Marine Polysaccharides in Pharmaceutical Applications
Se-Kwon Kim in Marine Biochemistry, 2023
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).
Aceclofenac
Anton C. de Groot in 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
Pamela E Macintyre, Suellen M Walker, David J Rowbotham in Clinical Pain Management, 2008
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).
Effect of lipid and edge activator concentration on development of aceclofenac-loaded transfersomes gel for transdermal application: in vitro and ex vivo skin permeation
Published in Drug Development and Industrial Pharmacy, 2020
Narendar Dudhipala, Riyaz Phasha Mohammed, Ahmed Adel Ali Youssef, Nagaraj Banala
Aceclofenac (AF) is a weakly acidic and lipophilic drug with pKa 4.7, and belongs to BCS Class II due to its low solubility. AF is frequently prescribed by oral route for the management of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis [23]. Chronic oral AF administration leads to unfavorable adverse effects especially on the gastric mucosa due to prostaglandin inhibition. These side effects can be precipitated as simple infirmities like dyspepsia, moderate problems like peptic ulcers, and severe concerns like gastrointestinal (GI) hemorrhage. AF has the potential to cause local irritation and GI mucosal lesions due to its acidic character [24]. Apart from therapeutic challenge due to side effects, physicochemical challenges of low aqueous solubility, chemical challenge of instability in alkaline, neutral media as well as higher Log p value nominate it to be formulated into TS formulation as a novel transdermal drug delivery system.
A comparative study of aceclofenac versus etoricoxib in the management of acute low back pain in a tertiary care hospital
Published in Journal of Drug Assessment, 2020
Hema Jagannathan, Amulya Thota, Ashok Kumar B. Kumarappa, Githa Kishore
Aceclofenac is a preferential COX-2 inhibitor with anti-inflammatory and analgesic properties. Aceclofenac also targets the synthesis of glycosaminoglycan and mediates chondroprotective effects8. It presents with more gastrointestinal side-effects like dyspepsia, abdominal pain, and nausea9. Etoricoxib is a COX-2 selective inhibitor with anti-inflammatory, analgesic properties and potential antineoplastic properties. It presents with lesser incidence of gastrointestinal side-effects, but increased cardiovascular adverse events10.
Related Knowledge Centers
- Ankylosing Spondylitis
- Diclofenac
- Indometacin
- Osteoarthritis
- Rheumatoid Arthritis
- Porphyria
- NONsteroidal Anti-Inflammatory Drug
- Prescription Drug