Biodegradation and biocompatibility of contraceptive-steroid-loaded poly (DL-lactide-co-glycolide) injectable microspheres: in vitro and in vivo study |
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Authors: | Dhanaraju Magharla Dasaratha Rajkannan Rajagopalan Selvaraj Devarajan Jayakumar Rajadas Vamsadhara Chandrasekar |
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Affiliation: | Department of Pharmaceutics, GIET School of Pharmacy, NH-5, Rajahmundry 533 294, India. mddhanaraju@yahoo.com |
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Abstract: | PURPOSE: A controlled-release drug delivery of contraceptive steroids levonorgestrel (LNG) and ethinyl estradiol (EE) has been developed by successful encapsulation of LNG and EE in poly (lactide-co-glycolide) (PLG) microspheres. MATERIALS AND METHODS: Smooth, spherical, steroid-loaded PLG microspheres with a mean size of 10-25 microm were prepared by using the water/oil/water double-emulsion solvent evaporation method. RESULTS: In vitro release profiles showed an increased burst release of LNG/EE on Week 1; thereafter, the release was sustained. At the end of Week 7, the release of LNG/EE from 1:5 and 1:10 PLG microspheres was 75.64% and 62.55%. respectively. In vitro degradation studies showed that the PLG microspheres maintained surface integrity up to Week 8 and then eroded completely by Week 20. In an in vivo study, the serum concentration of LNG/EE in rats showed a triphasic release response, with an initial burst release of 8 ng/mL LNG and 14 pg/mL EE on Day 1; thereafter, a controlled release of the drugs to the systemic circulation was maintained until Week 15, maintaining constant drug levels of 2 ng/mL LNG and 3-4 pg/mL EE in the blood. Histological examination of steroid-loaded PLG microspheres injected intramuscularly into the thigh muscle of Wistar rats showed minimal inflammatory reaction, demonstrating that contraceptive-steroid-loaded microspheres were biocompatible. CONCLUSION: This controlled-release and biocompatible nature of the PLG microspheres may have potential application in contraceptive therapy. |
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Keywords: | Poly (lactide-co-glycolide) (PLG) microspheres Levonorgestrel (LNG) Ethinyl estradiol (EE) Biocompatibility Biodegradability Controlled drug delivery |
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