Abstract:
:Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs in the world, primarily for symptoms associated with osteoarthritis and other chronic musculoskeletal conditions. However, adverse effects caused by oral administration, such as local or systemic disturbance in the gastrointestinal tract, have limited the clinical applications of these drugs. In the present study we have assessed the ability of polyamidoamine (PAMAM) dendrimers to facilitate transdermal delivery of NSAIDs, using Ketoprofen and Diflunisal as model drugs. In vitro permeation studies with excised rat skins indicated that PAMAM dendrimers significantly enhanced the accumulative permeated amount of both drugs after 24 h, as compared to drug suspensions without PAMAM dendrimers. Similarly, anti-nociceptive studies using the acetic acid-induced writhing model in mice showed a prolonged pharmacodynamic profile for the NSAIDs-PAMAM dendrimer complex after transdermal administration. In addition, blood drug level studies revealed that the bioavailability was 2.73 times higher for the Ketoprofen-PAMAM dendrimer complex and 2.48 times higher for the Diflunisal-PAMAM dendrimer complex, respectively, than the pure drug suspensions. These results demonstrated that PAMAM dendrimers can effectively facilitate skin penetration of NSAIDs and may have the potential applications for the development of new transdermal formulations.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Cheng Y,Man N,Xu T,Fu R,Wang X,Wang X,Wen Ldoi
10.1002/jps.20745subject
Has Abstractpub_date
2007-03-01 00:00:00pages
595-602issue
3eissn
0022-3549issn
1520-6017pii
S0022-3549(16)32209-2journal_volume
96pub_type
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