Modification of release and penetration behavior of water-soluble active ingredient from ball-milled glutinous starch matrix via carboxymethylcellulose blending

Author(s):  
Ekapol Limpongsa ◽  
May Thu Soe ◽  
Napaphak Jaipakdee
Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1547 ◽  
Author(s):  
Tiziana Esposito ◽  
Francesca Sansone ◽  
Paola Russo ◽  
Patrizia Picerno ◽  
Rita Patrizia Aquino ◽  
...  

The choice of formulation is often of crucial importance in order to obtain a pharmaceutical product for the administration of poorly soluble drugs. Recently, a new water-soluble microparticulate powder form (MTE-mp) for the oral administration of a high functionality/low solubility silymarin rich milk thistle extract (MTE) has been developed. Findings showed that extract-loaded microparticles by spray-drying were produced with high and reproducible yields and encapsulation efficiency. The in vitro dissolution and permeation rates of silymarin were dramatically improved with respect to the raw material, and also enhanced the silymarin anti-inflammatory abilities. Given these successful results, the new MTE-mp delivery system has been proposed as an active ingredient for dermal applications. The aim of this research was the design and development of two topical formulations, hydrogel and emulgel (O/W emulsion), containing the MTE-mp delivery system or MTE raw extract. All the formulations were compared to each other in terms of handling and incorporation amount of the active ingredient during the productive process. Moreover, the addition to the emulgel of lecithin (L) as enhancer of permeation was tested. The MTE-mp ingredient that resulted was stable and more-easily incorporated both in hydrogel and emulgel than raw MTE extract, obtaining the best permeation profile for MTE-mp from emulgel with the addition of L. The obtained results confirm that the MTE-mp system could be used as a stable, water-soluble, and easy-handling functional ingredient, giving the opportunity to develop new strategies for MTE delivery in health products.


2019 ◽  
Vol 55 (No. 2) ◽  
pp. 123-128
Author(s):  
Pavel Kolařík ◽  
Jiří Rotrekl ◽  
Karla Kolaříková

The effectiveness of selected insecticides against capsule weevils (Neoglocianus maculaalba) and capsule midges (Dasineura papaveris), which are the main pests of breadseed poppy, was verified in a small-plot field experiment in 2015–2017. The effect of foliar application was evaluated according to boreholes on capsule surfaces caused by the feeding of capsule weevil adults and larvae numbers in capsules collected approximately 4 weeks after application. Biological efficacy of the tested biological formulations Spintor (active ingredient spinosad 240 g/l) in dosage 0.4 l/ha and NeemAzal T/S (active ingredient azadirachtin A 10.6 g/l) in dosage 3 l/ha against N. maculaalba larvae in individual years of monitoring ranged from 46.4% to 77.7% and from 67.7% to 82.9%, respectively. The effect of the formulation Prev B2 (boron ethanolamine corresponding to 2.1% of water-soluble boron) in 0.3% dosage was in the range of 59.5–81.9%. Their efficacy did not differ significantly compared to the registered chemical standards Biscaya 240 OD (active ingredient thiacloprid 240 g/l) and Decis Mega (active ingredient deltamethrin 50 g/l). Therefore, these biological insecticides are potentially useful for the effective control of N. maculaalba and D. papaveris population densities and reduction of damage they cause to breadseed poppy.


Author(s):  
SIMRANJOT KAUR ◽  
SANDEEP KUMAR

For prolonged time there is a delusion for efficacious targeted drug delivery system, but the chemistry hold complex form had made situations thorny, but the development of new colloidal carrier called nanosponges (NSs) likely circumvent these problems. NSs are the nanoporous particles that can entangle a huge range of material and then be engulfed into a suitable formulation depend on the route of administration. They prevent the drug-protein degradation, lengthen the drug release in a controlled manner, and release the medicament to the target site. They can travel around the body and attach on the surface and liberate the drug in a controlled and predictable manner at the specific target site. They are fine aqueous solubility which makes them a bearer for low water-soluble drugs. Drugs having low bioavailability are best suited for this type of carrier system. Both lipophilic and hydrophilic drugs can be included in NSs. Particle size can change from smaller to bigger by varying the amount of crosslinker to the polymer. Various applications of NSs such as recovering bioavailability of active ingredient molecule and delivery of active ingredient into oral, topical, parenteral, and nasal route make them a superior candidate for targeted delivery of drugs. It can be used as a shipper for biocatalysts in the transport and release of enzymes, proteins, vaccines, and antibodies. They can be prepared by different methods such as emulsion solvent diffusion method, melt method, ultrasound-assisted method, Quasi emulsion solvent diffusion method. This analysis is focusing on the advantages, formulation, evaluation, application, and patent report of the NSs.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 211
Author(s):  
Petra Party ◽  
Csilla Bartos ◽  
Árpád Farkas ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus

Pulmonary delivery has high bioavailability, a large surface area for absorption, and limited drug degradation. Particle engineering is important to develop inhalable formulations to improve the therapeutic effect. In our work, the poorly water-soluble meloxicam (MX) was used as an active ingredient, which could be useful for the treatment of non-small cell lung cancer, cystic fibrosis, and chronic obstructive pulmonary disease. We aimed to produce inhalable “nano-in-micro” dry powder inhalers (DPIs) containing MX and additives (poly-vinyl-alcohol, leucine). We targeted the respiratory zone with the microcomposites and reached a higher drug concentration with the nanonized active ingredient. We did the following investigations: particle size analysis, morphology, density, interparticular interactions, crystallinity, in vitro dissolution, in vitro permeability, in vitro aerodynamics (Andersen cascade impactor), and in silico aerodynamics (stochastic lung model). We worked out a preparation method by combining wet milling and spray-drying. We produced spherical, 3–4 µm sized particles built up by MX nanoparticles. The increased surface area and amorphization improved the dissolution and diffusion of the MX. The formulations showed appropriate aerodynamical properties: 1.5–2.4 µm MMAD and 72–76% fine particle fraction (FPF) values. The in silico measurements proved the deposition in the deeper airways. The samples were suitable for the treatment of local lung diseases.


