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Dental Disease, Inflammation, Cardiovascular Disease, Nutrition and Nutritional Supplements
Published in Stephen T. Sinatra, Mark C. Houston, Nutritional and Integrative Strategies in Cardiovascular Medicine, 2022
Douglas G. Thompson, Gregori M. Kurtzman, Chelsea Q. Watkins
Although doxycycline has been used as an antibacterial agent, its use in lower doses has proven to help modulate the activities of some host-derived matrix metalloproteinases responsible for tissue breakdown.107,108 Additionally, it has an inhibitory effect on collagenase. During the inflammatory responses observed in periodontal and cardiovascular diseases, proinflammatory mediators are up-regulated not only in affected tissues, but also in the secreted, disease-affected oral fluids (saliva) as well as in serum and plasma. Therefore, inhibiting collagenase activity not only has a benefit orally with those hard and soft tissues, but also cadiovascularly.109 Studies show the use of a sub-antimicrobial dose of doxycycline 20 mg (Periostat® (doxycycline hyclate)) prescribed BID daily as an adjunct following scaling and root planing (SRP) provided significantly greater clinical benefits than SRP alone in the treatment of moderate to severe periodontal disease.110,111 It can be prescribed for up to 9 months followed by a 3-month drug holiday and then repeated. Usage beyond 9 months has not been well reported, so continued benefits may be present, but further studies are needed to confirm.
Safety Pharmacology and the GI Tract
Published in Shayne C. Gad, Toxicology of the Gastrointestinal Tract, 2018
The only model useful for specific evaluation of potential damage to small intestinal and colonic mucosa was published by Fara [28]. He used an in situ rabbit colon or intestine model as a sensitive and reproducible test to evaluate the topical effect of up to three substances applied to the colonic mucosa, and found that doxycycline hyclate tablets and propranolol hydrochloride tablets produced macroscopic and histologic damage. Potassium released from Slow-K and Micro-K Extencaps caused more irritation than from controlled-release KCl. This model may be useful in evaluating sustained or enteric coated formulation for potential lesion-producing activity and may be the only suitable way of evaluating potential problems with formulated products, which are too large to be dosed to most laboratory animals. The fed rat can also be used to evaluate the diarrheogenic potential by observing fecal pellet.
Doxycycline
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Doxycycline (alpha-6-deoxytetracycline) has the empirical formulas C22H24N2O8·HCl and ½ [C2H5OH·H2O] and molecular weight 512.9. Doxycycline is a second-generation tetracycline with increased oral bioavailability and tissue penetration as a result of its improved lipophilicity compared with earlier tetracyclines. Its mechanism of action is inhibition of microbial protein synthesis through interaction with 30S ribosomal subunits. It is almost universally administered orally and has a prolonged serum half-life. It is available as both doxycycline monohydrate and doxycycline hyclate. Tradenames include Vibramycin, Doryx, Doxy-100, Doxsig, Zadorin, Doxylag, Periostat, and Doxycin (Figure 68.1).
177Lu-doxycycline as potential radiopharmaceutical: electrochemical characterization, radiolabeling, and biodistribution in tumor-bearing mice
Published in International Journal of Radiation Biology, 2021
Zorana Milanović, Drina Janković, Sanja Vranješ-Đurić, Magdalena Radović, Željko Prijović, Gordana Zavišić, Marko Perić, Dalibor Stanković, Marija Mirković
A series of experiments were performed to define the optimal 177Lu-labeling conditions for the doxycycline ligand based on our previous experience (Aleksandar et al. 2020; Mirković et al. 2020). The labeling yield was determined by ascending paper and ITLC methods. The ITLC method with ammonia/methanol/water = 1:20:10 as the mobile phase, indicated that 177Lu-doxycycline complex migrated to the front of the SG plates (Rf = 0.9–1.0), while the free 177Lu stayed at the origin. The ascending paper chromatography on Whatman 3MM strips and saline as a mobile phase has not been shown as an appropriate method for determining radiochemical purity. Under optimized conditions, by radiolabeling of 10 mg of doxycycline hyclate with 177Lu (37 MBq) in a final volume of 1.0 ml (0.9% NaCl) at pH 6–7 and incubation at room temperature for 60 min, the radiochemical purity of 177Lu-doxycycline complex was 99%. When the labeling of the ligand with 177Lu was carried out at a higher temperature (60 °C) for a different time, it was observed that temperature and increased incubation time did not significantly affect the radiolabeling yield. The labeling of doxycycline was observed by the determination of one peak at the origin for 177LuCl3 (Figure 1(A)) and one at the solvent front for 177Lu-doxycycline (Figure 1(B)) on TLC chromatograms. Further radiolabeling verification was done by HPLC. It was noticed that the retention time of 177LuCl3 was 1.81 min and of 177Lu-doxycycline was 3.39 min (Figure 1(C)).
Development of rGO encapsulated polymeric beads as drug delivery system for improved loading and controlled release of doxycycline drug
Published in Drug Development and Industrial Pharmacy, 2020
Geetanjali Singh, Bhavani P. Nenavathu
Doxycycline hyclate was purchased from Sisco Research Laboratories Pvt. Ltd., India. Sulfuric acid and HCl were purchased from Fine Chemicals Ltd., India. Sodium nitrate was purchased from Central Drug House Pvt. Ltd., Delhi, India. Graphite fine powder was purchased from Titan Biotech Ltd., India. Potassium permanganate was purchased from RFCL Ltd., India. Hydroperoxide and distilled water were purchased from Merck Life Science Pvt. Ltd., India. ZnCl2 was purchased from Thermo Fisher Scientific Pvt. Ltd., India. Sodium ALG was obtained from Loba Chemie Pvt. Ltd., India. CS was obtained from SEZ Enterprise, India. Acetic acid was procured from Ranbaxy Fine Chemicals Ltd., India. All the chemicals and solvents were used without further purification.
Design, optimization and characterizations of chitosan fortified calcium alginate microspheres for the controlled delivery of dual drugs
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Sarita Kumari Yadav, Gayasuddin Khan, Gunjan Vasant Bonde, Monika Bansal, Brahmeshwar Mishra
Consequently, in the following study, antimicrobial drugs encapsulated CS-Ca-SA microspheres were formulated for controlled release therapy. The combination of antibiotics has been more effective for the treatment of microbial infections of oral cavity [26]. Ornidazole (OZ) is a nitroimidazole antiprotozoal drug that also has potent antibacterial activity against 94% of oral anaerobic bacteria and Bacteroides and Clostridium species [27]. Doxycycline hyclate (DX) is an FDA-approved, potent broad-spectrum tetracycline antibiotic active against oral aerobic microorganisms [28]. Thus, OZ and DX combination has been proposed to eradicate broad range of microbes (both aerobic and anaerobic) living in the periodontal cavity.