title: Optimisation of microstructured biodegradable finasteride formulation for depot parenteral application.
abstract: This study aimed to use the biocompatibility features of the biodegradable polymers to prepare depot injectable finasteride (FIN) microspheres for the treatment of benign prostatic hyperplasia. FIN microspheres were prepared utilising an emulsion-solvent evaporation/extraction technique. The Box-Behnken experimental design was adopted to optimise the preparation process. FIN plasma levels in albino rabbits were determined after injection with optimised FIN microspheres formula and compared with oral FIN suspension. Results revealed that the optimum microspheres displayed an amended sustained release pattern with lower initial burst. The cumulative FIN % released after 25 days was in the range 27.83-73.18% for F4 and F1, respectively. The optimised formula, with 50.0% (X1), and 22.316% (X2) and 1.38% (X3) showed 6.503 μm, 93.213%, 14.574%, and 64.838% for Y1, Y2, Y3, and Y4, respectively. In vivo studies displayed a sustained release pattern with minimal initial burst release when injected into rabbits.
authors.affiliation: a Department of Pharmaceutics & Industrial Pharmacy, Faculty of Pharmacy , King Abdulaziz University , Jeddah , Saudi Arabia ;|c Department of Pharmaceutics & Industrial Pharmacy, Faculty of Pharmacy , Minia University , Minia , Egypt.
authors.forename: Osama A
authors.initials: OA
authors.lastname: Ahmed
authors.affiliation: c Department of Pharmaceutics & Industrial Pharmacy, Faculty of Pharmacy , Minia University , Minia , Egypt.
authors.forename: Amal K
authors.initials: AK
authors.lastname: Hussein
authors.affiliation: b Department of Pharmaceutics & Pharmaceutical Technology, Faculty of Pharmacy , Taibah University , Medina , Saudi Arabia ;|c Department of Pharmaceutics & Industrial Pharmacy, Faculty of Pharmacy , Minia University , Minia , Egypt.
authors.forename: Fatma M
authors.initials: FM
authors.lastname: Mady
mesh_terms: D000818:Animals; D001672:Biocompatible Materials / Q000737:chemistry; D002208:Caproates / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D018120:Finasteride / Q000008:administration & dosage* / Q000097:blood*; D006801:Humans; D007267:Injections; D019344:Lactic Acid / Q000737:chemistry; D007783:Lactones / Q000737:chemistry; D008297:Male; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011470:Prostatic Hyperplasia / Q000188:drug therapy; D011817:Rabbits; D064804:Urological Agents / Q000008:administration & dosage* / Q000097:blood*
chemical_list: D001672:Biocompatible Materials; D002208:Caproates; D003692:Delayed-Action Preparations; D007783:Lactones; D064804:Urological Agents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C121056:caprolactone; D018120:Finasteride
keywords: Box–Behnken design; biodegradable; depot parenteral preparation; finasteride; microencapsulation