35 research outputs found
Mechanochemistry and solubilization of drugs
The results on solubilization of poorly water-soluble drugs,
indomethacin, piroxicam, and meloxicam, with the help of
mechanochemical methods are presented. The mechanocomposites
of the drugs with various excipients, including soluble
polymers and non-soluble fine porous inorganic oxides, were
obtained by co-grinding using vibrational and planetary
centrifugal mills. The samples obtained revealed higher release rate and apparent solubility of the drugs with respect to the initial ones. Nevertheless, in some cases, e.g. for composites of piroxicam with alumina and ferric oxide, decreasing the release rate and solubility of the drug was observed suggesting the formation of poorly soluble strong drug - carrier associates
Radiation-Thermal Synthesis of Copolymers of Chitosan with Acrylamide as a Means of Betulin Delivering
Π Π°Π΄ΠΈΠ°ΡΠΈΠΎΠ½Π½ΠΎ-ΡΠ΅ΡΠΌΠΈΡΠ΅ΡΠΊΠΈΠΌ
ΠΌΠ΅ΡΠΎΠ΄ΠΎΠΌ Ρ ΠΈΡΠΏΠΎΠ»ΡΠ·ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ ΡΡΠΊΠΎΡΠ΅Π½Π½ΡΡ
ΡΠ»Π΅ΠΊΡΡΠΎΠ½ΠΎΠ²
ΠΏΠΎΠ»ΡΡΠ΅Π½Ρ ΠΏΡΠΈΠ²ΠΈΡΡΠ΅ ΡΠΎΠΏΠΎΠ»ΠΈΠΌΠ΅ΡΡ Ρ
ΠΈΡΠΎΠ·Π°Π½Π° Ρ Π°ΠΊΡΠΈΠ»Π°ΠΌΠΈΠ΄ΠΎΠΌ. ΠΠ±ΡΠ°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ ΠΏΡΠΈΠ²ΠΈΡΡΡ
ΡΠΎΠΏΠΎΠ»ΠΈΠΌΠ΅ΡΠΎΠ²
ΠΏΠΎΠ΄ΡΠ²Π΅ΡΠΆΠ΄Π΅Π½ΠΎ ΠΌΠ΅ΡΠΎΠ΄Π°ΠΌΠΈ ΠΠβΡΠΏΠ΅ΠΊΡΡΠΎΡΠΊΠΎΠΏΠΈΠΈ ΠΈ Π³Π΅Π»Ρ-ΠΏΡΠΎΠ½ΠΈΠΊΠ°ΡΡΠ΅ΠΉ
Ρ
ΡΠΎΠΌΠ°ΡΠΎΠ³ΡΠ°ΡΠΈΠΈ. ΠΠΎΠΊΠ°Π·Π°Π½ΠΎ,
ΡΡΠΎ ΡΡΡΠ΅ΠΊΡΠΈΠ²Π½ΠΎΡΡΡ ΠΈ ΡΡΠ΅ΠΏΠ΅Π½Ρ ΠΏΡΠΈΠ²ΠΈΠ²ΠΊΠΈ Π·Π°Π²ΠΈΡΡΡ ΠΎΡ Π΄ΠΎΠ·Ρ ΠΈΠΎΠ½ΠΈΠ·ΠΈΡΡΡΡΠ΅Π³ΠΎ ΠΎΠ±Π»ΡΡΠ΅Π½ΠΈΡ ΠΈ Ρ ΡΠΎΡΡΠΎΠΌ
Π΄ΠΎΠ·Ρ ΠΏΡΠΎΡ
ΠΎΠ΄ΡΡ ΡΠ΅ΡΠ΅Π· ΠΌΠ°ΠΊΡΠΈΠΌΡΠΌ. ΠΠ°ΠΉΠ΄Π΅Π½Ρ ΡΡΠ»ΠΎΠ²ΠΈΡ ΠΏΠΎΠ»ΡΡΠ΅Π½ΠΈΡ ΡΠΎΠΏΠΎΠ»ΠΈΠΌΠ΅ΡΠΎΠ² Ρ Π²ΡΡΠΎΠΊΠΈΠΌ Π²ΡΡ
ΠΎΠ΄ΠΎΠΌ
ΠΏΡΠΎΠ΄ΡΠΊΡΠ°. ΠΠΎΠ»ΡΡΠ΅Π½Π½ΡΠ΅ ΡΠΎΠΏΠΎΠ»ΠΈΠΌΠ΅ΡΡ ΠΈΡΠΏΠΎΠ»ΡΠ·ΠΎΠ²Π°Π½Ρ Π΄Π»Ρ ΠΏΠΎΠ»ΡΡΠ΅Π½ΠΈΡ ΠΊΠΎΠΌΠΏΠΎΠ·ΠΈΡΠΎΠ² Π±Π΅ΡΡΠ»ΠΈΠ½Π°
Ρ ΠΏΠΎΠΌΠΎΡΡΡ ΠΌΠ΅Ρ
Π°Π½ΠΎΡ
ΠΈΠΌΠΈΡΠ΅ΡΠΊΠΎΠΉ ΠΎΠ±ΡΠ°Π±ΠΎΡΠΊΠΈ. ΠΠΎΠΊΠ°Π·Π°Π½ΠΎ, ΡΡΠΎ ΡΠΊΠΎΡΠΎΡΡΡ Π²ΡΠ΄Π΅Π»Π΅Π½ΠΈΡ Π±Π΅ΡΡΠ»ΠΈΠ½Π° Π² Π²ΠΎΠ΄Π½ΡΠΉ
ΡΠ°ΡΡΠ²ΠΎΡ ΠΏΡΠΈ ΡΠ°ΡΡΠ²ΠΎΡΠ΅Π½ΠΈΠΈ ΠΊΠΎΠΌΠΏΠΎΠ·ΠΈΡΠ° Π·Π°Π²ΠΈΡΠΈΡ ΠΎΡ pH ΡΠ°ΡΡΠ²ΠΎΡΠ°, ΡΡΠΎ ΠΏΠΎΠ·Π²ΠΎΠ»ΡΠ΅Ρ ΡΠ°ΡΡΠΌΠ°ΡΡΠΈΠ²Π°ΡΡ
ΠΌΠ΅Ρ
Π°Π½ΠΎΠΊΠΎΠΌΠΏΠΎΠ·ΠΈΡΡ Π½Π° ΠΎΡΠ½ΠΎΠ²Π΅ ΡΠΎΠΏΠΎΠ»ΠΈΠΌΠ΅ΡΠΎΠ² Ρ
ΠΈΡΠΎΠ·Π°Π½Π° Ρ Π°ΠΊΡΠΈΠ»Π°ΠΌΠΈΠ΄ΠΎΠΌ ΠΊΠ°ΠΊ ΠΏΠ΅ΡΡΠΏΠ΅ΠΊΡΠΈΠ²Π½ΡΠ΅ ΡΡΠ΅Π΄ΡΡΠ²Π°
Π΄Π»Ρ ΠΊΠΎΠ½ΡΡΠΎΠ»ΠΈΡΡΠ΅ΠΌΠΎΠΉ Π΄ΠΎΡΡΠ°Π²ΠΊΠΈ Π»Π΅ΠΊΠ°ΡΡΡΠ²Π΅Π½Π½ΡΡ
