2D) NMR experiments including (1)H-(1)H correlation, (1)H-(13)C heteronuclear multiple bond correlation, and (1)H-(13)C heteronuclear multiple quantum coherence spectroscopies. The (1)H and (13)C peaks clearly showed the incorporation of two glucose units into rebaudioside-A to produce Stevia-G, supported by steviol glycoside and glucosyl residue assays.

Characterization of cromolyn sodium hydrates and its formulation by (23) Na-multiquantum and magic-angle spinning nuclear magnetic resonance spectroscopy.

We characterized cromolyn sodium (CS) hydrates and evaluated their molecular states in low-dose formulations using Na-multiquantum magic-angle spinning (MQMAS) nuclear magnetic resonance (NMR) analysis. Two CS hydrates, low-water-content hydrated form and high-water-content hydrated form containing 2-3 and 5-6 hydrates, respectively, were prepared by humidification. Single-crystal X-ray diffraction and powder X-ray diffraction analysis revealed that these CS hydrates contained sodium channel structures and that water molecules were adsorbed on the sodium nucleus.

Nano-sized crystalline drug production by milling technology.

Nano-formulation of poorly water-soluble drugs has been developed to enhance drug dissolution. In this review, we introduce nano-milling technology described in recently published papers. Factors affecting the size of drug crystals are compared based on the preparation methods and drug and excipient types.

Mechanistic differences in permeation behavior of supersaturated and solubilized solutions of carbamazepine revealed by nuclear magnetic resonance measurements.

A solid dispersion (SPD) of carbamazepine (CBZ) with hydroxypropyl methylcellulose acetate succinate (HPMC-AS) was prepared by the spray drying method. The apparent solubility (37 °C, pH 7.4) of CBZ observed with the SPD was over 3 times higher than the solubility of unprocessed CBZ.

Formation mechanism of a new carbamazepine/malonic acid cocrystal polymorph.

A new 2/1 carbamazepine (CBZ)/malonic acid (MA) cocrystal polymorph form C was formed using a vibrational rod mill, whereas the known cocrystal polymorph form A was prepared using a ball mill. IR measurements showed that the interaction between CBZ and MA in cocrystal form C was formed by amide-carboxylic acid heterosynthons, similar to that in cocrystal form A. However, NMR results showed that the molecular states of CBZ at the dibenzazepine ring appeared to be different, which could be due to variation in either the conjugation of the aromatic rings or the π-π interaction of CBZ.

Mechanism of nanoparticle formation from ternary coground phenytoin and its derivatives.

The mechanism of drug nanoparticle formation of phenytoin (DPH) and its derivatives monomethylphenytoin (MDPH) and dimethylphenytoin (DMDPH) was investigated. The drug, polyvinylpyrrolidone K17 (PVP), and sodium dodecyl sulfate were coground to obtain the ground mixture (GM). The DPH GM was amorphous; however, MDPH and DMDPH GMs contained drug crystals.

Yellow coloration phenomena of incorporated indomethacin into folded sheet mesoporous materials.

Solid-state (13)C nuclear magnetic resonance (NMR) spectroscopy that included relaxation time measurement was utilized to evaluate the yellow coloration of evaporated samples (EVPs) of indomethacin (IMC) with commercially available folded sheet mesoporous materials (TMPS). Colorimetric analysis by visible light reflection spectroscopy clarified the color differences in each sample: deep yellow-colored melt-quenched amorphous IMC, a slightly yellow-colored EVP of TMPS-1.5 (pore size: 1.

Structural evaluation of probucol nanoparticles in water by atomic force microscopy.

Structural evaluation of probucol nanoparticles coground with polyvinylpyrrolidone K17 and sodium dodecyl sulfate for 90 min was performed by solid-state nuclear magnetic resonance (NMR) spectroscopy and atomic force microscopy (AFM) with force-distance curve analysis. The results of solid-state NMR indicated that the cogrinding changed crystalline probucol to amorphous form. The number-averaged mean heights of probucol particles in the ground mixture (GM) suspension were determined by AFM to be 6 and 15 nm for freshly prepared and 24h-stored samples, respectively.

Discrimination of paper-based kraft tapes using Fourier transform of transmitted light images.

This study focused on two-dimensional fast Fourier transform (2D-FFT) as a new technique for the discrimination of kraft tapes, which is a kind of adhesive packing tape. The 2D power spectrum (2D-PS) obtained by applying 2D-FFT to an image enables us to obtain information about the spatial periodicity, even if the periodicity is invisible within the image. However, in the case of kraft tape, peaks in the 2D-PS are too unclear to determine its periodicity.

Molecular-level characterization of probucol nanocrystal in water by in situ solid-state NMR spectroscopy.

The molecular state of colloidal probucol nanoparticles with additives was evaluated by (13)C in situ solid-state NMR spectroscopy. The nanoparticles were obtained by dispersing a ternary co-ground mixture of probucol/polyvinylpyrrolidon (PVP)/sodium dodecyl sulfate (SDS) in water. Their mean particle size was found to be approximately 150 nm by dynamic light scattering and cryogenic-scanning electron microscopy measurements.

Guest molecular size-dependent inclusion complexation of parabens with cholic acid by cogrinding.

Effects of p-hydroxybenzoate (paraben) ester chain length on the stoichiometry and structure of grinding-induced inclusion complexes with cholic acid (CA) were investigated. Physicochemical properties of the ground mixture were evaluated by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, and solid-state nuclear magnetic resonance (NMR) measurements. Ethyl-, n-propyl-, and isopropyl-parabens formed equimolar inclusion complexes with CA, and the complex structures were of the β-trans bilayer type.

Drug nanoparticle formulation using ascorbic Acid derivatives.

Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside.

Analysis of molecular interactions in solid dosage forms; challenge to molecular pharmaceutics.

The molecular states of active pharmaceutical ingredients (APIs) in pharmaceutical dosage forms strongly affect the properties and quality of a drug. Various important fundamental physicochemical studies were reviewed from the standpoint of molecular pharmaceutics. Mechanochemical effects were evaluated in mixtures of APIs and pharmaceutical additives.

Simultaneous dissolution of naproxen and flurbiprofen from a novel ternary gamma-cyclodextrin complex.

A crystalline ternary complex was prepared by sealed-heating of naproxen (NPX) with a flurbiprofen (FBP)/gamma-cyclodextrin (gamma-CD) inclusion complex. The dissolution rates of NPX and FBP in the ternary complex were almost the same, indicating that FBP and NPX from the complex dissolved simultaneously. The ternary CD complex showing a fascinating dissolution property could be a new formulation for combination therapies.