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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
Chawla et al. have investigated the efficacy of alginate-based mucoadhesive microbeads for delivering naproxen sodium. Emulsification method was employed to synthesize calcium chloride cross-linked alginate microbeads. Eudragit S-100 was used to coat the developed microbeads. The core microbeads showed an enhanced mucoadhesive property in respect to coated microbeads. The uncoated microspheres exhibited pH-dependent sustained drug release following Higuchi kinetics, where s the coated microspheres demonstrated Korsmeyer-Peppas kinetics (Chawla et al. 2012). Alginate-gellan gum based microspheres were synthesized for oral delivery of aceclofenac by Jana et al. The average size of the microparticles was reported between 270 and 490 μm. An in vitro drug release study revealed a sustained release of aceclofenac over 6 hours following Korsemeyer-Peppas kinetics. An in vivo study performed on a rabbit model revealed sustained absorption of drug with an excellent anti-inflammatory effect (Jana et al. 2013). Another study conducted by Jana et al. reported the development of alginate and locust bean gum based interpenetrating polymeric network (IPN) microspheres for oral delivery of aceclofenac. The ionic gelation technique was employed to develop calcium ion cross-linked microspheres. An in vitro study revealed sustained release of aceclofenac over 8 hours in pH 6.8 phosphate buffer. An increased polymer concentration has decreased the aceclofenac release percentage, as shown in Figure 5.3. Pharmacodynamic analysis exhibited a sustained anti-inflammatory effect after oral administration (Jana et al. 2015).
Aceclofenac
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Aceclofenac, the carboxymethyl ester of diclofenac, is a nonsteroidal anti-inflammatory drug (NSAID) with marked anti-inflammatory and analgesic properties. It is orally administered for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. Aceclofenac is also reported to be effective in other painful conditions such as dental and gynecological conditions (1). Aceclofenac is also widely used in topical form for acute soft trauma and inflammatory or degenerative musculoskeletal disorders (3). Aceclofenac is metabolized into diclofenac after systemic administration; possibly, hydrolysis also occurs in the skin (4).
Clinical pharmacology: traditional NSAIDs and selective COX-2 inhibitors
Published in Pamela E Macintyre, Suellen M Walker, David J Rowbotham, Clinical Pain Management, 2008
Stephen F Jones, Aidan M O’Donnell
Aceclofenac is an ester of diclofenac with fewer gastrointestinal side effects. It has no intrinsic inhibitory effect on COX-1 or COX-2, and its mechanism of analgesic effect probably relies on its biotransformation into diclofenac.106
A drift on liposomes to proliposomes: recent advances and promising approaches
Published in Journal of Liposome Research, 2022
Neha Dhiman, Jayrajsinh Sarvaiya, Poorti Mohindroo
Gupta et al. developed PLs of Aceclofenac for transdermal drug delivery. The permeation (through Franz diffusion cell) under the occlusive condition on Wistar rat’s skin was studied by direct spread on the skin followed by dressing. Aceclofenac is under the category of non-steroidal anti-inflammatory drugs (NSAIDs); however oral administration of drugs represented side effects, such as gastrointestinal ulcers, anemia, etc. Hence an alternative topical route offers the advantage of safer, continuous, and controlled drug absorption. Proliposomes of Aceclofenac were prepared by film deposition of drug and lecithin taken in methanol-chloroform solution onto microporous mannitol followed by subsequent vacuum drying. The results reported that % EE started increasing by increasing the lecithin content in formulation from a ratio 5 to 20 times than the drug content. In addition in vitro, drug release studies in PBS revealed the sustained release of drugs for a longer period (Heyneman et al.2000, Gupta et al.2008).
An update of cyclooxygenase (COX)-inhibitors in epilepsy disorders
Published in Expert Opinion on Investigational Drugs, 2019
In a rat model of penicillin-induced seizures, Taskiran and colleagues have demonstrated the proconvulsant effect of aceclofenac (an analog of diclofenac with nonselective COX-inhibitor property) at doses of 10 and 20 mg/kg, IP [66]. The authors reported that the epileptiform activity in this animal model reached constant levels after 30 min of penicillin administration [66]. Aceclofenac at 10 and 20 mg/kg was administered 30 min after the penicillin challenge. The effect of these inhibitors is not studied when administered at early time-points in this animal model. Additionally, there is no positive reference control group to compare the effect of COX-inhibitors in this study [66]. It is not known whether, in any means, the pretreatment of aceclofenac is protective in this seizure model and this might be worth investigation.
Comparative safety review of current treatment options for chronic low back pain and unmet needs: a narrative review
Published in Expert Opinion on Drug Safety, 2021
Filip Jovanovic, Iulia Pirvulescu, Emilija Knezevic, Kenneth D. Candido, Nebojsa Nick Knezevic
NSAIDs are well known for their gastrointestinal AEs and, even though selective COX inhibitors are expected to have safer profile, studies show that aceclofenac caused heartburn in more than 20% of patients if controlled-release form was used. Etoricoxib alone led to TRAEs in 26% of patients taking 60 mg and 25% of patients taking 90 mg. Furthermore, when etoricoxib was compared with nonselective NSAID diclofenac, it showed similar percentage of gastrointestinal -related AEs (13–20%). However, when rofecoxib was compared with placebo, there was no difference in gastrointestinal as well as other AEs (headache and upper respiratory infections).