Π²Π΅ΡΠ΅ΡΡΠ²Graft copolymers of chitosan with acrylamide were obtained by the radiation-thermal method using accelerated electrons. The formation of graft copolymers was confirmed by IR spectroscopy and gel permeation chromatography. It is shown that the efficiency and degree of grafting depend on the dose of ionizing radiation, and pass through a maximum with increasing dose. The conditions for obtaining copolymers with a high yield of the product were found. The resulting copolymers were used to obtain betulin composites using mechanochemical processing. It has been shown that the rate of release of betulin into an aqueous solution during the dissolution of the composite depends on the pH of the solution, which makes it possible to consider mechanocomposites based on copolymers of chitosan with acrylamide as promising means for controlled drug deliver
Diffusional-kinetic model of the joint dissolution of interacting poorly soluble substances
Effect of ball-milling on the formation of betulin and betulin diacetate composites with polyethylene glycol
Betulin and betulin diacetate (BDA) composites with polyethylene glycol (PEG) were obtained by ball-milling. In case of betulin - PEG mixtures, there was almost complete amorphization under ball-milling. On the contrary, there were no significant changes in the intensity of the reflections in the powder X-ray diffraction patterns for ball-milled mixtures of BDA with PEG. Dissolution of BDA in PEG melts formed at the contacts of particles under collisions with milling bodies leading to crystallization of the drug was suggested. An opportunity to dissolve BDA crystals in PEG melt followed by their crystallization was proven by DSC and hot stage optical microscopic observatio
Effect of the Selected Inorganic Carriers on the Properties of Mechanocomposites with Drugs
Hybrid coreβshell type composites, including organicinorganic composites, possess unique proper
ties and, hence, find use in many areas of science and
technology, in particular, in pharmacy [1]. Mecha
nochemical methods are efficient for the preparation
of such materials because they shorten the duration of
synthesis and avoid using large amounts of organic sol
vents [2]. Rather popular inorganic drug carriers are
highly porous alumina, silica, and magnesia [3, 4].
