Abstract
The objective of this investigation was to develop a bleomycin depot based on monolithic microparticulate technology to suppress tumour growth and to maintain constant plasma drag concentrations within an optimal therapeutic window over a prolonged period of time. Formulations were optimized with biodegradable poly-ε-carpolactone and evaluated in vitro for physicochemical characteristics, drug release in phosphate buffered saline (pH 7.4) and evaluated in vivo in tumour beating mice. This investigation revealed that upon subcutaneous injection, the biodegradable depot-forming poly-ε-carpolactone microspheres controlled drag release and suppressed tumour growth kinetics significantly compared to control. A preliminary pharmacokinetic evaluation exhibited steady plasma drag concentrations during the study period. This formulation with its reduced frequency of administration and better control of drag disposition is expected to provide an economic benefit to the user compared with products currently available for chemotherapy.
| Original language | English |
|---|---|
| Pages (from-to) | 256-260 |
| Number of pages | 5 |
| Journal | Pharmazie |
| Volume | 57 |
| Issue number | 4 |
| Publication status | Published - 2002 |
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry
- Chemistry(all)
- Molecular Medicine
- Pharmacology
- Pharmaceutical Science