title: Preparation of High-Payload, Prolonged-Release Biodegradable Poly(lactic-co-glycolic acid)-Based Tacrolimus Microspheres Using the Single-Jet Electrospray Method.
abstract: Tacrolimus-loaded poly(lactic-co-glycolic acid) microspheres (TAC-PLGA-M) can be administered for the long-term survival of transplanted organs due to their immunosuppressive activity. The purpose of our study was to optimize the parameters of the electrospray method, and to prepare TAC-PLGA-M with a high payload and desirable release properties. TAC-PLGA-M were prepared using the electrospray method. In vitro characterization and evaluation were performed using scanning electron microscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy. Drug-loading efficiency was greater than 80% in all formulations with a maximum loading capacity of 16.81±0.37%. XRD and DSC studies suggested that the drug was incorporated in an amorphous state or was molecularly dispersed in the microspheres. The in vitro release study showed prolonged release patterns. TAC-PLGA-M with enhanced drug loading and prolonged-release patterns were successfully prepared using the electrospray method.
authors.affiliation: College of Pharmacy, Yeungnam University.
authors.forename: Shiva
authors.initials: S
authors.lastname: Pathak
authors.forename: Biki
authors.initials: B
authors.lastname: Gupta
authors.forename: Bijay Kumar
authors.initials: BK
authors.lastname: Poudel
authors.forename: Tuan Hiep
authors.initials: TH
authors.lastname: Tran
authors.forename: Shobha
authors.initials: S
authors.lastname: Regmi
authors.forename: Tung Thanh
authors.initials: TT
authors.lastname: Pham
authors.forename: Raj Kumar
authors.initials: RK
authors.lastname: Thapa
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
authors.forename: Jee-Heon
authors.initials: JH
authors.lastname: Jeong
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D065546:Drug Liberation; D019344:Lactic Acid / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship; D013499:Surface Properties; D016559:Tacrolimus / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D016559:Tacrolimus