Hydroxides, which are mechanically softer and, due to
layered structure, can be more easily mechanically
activated are even more promising for the use in pharmacy
ΠΠ»ΠΈΡΠ½ΠΈΠ΅ ΠΌΠΈΠΊΡΠΎΠ²ΠΎΠ»Π½ΠΎΠ²ΠΎΠ³ΠΎ ΠΎΠ±Π»ΡΡΠ΅Π½ΠΈΡ Π½Π° Π°ΡΠ°Π±ΠΈΠ½ΠΎΠ³Π°Π»Π°ΠΊΡΠ°Π½ ΠΈ Π΅Π³ΠΎ Π²Π·Π°ΠΈΠΌΠΎΠ΄Π΅ΠΉΡΡΠ²ΠΈΠ΅ Ρ Π΄ΠΈΠ°ΡΠ΅ΡΠ°ΡΠΎΠΌ Π±Π΅ΡΡΠ»ΠΈΠ½Π°
Π’Π΅ΠΊΡΡ ΡΡΠ°ΡΡΠΈ Π½Π΅ ΠΏΡΠ±Π»ΠΈΠΊΡΠ΅ΡΡΡ Π² ΠΎΡΠΊΡΡΡΠΎΠΌ Π΄ΠΎΡΡΡΠΏΠ΅ Π² ΡΠΎΠΎΡΠ²Π΅ΡΡΡΠ²ΠΈΠΈ Ρ ΠΏΠΎΠ»ΠΈΡΠΈΠΊΠΎΠΉ ΠΆΡΡΠ½Π°Π»Π°.Betulin diacetate (BDA) has a variety of biological activities, but poor solubility in water limits its application. The use of arabinogalactan (AG) as a complexing agent is a promising method for solving the problem of solubilization of drugs. In this study, effect of microwave (MW) irradiation on the properties of AG and BDA and their interaction in aqueous suspension with the formation of a water-soluble supramolecular complex was studied. It is shown that the microwave heating of AG under harsh conditions can lead to degradation of the biopolymer. The use of microwave heating could significantly reduce the complex preparation time compared to the conventional synthesis in a water bath. The preliminary mechanical treatment of the mixture of components, leading to the formation of mechanocomposites, inhibited the reaction between the components in the aqueous suspension under microwave irradiation. The IR spectroscopy method has shown that a supramolecular complex formed under microwave irradiation similar to that formed by conventional heating. The BDA-AG complex was isolated from a microwave heated solution as a thin film, which may be a promising material for pharmaceutical applications
New composites of betulin esters with arabinogalactan as highly potent anti-cancer agents
Betulin and its esters are the natural compounds with high in vitro cytotoxicity toward many cancer cells. However, the poor water solubility of these compounds has limited their applications. We prepared new composites of betulin esters using two methods, namely ball milling of the mixtures of betulin esters with arabinogalactan and preparation of thin films of these mixtures by evaporating the aqueous solutions. These composites revealed higher water solubility as compared to the initial substances without losing the structural integrity and functionality of these compounds. As a result, the new composites have shown much higher inhibitory effects against different cancer cell lines such as Ehrlich ascite carcinoma cells and lung carcinoma cells (A549) in comparison with the initial substances. The cell viability studies based on Annexin V and Propidium iodide probes have confirmed the high proapoptotic effect of betulin esters derivatives against cancer cells
New composites of betulin esters with arabinogalactan as highly potent anti-cancer agents
Betulin and its esters are the natural compounds with high in vitro cytotoxicity toward many cancer cells. However, the poor water solubility of these compounds has limited their applications. We prepared new composites of betulin esters using two methods, namely ball milling of the mixtures of betulin esters with arabinogalactan and preparation of thin films of these mixtures by evaporating the aqueous solutions. These composites revealed higher water solubility as compared to the initial substances without losing the structural integrity and functionality of these compounds. As a result, the new composites have shown much higher inhibitory effects against different cancer cell lines such as Ehrlich ascite carcinoma cells and lung carcinoma cells (A549) in comparison with the initial substances. The cell viability studies based on Annexin V and Propidium iodide probes have confirmed the high proapoptotic effect of betulin esters derivatives against cancer cells