- Double Drug Delivery Using Capped Mesoporous Silica Microparticles for the Effective Treatment of Inflammatory Bowel Disease
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Silica mesoporous microparticles loaded with both rhodamine B fluorophore (S1) or hydrocortisone (S2), and capped with an olsalazine derivative, are prepared and fully characterized. Suspensions of S1 and S2 in water at an acidic and a neutral pH show negligible dye/drug release, yet a notable delivery took place when the reducing agent sodium dithionite is added because of hydrolysis of an azo bond in the capping ensemble. Additionally, olsalazine fragmentation induced 5-aminosalicylic acid (5-ASA) release. In vitro digestion models show that S1 and S2 solids are suitable systems to specifically release a pharmaceutical agent in the colon. In vivo pharmacokinetic studies in rats show a preferential rhodamine B release from S1 in the colon. Moreover, a model of ulcerative colitis is induced in rats by oral administration of 2,4,6-trinitrobenzenesulfonic acid (TNBS) solutions, which was also used to prove the efficacy of S2 for colitis treatment. The specific delivery of hydrocortisone and 5-ASA from S2 material to the colon tissue in injured rats markedly lowers the colon/body weight ratio and the clinical activity score. Histological studies showed a remarkable reduction in inflammation, as well as an intensive regeneration of the affected tissues.
- Teruel, Adrián H.,Pérez-Esteve, édgar,González-álvarez, Isabel,González-álvarez, Marta,Costero, Ana M.,Ferri, Daniel,Gavi?a, Pablo,Merino, Virginia,Martínez-Má?ez, Ramón,Sancenón, Félix
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- Anticancer activity ofwater-soluble olsalazine-pamam-dendrimer-salicylic acid-conjugates
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Improving the activity and selectivity profile of anticancer agents will require designing drug carrier systems that employ soluble macromolecules. Olsalazine-PAMAM-dendrimer-salicylic acid-conjugates with dendritic arms of different lengths have shown good stability regarding the chemical link between drug and spacer. In this study, the drug release was followed in vitro by ultraviolet (UV) studies. Evaluation of the cytotoxicity of the olsalazine-PAMAM-dendrimer-salicylic acid-conjugates employing a sulforhodamine B (SRB) assay in PC-3 (human prostatic adenocarcinoma) and MCF-7 (human mammary adenocarcinoma) cell lines demonstrated that conjugate 9 was more active as an antiproliferative agent than cisplatin, and no cytotoxicity towards the African green monkey kidney fibroblast (COS-7) cell line was observed in any of the conjugates synthesized in the present work.
- Cortez-Maya, Sandra,Pedro-Hernández, Luis Daniel,Martínez-Klimova, Elena,Ramírez-ápan, Teresa,Martínez-García, Marcos
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- Calcium Coordination Solids for pH-Triggered Release of Olsalazine
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Calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H4olz), an anti-inflammatory compound used for treatment of ulcerative colitis. The materials include one-dimensional Ca(H2olz)?4 H2O chains, two-dimensional Ca(H2olz)?2 H2O sheets, and a three-dimensional metal-organic framework Ca(H2olz)?2DMF (DMF=N,N-dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H2olz) phase when exposed to aqueous HCl. The compounds Ca(H2olz)?x H2O (x=0, 2, 4) were each pressed into pellets and exposed to simulated gastrointestinal fluids to mimic the passage of a pill from the acidic stomach to the pH-neutral intestines. All three calcium materials exhibited a delayed release of olsalazine relative to Na2(H2olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.
- Levine, Dana J.,Gonzalez, Miguel I.,Legendre, Christina M.,Run?evski, Tom?e,Oktawiec, Julia,Colwell, Kristen A.,Long, Jeffrey R.
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p. 1739 - 1742
(2017/11/15)
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- Controlled release of 5-Aminosalicylic acid (5-asa) from new biodegradable polyurethanes
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Segmented polyurethanes containing azo aromatic groups in the main chain were synthesized by reaction of 3,3'-azobis(6-hydroxybenzoic acid) (ABHB), 5-[4(hydroxyphenyl)azo] salicylic acid (HPAS), and 5-[1-hydroxynaphthyl)azo] salicylic acid (HNAS) with hex
- Kenawy, El-Refaie,Al-Deyab, Salem,El-Newehy, Mohamed H.
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experimental part
p. 2257 - 2268
(2010/08/04)
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