Author(s):  
J. G. Robertson ◽  
D. F. Parsons

The extraction of lipids from tissues during fixation and embedding for electron microscopy is widely recognized as a source of possible artifact, especially at the membrane level of cell organization. Lipid extraction is also a major disadvantage in electron microscope autoradiography of radioactive lipids, as in studies of the uptake of radioactive fatty acids by intestinal slices. Retention of lipids by fixation with osmium tetroxide is generally limited to glycolipids, phospholipids and highly unsaturated neutral lipids. Saturated neutral lipids and sterols tend to be easily extracted by organic dehydrating reagents prior to embedding. Retention of the more saturated lipids in embedded tissue might be achieved by developing new cross-linking reagents, by the use of highly water soluble embedding materials or by working at very low temperatures.


Author(s):  
J. D. McLean ◽  
S. J. Singer

The successful application of ferritin labeled antibodies (F-A) to ultrathin sections of biological material has been hampered by two main difficulties. Firstly the normally used procedures for the preparation of material for thin sectioning often result in a loss of antigenicity. Secondly the polymers employed for embedding may non-specifically absorb the F-A. Our earlier use of cross-linked polyampholytes as embedding media partially overcame these problems. However the water-soluble monomers used for this method still extract many lipids from the material.


Author(s):  
D.R. Mattie ◽  
J.W. Fisher

Jet fuels such as JP-4 can be introduced into the environment and come in contact with aquatic biota in several ways. Studies in this laboratory have demonstrated JP-4 toxicity to fish. Benzene is the major constituent of the water soluble fraction of JP-4. The normal surface morphology of bluegill olfactory lamellae was examined in conjunction with electrophysiology experiments. There was no information regarding the ultrastructural and physiological responses of the olfactory epithelium of bluegills to acute benzene exposure.The purpose of this investigation was to determine the effects of benzene on the surface morphology of the nasal rosettes of the bluegill sunfish (Lepomis macrochirus). Bluegills were exposed to a sublethal concentration of 7.7±0.2ppm (+S.E.M.) benzene for five, ten or fourteen days. Nasal rosettes were fixed in 2.5% glutaraldehyde and 2.0% paraformaldehyde in 0.1M cacodylate buffer (pH 7.4) containing 1.25mM calcium chloride. Specimens were processed for scanning electron microscopy.


Author(s):  
H. J. Arnott ◽  
M. A. Webb ◽  
L. E. Lopez

Many papers have been published on the structure of calcium oxalate crystals in plants, however, few deal with the early development of crystals. Large numbers of idioblastic calcium oxalate crystal cells are found in the leaves of Vitis mustangensis, V. labrusca and V. vulpina. A crystal idioblast, or raphide cell, will produce 150-300 needle-like calcium oxalate crystals within a central vacuole. Each raphide crystal is autonomous, having been produced in a separate membrane-defined crystal chamber; the idioblast''s crystal complement is collectively embedded in a water soluble glycoprotein matrix which fills the vacuole. The crystals are twins, each having a pointed and a bidentate end (Fig 1); when mature they are about 0.5-1.2 μn in diameter and 30-70 μm in length. Crystal bundles, i.e., crystals and their matrix, can be isolated from leaves using 100% ETOH. If the bundles are treated with H2O the matrix surrounding the crystals rapidly disperses.


Author(s):  
B. J. Grenon ◽  
A. J. Tousimis

Ever since the introduction of glutaraldehyde as a fixative in electron microscopy of biological specimens, the identification of impurities and consequently their effects on biologic ultrastructure have been under investigation. Several reports postulate that the impurities of glutaraldehyde, used as a fixative, are glutaric acid, glutaraldehyde polymer, acrolein and glutaraldoxime.Analysis of commercially available biological or technical grade glutaraldehyde revealed two major impurity components, none of which has been reported. The first compound is a colorless, water-soluble liquid with a boiling point of 42°C at 16 mm. Utilizing Nuclear Magnetic Resonance (NMR) spectroscopic analysis, this compound has been identified to be — dihydro-2-ethoxy 2H-pyran. This impurity component of the glutaraldehyde biological or technical grades has an UV absorption peak at 235nm. The second compound is a white amorphous solid which is insoluble in water and has a melting point of 80-82°C. Initial chemical analysis indicates that this compound is an aldol condensation product(s) of glutaraldehyde.


2020 ◽  
Vol 56 (65) ◽  
pp. 9332-9335
Author(s):  
Sandra Estalayo-Adrián ◽  
Salvador Blasco ◽  
Sandra A. Bright ◽  
Gavin J. McManus ◽  
Guillermo Orellana ◽  
...  

Two new water-soluble amphiphilic Ru(ii) polypyridyl complexes were synthesised and their photophysical and photobiological properties evaluated; both complexes showed a rapid cellular uptake and phototoxicity against HeLa cervical cancer cells.


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