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Marine Polysaccharides in Pharmaceutical Applications
Published in Se-Kwon Kim, Marine Biochemistry, 2023
Riyasree Paul, Sourav Kabiraj, Sreejan Manna, Sougata Jana
Mahdavinia et al. have developed κ-CG- and chitosan-based beads for oral delivery of diclofenac sodium. Incorporation of iron oxide magnetic NPs resulted in a decreased swelling ability. At pH 7.4, the maximum diclofenac sodium release was reported around 82% (Mahdavinia et al. 2015). Chitosan and chondroitin sulfate were employed to develop NPs for transdermal application of ketoprofen. The synthesized NPs were incorporated in an emulgel of argan oil. Sustained release of ketoprofen was observed up to 72 hours. A skin permeation study indicated higher permeation of ketoprofen than the marketed gel (Gul et al. 2018). Aceclofenac-loaded IPN nanocarriers were developed using glutaraldehyde cross-linked chitosan and locust bean gum. An increase in locust bean gum percentage decreased the drug entrapment. An in vitro study demonstrated restricted release of aceclofenac in acidic pH (Jana and Sen 2017). Jana et al. investigated the efficacy of chitosan-albumin based NPs for transdermal delivery of aceclofenac. The synthesized NPs were further incorporated into carbopol gel for easy topical application. The drug release study indicated sustained release pattern over 8 hours. A negative zeta potential of -22.10 mV was reported. The ex vivo skin permeation exhibited sustained penetration of aceclofenac through mice skin. Thein vivo study performed in carrageenan injected rats demonstrated higher swelling inhibition of rat paw compared to the marketed gel preparation (Jana et al. 2014).
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Ketoprofen is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic effects. Ketoprofen inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis, by prostaglandin synthase, is responsible for the therapeutic effects of this NSAID. Ketoprofen is indicated for symptomatic treatment of acute and chronic rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, primary dysmenorrhea and mild to moderate pain associated with musculotendinous trauma (sprains and strains), postoperative (including dental surgery) or postpartum pain. It is also, and far more frequently, used in topical formulations (gel, cream, foam, ointment, tape) for musculoskeletal diseases and injuries for its analgesic and anti- inflammatory effects (1).
Drugs Affecting the Musculoskeletal System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It is better to be avoided during the 1st and 3rd Trimesters because the pregnancy experience in humans suggests a risk of pulmonary hypertension of the newborn, SABs, and congenital malformations linked to the use of Ketoprofen. Furthermore, Ketoprofen has been found to inhibit labor and to prolong the length of pregnancy.
Effect of chronic spinal cord injury’s severity on sperm parameters in rat: correlation with locomotion deficits
Published in International Journal of Neuroscience, 2021
Ezidin G. Kaddumi, Dalal A. Shuqair, Samya A. Omoush, Wesam Abdel-Razaq, Hakam H. Alkhateeb
Animals in the SCI and the sham groups were anesthetized with an intraperitoneal injection of a mixture of ketamine (80 mg/kg) and xylazine (10 mg/kg). Then, the T8 spinal segment was exposed by a laminectomy for the overlying T7 vertebra, which had accessed through a dorsal longitudinal incision. SCIs were performed using a needle (for the 1/3 and 2/3 SCI groups) or by micro-scissor (for Tx group). The incision was then sutured. All surgical procedures were done under aseptic conditions and visualized under a surgical microscope. In order to avoid any possible infection, gentamicin (5 mg/kg) was administered prior to the surgery and was given once a day for the following five days. Ketoprofen (2.5 mg/kg) were also administered for two days following the surgery in order to alleviate any post-surgical pain. The given drugs were administered for all SCI groups and the sham group, as well, in order to exclude any possible effect of these drugs on the results. Animals were individually housed to recover for 4 weeks before being sacrificed for the final experiment. During the recovery period a behavioral record indicating all necessary bowel and bladder management were kept for each animal.
Experimental design, development and evaluation of extended release subcutaneous thermo-responsive in situ gels for small molecules in drug discovery
Published in Pharmaceutical Development and Technology, 2021
Divya Sharma, Faraj Atassi, Steve Cook, Stacey Marden, Jianyan Wang, Aixiang Xue, David J. Wagner, Guangnong Zhang, Wenzhan Yang
The in vivo plasma concentration profiles were compared between the two thermogel formulations after subcutaneous administration, and with the intravenous (IV) administration of drug in solution (Figure 8). As shown in Figure 8, no obvious absorption phase was observed from either thermogel after subcutaneous dosing and the plasma drug levels reached 50–70 µM within the first 1 h sampling time point and declined over the time course of the experiment, indicating that the drug release and absorption in vivo was rapid which differs from the extended release observed in vitro. Moreover, no apparent differences in plasma pharmacokinetic parameters of ketoprofen were observed between the two formulations (Table 6). Also, the terminal half-life values and the overall profiles observed in this study are similar to our own and previously reported measurements with intravenous or intraperitoneal administration (Foster and Jamali 1988), suggesting that, for ketoprofen, the in vivo release from either thermogel formulation was not rate limiting relative to absorption from the subcutaneous injection site. The longer terminal half-life is within the range observed by others when dosing ketoprofen IV at 10 mg·kg−1; however, all concentrations at 192 h from our 1 mg·kg−1 IV dose were below the limit of quantification (Foster and Jamali 1988). It is likely that the longer apparent terminal half-life would become observable at a higher IV dose level.
Topical nonsteroidal anti-inflammatory drugs in the treatment of knee osteoarthritis: a systematic review and meta-analysis
Published in The Physician and Sportsmedicine, 2021
Dylan G. Wolff, Christy Christophersen, Symone M. Brown, Mary K Mulcahey
Ketoprofen was shown to be non-inferior to both topical diclofenac and oral celecoxib, but studies using a transferosome carrier [TDT] showed that this carrier alone was non-inferior to the preparation including ketoprofen [27,28]. A recent meta-analysis reported that 85% (95% CI 77%, 93%) of the effectiveness of topical NSAIDS for OA can be attributed to placebo effect, which could provide an explanation for the strong response to the placebo arm in some studies [37]. Given this suggestion of a strong placebo effect, future studies could incorporate objective measures such as radiography or measurement of inflammatory markers to further investigate the effect of topical NSAIDs on the disease progress. Additionally, ketoprofen is available as a topical gel but not in the United States, which limits options for these clinicians in choosing which topical NSAID to prescribe. The studies evaluating ibuprofen demonstrated small sample sizes (n = 25, 30, 50) and large confidence intervals for effect size prevent a strong conclusion regarding comparative efficacy.