Abstract:
:The physical entrapment of a hydrophilic drug within degradable microspheres is generally difficult because of poor entrapment yield and/or fast release, depending on the microsphere fabrication method. In order to counter the effects of drug hydrophilicity, it is proposed to covalently attach the drug to lactic acid oligomers, with the aim of achieving temporary hydrophobization and slower release controlled by the separation of the drug from the degradable link within the polymer matrix. This strategy was tested on microspheres of the antibiotic cephradin. As the prodrug form, the entrapment of the drug was almost quantitative. The prodrug did degrade in an aqueous medium, modelling body fluids, but cleavage did not occur at the drug-oligomer junction and drug molecules bearing two lactyl residual units were released. When the prodrug is entrapped within a PLAGA matrix, no release was observed within the experimental time period. However, data suggest that conjugation via a bond more sensitive to hydrolysis than the main chain PLA ester bonds should make the system work as desired.
journal_name
J Microencapsuljournal_title
Journal of microencapsulationauthors
Ustariz-Peyret C,Coudane J,Vert M,Kaltsatos V,Boisramené Bdoi
10.1080/026520400417667subject
Has Abstractpub_date
2000-09-01 00:00:00pages
615-24issue
5eissn
0265-2048issn
1464-5246journal_volume
17pub_type
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