The development of a long-acting orally administered dosage form is a challenge. Here, we report development of a multi-layered mucoadhesive gastric patch that could deliver entrapped chemotherapeutic agent for eight days after oral administration. The multi-layered patch was designed to contain core layer, mucoadhesive layer and backing layer. The core layer contained the model chemotherapeutic agent, regorafenib. The mucoadhesive layer made of chitosan-hydrocaffeic acid conjugate showed greatest mucoadhesion strength of 18.1 0.78 kPa in freshly excised rat gastric mucosa. The backing layer made of hydrophobic polycaprolactone-polydimethylsiloxane composite showed the contact angle of 120 4.7 after placement of water drop. The entrapped regorafenib predominantly released from the mucoadhesive-side of the patch into simulated gastric fluid and showed a zero-order release profile. The patches were found to be stable for desired characteristics for up to 3 months in long term storage conditions. The pharmacokinetic studies in rat model revealed constant plasma concentration of regorafenib sustained for 8 days after oral administration of gastric patch. The gastric tissue where the patch adhered for 8 days did not show any significant histological changes compared with the normal gastric tissue. The oral administration of single dose of regorafenib-loaded gastric patch in FaDu cell xenografted tumor bearing athymic nude mice has shown significant (P < 0.05) reduction in the tumor volume over 7 days compared to the control group. Taken together, the multi-layered mucoadhesive gastric patch can be developed as a long-acting oral drug delivery system.
Reviewed by: Sony Media Acid 5.0 Music Studio and Acid 5.0 Pro Eric S. Strother Sony Media Acid 5.0 Music Studio and Acid 5.0 Pro Acid 5.0 Music Studio, US$ 69.95; Acid 5.0 Pro, US$ 399.95; available from Sony Media Software, 1617 Sherman Avenue, Madison, Wisconsin 53704, USA; telephone (+1) 800 577-6642 or (+1) 608-256-3133; fax (+1) 608-250-1745; Web www.mediasoftware.sonypictures.com/ products/acidfamily.asp. Acid 5.0 is the latest in the line of the Acid music mixing software, formerly produced by Sonic Foundry, recently taken over by Sony. It is offered in two packages: Music Studio for the casual user, and Pro for those who take their creating and mixing more seriously. For those unfamiliar with Acid, it is a software package for creating and editing music based on sound loops. In a way, this is a return to earlier forms of electronic music where the electronic medium was a way of organizing and manipulating samples of sounds. As someone who was not really familiar with this type of composition, I had a little difficulty getting the hang of it, but it did not take long before I was able to work quickly and freely with the software.
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