Controlled-release nanoencapsulating microcapsules to combat inflammatory diseases

Abstract

The World Health Organization (WHO) has reported that globally 235 million people suffer from chronic and other inflammatory diseases. The short half-lives of nonsteroidal anti-inflammatory drugs (NSAIDs) and their notoriety in causing gastrointestinal discomforts, warrants these drugs to be released in a controlled and sustained manner. Although polymeric particles have been widely used for drug delivery, there are few reports that showcase their ability in encapsulating and sustaining the release of NSAIDs. In this paper, polymeric nanoencapsulating microcapsules loaded with NSAIDs were fabricated using solid/water/oil/water emulsion solvent evaporation method. Two NSAIDs, ibuprofen and naproxen, were first pre-loaded into nanoparticles and then encapsulated into a larger hollow microcapsule that contained the third NSAID, celecoxib. A high encapsulation efficiency (%) of these NSAIDs was achieved and a sustained release (up to 30 days) of these drugs in phosphate-buffered saline was observed. Then, a gastrointestinal drug – cimetidine (CIM) – was co-loaded with the NSAIDs. This floating delivery system exhibited excellent buoyancy (~88% up to 24 h) in simulated gastric fluid. It also allowed a sequential release of the drugs, whereby an immediate release of CIM followed by NSAIDs was observed. Drug release of the NSAIDs observed Fickian diffusion mechanism, whereas CIM observed non-Fickian diffusion. Therefore, this delivery system is a promising platform to control the delivery of NSAIDs to combat inflammatory diseases, thereby protecting against possible gastrointestinal side effects that may arise from the overuse of NSAIDs.

Development, Optimization and In Vitro/In Vivo Characterization of Collagen-Dextran Spongious Wound Dressings Loaded with Flufenamic Acid

“…Among the large group of classical NSAIDs, flufenamic acid (FFA) was selected as the model compound in this research. FFA is an anthranilic acid derivative that inhibits both forms of cyclooxygenase izoenzymes, and is accountable for prostaglandin biosynthesis [ 17 , 18 , 19 , 20 ]. FFA demonstrated its anti-inflammatory and analgesic potential in various topical marketed formulations intended for use in different rheumatic disorders and soft tissue injuries [ 21 , 22 ].…”

Biodegradable Nanoparticles-Loaded PLGA Microcapsule for the Enhanced Encapsulation Efficiency and Controlled Release of Hydrophilic Drug

“…Regardless of the materials of NPs, all the NPs were localized near the capsule shell. This is further supported by the studies done, where the drug-loaded particles were successfully encapsulated in a hollow microcapsule [ 18 ].…”

“…As for PLGA MCs, first-order equation exhibited the highest R2 values among the three equations, indicating the release mechanism depending on the drug concentration. On the other hand, the values of the PLGA MCs exhibited higher than that of PLGA MPs, indicating the mechanism of release profile was controlled-diffusion [ 18 ]. Both PLGA MCs would release the MET by the diffusion from alginate and chitosan matrix, while the drug was directly released from the outer rim of the PLGA MPs.…”

Design of multicomponent indomethacin‐paracetamol and famotidine loaded nanoparticles for sustained and effective anti‐inflammatory therapy

“…On this point, combination therapy through combining multiple treatments with various mechanisms is a highly effective strategy in the treatment of various diseases like cancer, inflammatory diseases, HIV, and others (Baek et al, 2017; Baek & Cho, 2015; Coradini et al, 2015; Freeling et al, 2014). To achieve this approach, different drug delivery systems based on suitable nanomaterials and capable of behaving combinations of various therapies have been successfully explored (Gadde, 2015).…”