Abstract
The aim of the present work was to study the in vitro/in vivo characteristics of dutasteride loaded biodegradable microspheres designed for sustained release of dutasteride over four weeks. An O/W emulsion-solvent evaporation method was used to incorporate dutasteride, which is of interest in the treatment of benign prostatic hyperplasia (BPH), into poly(lactide-co-glycolide) (PLGA). A response surface method (RSM) with central composite design (CCD) was employed to optimize the formulation variables. A prolonged in vitro drug release profile was observed, with a complete release of the entrapped drug within 28 days. The pharmacokinetics study showed sustained plasma drug concentration-time profile of dutasteride loaded microspheres after subcutaneous injection into rats. The in vitro drug release in rats correlated well with the in vivo pharmacokinetics profile. The pharmacodynamics evaluated by determination of the BPH inhibition in the rat models also showed a prolonged pharmacological response. These results suggest the potential use of dutasteride loaded biodegradable microspheres for the management of BPH over long periods.
Highlights
Benign prostatic hyperplasia (BPH) is age related proliferative diseases, which is extremely common medical condition in aged men 50 years or older [1, 2]
For the central composite design (CCD), a total 20 trial formulations were proposed by Design-Expert software for three factors, PVA concentration (X1), PLGA content (X2) and theoretical content (X3), which were varied at five different levels
Dutasteride-loaded PLGA microspheres were successfully prepared by an O/W emulsion solvent evaporation method
Summary
Benign prostatic hyperplasia (BPH) is age related proliferative diseases, which is extremely common medical condition in aged men 50 years or older [1, 2]. Controlled Release of Dutasteride Microspheres lead to severe lower urinary tract symptoms, such as decreased maximum urinary flow rate, urinary frequency and urgency [3]. According to the report of Roehrborn et al, patients with long-term (4-year) treatment of dutasteride were proved to have continuing improvements in symptoms and peak urinary flow [5]. Dutasteride is available in the market as soft gelatin capsule (0.5 mg), and daily oral administration is required. A sustained release dosage form for long periods of time avoids daily administration, and is the best way to improve patient compliance and secure the therapeutic efficiency
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