The release profiles of acidic form of diclofenac sodium adsorbed on mesoporous silicas (Silochrom and two samples of spherical silicas) were compared with the dissolution characteristics of the pure drug. Desorption of diclofenac sodium from impregnated silicas with various surface liophilicity and composites of silica with chitosan have been studied using rotating basket method in phosphate buffer, pH 6.8. Sedimentations of sodium diclofenac via adsorption and impregnation from alcohol … Show more
“…CHIT is a polycationic polysaccharide derived from deacetylation of chitin [26,27]. The use of CHIT as a natural carrier of controlled release drugs was previously reported [28,29]. This is due to its improved cost effectiveness, biocompatibility, bioavailability, biodegradability, and reduced toxicity.…”
This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon cancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100) microparticles. The release of EA double-coated microparticles (MPs) was tested at simulative pH values. Maximum release was observed at 24 h and pH 7.4. The cytotoxicity of EA MPs on HCT 116 colon cancer cells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry suggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher cell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic activity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation of the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and total cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the double-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography. In conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting as well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared with the administration of raw EA.
“…CHIT is a polycationic polysaccharide derived from deacetylation of chitin [26,27]. The use of CHIT as a natural carrier of controlled release drugs was previously reported [28,29]. This is due to its improved cost effectiveness, biocompatibility, bioavailability, biodegradability, and reduced toxicity.…”
This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon cancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100) microparticles. The release of EA double-coated microparticles (MPs) was tested at simulative pH values. Maximum release was observed at 24 h and pH 7.4. The cytotoxicity of EA MPs on HCT 116 colon cancer cells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry suggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher cell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic activity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation of the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and total cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the double-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography. In conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting as well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared with the administration of raw EA.
“…Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of a phenylacetic acid derivative with analgesic and antipyretic properties. It has been extensively used to relieve menstrual pain, migraines, and arthritis pain 22 . However, the biological half-life of diclofenac was very short (only 1-2 h), which led to the propensity of systemic accumulation.…”
This study is the first report on the preparation of mesoporous carbon/silica (MCS) nanocomposites with tunable mesoporosity and hydrophobicity using natural rubber (NR) as a renewable and cheap carbon source. A series of mesoporous nanocomposites based on NR and hexagonal mesoporous silica (HMS) were prepared via an in situ sol-gel process and used as precursors; then, they were converted into MCS materials by controlled carbonization. The NR/HMS precursors exhibited a high dispersion of rubber phase incorporated into the mesostructured silica framework as confirmed by small-angle X-ray scattering and high-resolution transmission electron microscopy. An increase in the carbonization temperature up to 700 °C resulted in MCS nanocomposites with a well-ordered mesostructure and uniform framework-confined wormhole-like channels. The NR/HMS nanocomposites possessed high specific surface area (500-675 m 2 g −1) and large pore volume (1.14-1.44 cm 3 g −1). The carbon content of MCS (3.0-16.1 wt%) was increased with an increase in the H 2 So 4 concentration. Raman spectroscopy and X-ray photoelectron spectroscopy revealed the high dispersion of graphene oxidelike carbonaceous moieties in MCS materials; the type and amount of oxygen-containing groups in obtained MCS materials were determined by H 2 So 4 concentration. The enhanced hydrophobicity of MCS nanocomposites was related to the carbon content and the depletion of surface silanol groups, as confirmed by the water sorption measurement. The study on the controlled release of diclofenac in simulated gastrointestinal environment suggests a potential application of MCS materials as drug carriers. Mesoporous carbon/silica nanocomposites (MCS) have received considerable attention in catalysis 1 , adsorption 2 , energy storage 3,4 , and drug delivery 5 owing to the combined advantages of inorganic silica and organic carbon in their mesostructure. Silica framework provides high mesoporosity, specific surface area, and thermal/mechanical stability. Due to the high density of silanol groups, the silica surface can be simply modified by either direct co-condensation or postsynthesis grafting to acquire various chemically active functionalities to serve a wide range of applications 6,7. However, amorphous carbon is characterized by its tunable physicochemical properties by controlling the ratio of sp 2 /sp 3 bonds and quantity of heteroatoms (i.e., oxygen) 8,9. The oxygen-containing functional groups on the carbon surface provide acidic (i.e., carboxyl, lactone, and phenol) and basic (i.e., pyrone, chromene, ether, and carbonyl) properties 10. An increase in the amount of sp 2-hybridized carbon transforms amorphous carbon into graphite-like carbon with enhanced textural properties and chemical reactivity 11,12. Typically, the preparation of MCS materials consists of two steps. The first step is to introduce an organic substance (e.g., glucose, furfuryl alcohol, phenol, and formaldehyde) as a carbon source into mesostructured silica. Then, the organic substance is converted to ...
“…Dosadašnja istraživanja bave se vezivanjem diklofenaka na različite prirodne [10][11][12][13] i sintetičke polimere [14][15][16], kao i na derivate celuloze, karboksimetilcelulozu [17] i hidroksipropilmetilcelulozu (HPMC) [18].…”
Izvod Vezivanje ljekovitih preparata na polimerne nosače određeno je vrstom nosača i strukturom samog lijeka. U ovom radu kao polimerni nosač korištena je selektivno oksidovana celuloza (OC) sa 0,547 i 1,163 mmol/g COOH. Dobijena je oksidacijom celuloznog zavoja smjesom HNO3-H3PO4-NaNO2 u trajanju od 5 i 10 časova na temperaturi 25±1 o C, i upotrebljena je za vezivanje analgetika diklofenak-kalijuma. Vezivanje lijeka vršeno je iz vodenog rastvora koncentracija c = 2,5•10-3 , 3,4•10-3 i 5,1•10-3 mol/L na temperaturi 26±1 o C, a desorpcija analgetika u fiziološkom rastvoru. Količine vezanog i otpuštenog lijeka određene su spektrofotometrijski na talasnoj dužini od λmax = 276 nm. Maksimalna količina vezanog lijeka nakon 24 h iznosila je 0,814 mmol/g OC (iz rastvora c = 5,1•10-3 mol/L, na uzorku sa 1,163 mmol/g COOH), a maksimalna količina desorbovanog lijeka 0,063 mmol/g OC (nakon 24 h u fiziološkom rastvoru, uzorak sa 1,163 mmol/g COOH). U radu se proučava uticaj sadržaja COOH grupa i sorpcionih svojstava OC, kao i uticaj hemijske strukture diklofenaka, pH vrijednosti rastvora i trajanja sorpcije na količinu vezanog lijeka. Takođe, ispitana je i prekidna jačina oksidovanih celuloznih vlakana. Ustanovljeno je da se vezivanje lijeka ostvaruje pretežno vodoničnim vezama.
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