title: Microencapsulation of alpha-mangostin into PLGA microspheres and optimization using response surface methodology intended for pulmonary delivery.
abstract: Documented to exhibit cytotoxicity and poor oral bioavailability, alpha-mangostin was encapsulated into PLGA microspheres with optimization of formulation using response surface methodology. Mixed levels of four factors Face central composite design was employed to evaluate critical formulation variables. With 30 runs, optimized formula was 1% w/v polyvinyl alcohol, 1:10 ratio of oil to aqueous and sonicated at 2 and 5 min time for primary and secondary emulsion, respectively. Optimized responses for encapsulation efficiency, particle size and polydispersity index were found to be 39.12 ± 0.01%, 2.06 ± 0.017 µm and 0.95 ± 0.009, respectively, which matched values predicted by mathematical models. About 44.4% of the encapsulated alpha-mangostin was released over 4 weeks. Thermal analysis of the microspheres showed physical conversion of alpha-mangostin from crystallinity to amorphous with encapsulated one had lower in vitro cytotoxicity than free alpha-mangostin. Aerodynamic diameter (784.3 ± 7.5 nm) of this alpha-mangostin microsphere suggests suitability for peripheral pulmonary delivery.
authors: Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia , Kuantan, Pahang , Malaysia.
authors: Aimen Abdo
authors: AA
authors: Elsaid Ali
authors: Muhammad
authors: M
authors: Taher
authors: Farahidah
authors: F
authors: Mohamed
mesh_terms: D000280:Administration, Inhalation; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008175:Lung Neoplasms / Q000188:drug therapy; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology; D044004:Xanthones / Q000008:administration & dosage* / Q000494:pharmacology
chemical_list: D004337:Drug Carriers; D047428:Protein Kinase Inhibitors; D044004:Xanthones; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C021053:mangostin