Biphasic Drug Release from Rolled-Up Gelatin Capsules with a Cylindrical Cavity

Abstract

Biphasic drug delivery systems are used for quick release of a specific amount of drug for immediate amelioration of a patient’s state, followed by sustained release, to avoid repeated administration. This type of delivery is often necessary for pain management and the treatment of many pathologies, such as migraines, hypertension, and insomnia. In this work, we propose a novel architecture of a biphasic release media that does not need the rapidly disintegrating layer and that allows for easily setting the sustained release rate. A drug-containing capsule is made by rolling up a thermally crosslinked gelatin strip on which drug reservoirs are formed by casting. The quick-release reservoir (QRR) is placed at the strip’s extremity, from which the rolling starts, while the sustained-release reservoir (SRR) is formed in the middle part of the strip. The strip is rolled around a cylinder that is a few millimeters wide, which is removed after rolling. The roll is stabilized by transglutaminase-catalyzed crosslinking of the consecutive shells. A biphasic release is successfully demonstrated with the use of model fluorescent drugs for single-dye and double-dye systems in phosphate-buffered saline (PBS) solution with pH = 7.4. In vitro, the drug from the QRR, placed at the walls of the cavity of the roll, is released immediately upon the capsule’s contact with the PBS solution. The drug from the SRR, embedded between the roll’s layers, diffuses steadily, with the lag time defined by the radial position of the reservoir.

A combination of chitosan nanoparticles loaded with celecoxib and kartogenin has anti-inflammatory and chondroprotective effects: Results from an in vitro model of osteoarthritis

“…The results were in line with other reports [ 37 , 38 ]. A PDI below 0.5 indicates that NPs have a monodisperse distribution [ [37] , [38] , [39] ].…”

“…The initial burst release is probably caused by the release of drugs that were weakly attached to the surface of CNPs. The rapid release of a significant amount of celecoxib from CNPs can enable the drug to rapidly reach curative levels to manage pain and suppress the symptoms of inflammatory diseases such as OA [ 39 ]. In general, around 34% of celecoxib loaded in CNPs was released in the first hour, and then it provided a continuous release of celecoxib for up to 48 h. The slow release may be due to drug diffusion from the CNPs matrix.…”

Formulation and characterization of floating biphasic tablet consisting of cefdinir nanosuspension

“…The instrument was run until dry powder was achieved, after which the frozen flasks were connected to the device's vacuum port, followed by four flasks each containing 100 ml of nanosuspension. It took (48 to 72) hr to sublimate a solvent from frozen materials (21).…”

Untitled

“…Moreover, the drug release profile can be efficaciously altered by enhancing the drug's amount 14 . The fabricated <100nm gelatin NPs have splendid potential in drug shipping and possess the benefits of any gelatin-based scientific device while overcoming the weaknesses of standard gelatin NPs 15,16 .…”