In-vitro/In-vivo comparison of leuprolide acetate release from an in-situ forming plga system
Open Access
- 15 July 2013
- journal article
- Published by Springer Science and Business Media LLC in DARU Journal of Pharmaceutical Sciences
- Vol. 21 (1), 57
- https://doi.org/10.1186/2008-2231-21-57
Abstract
A poly (lactide-co-glycolide) (PLGA) implant was used to control the release profile of leuprolide acetate (LA) drug. The system is an in-situ polymeric precipitation system. And the formulation consisted of PLGA polymer, LA drug and N-methyl-2-pyrrolidon solvent with no additives. First, the formulation was injected into PBS solution for in-vitro studies and then it was administered to the animal models (female rats) for in-vivo release studies. The release profiles of leuprolide acetate were measured by UV spectrophotometry for a period of 28 days. The initial burst release of LA was 14% in in-vitro whereas it was 7% in in-vivo. In-vitro and in-vivo release profiles of LA had similar trends after 72 hours. However, the rate of LA release was slower in-vivo. This might be attributed to the limited diffusion process of solvent and the drug molecules. This could be due to presence of an additional pressure caused by the surrounding tissue and also the presence of small amount of water between cells in the subcutaneous site. Cross-section and surface of the implants were studied via scanning electron microscopy. Morphology of both in-vitro and in-vivo implants confirmed the release behaviours. No toxicity effects were reported in the histopathological assay. Furthermore, the pharmacological analysis showed more inactive ovaries due to release of LA.Keywords
This publication has 15 references indexed in Scilit:
- Biocompatibility of an Injectable In Situ Forming Depot for Peptide DeliveryJournal of Pharmaceutical Sciences, 2010
- Effect of additives on release profile of leuprolide acetate in an in situ forming controlled‐release system: In vitro studyJournal of Applied Polymer Science, 2007
- Miscibility of Bioerodible Polyphosphazene/Poly(lactide-co-glycolide) BlendsBiomacromolecules, 2007
- Stability of poly(d,l-lactide-co-glycolide) and leuprolide acetate in in-situ forming drug delivery systemsJournal of Controlled Release, 2006
- Modification of the tri-phasic drug release pattern of leuprolide acetate-loaded poly(lactide-co-glycolide) microparticlesEuropean Journal of Pharmaceutics and Biopharmaceutics, 2006
- The effect of additives on naltrexone hydrochloride release and solvent removal rate from an injectablein situ forming PLGA implantPolymers for Advanced Technologies, 2006
- Influence of the poly(lactide-co-glycolide) type on the leuprolide release from in situ forming microparticle systemsJournal of Controlled Release, 2006
- Solubilizing Excipients in Oral and Injectable FormulationsPharmaceutical Research, 2004
- Myotoxicity studies of injectable biodegradable in-situ forming drug delivery systemsInternational Journal of Pharmaceutics, 2001
- Persistent Suppression of the Pituitary-Gonadal System in Female Rats by Three-Month Depot Injectable Microspheres of Leuprorelin AcetateJournal of Pharmaceutical Sciences, 1996