title: Evaluation of P(L)LA-PEG-P(L)LA as processing aid for biodegradable particles from gas saturated solutions (PGSS) process.
abstract: A series of biodegradable P(L)LA-PEG1.5 kDa-P(L)LA copolymers have been synthesized and compared as processing aid versus Poloxamer 407 (PEO-PPO-PEO), in the formulation of protein encapsulated microparticles, using supercritical carbon dioxide (scCO2). Bovine serum albumin (BSA) loaded microcarriers were prepared applying the particles from the gas saturated solutions (PGSS) technique using scCO2 and thus, avoiding the standard practice of organic solvent encapsulation. Four triblock copolymers were synthesized and characterized, particularly in terms of thermal properties and behaviour when exposed to scCO2. The effects of the inclusion of these copolymers in the formulation of poly(α-hydroxy acids) based microparticles - e.g. poly(D,L-lactic-co-glycolic acid) (PLGA) and poly(D,L-lactide) (PLA) - were analysed in terms of yield, particle size, morphology and drug release. The use of P(L)LA-PEG1.5 kDa-P(L)LA triblock copolymers were found to increase the yield of the PGSS-based process and to decrease the size of the microparticles produced, in comparison with the formulation containing the Poloxamer 407. Moreover the microparticles formulated with the triblock copolymers possessing the higher hydrophobic character were able to maintain a controlled drug release profile.
authors.affiliation: School of Pharmacy, University of Camerino, Via Sant'Agostino 1, Camerino, MC 62032, Italy.
authors.forename: D R
authors.initials: DR
authors.lastname: Perinelli
authors.affiliation: School of Pharmacy, University of Camerino, Via Sant'Agostino 1, Camerino, MC 62032, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Bonacucina
authors.affiliation: School of Pharmacy, University of Camerino, Via Sant'Agostino 1, Camerino, MC 62032, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Cespi
authors.affiliation: Critical Pharmaceuticals Limited BioCity, Pennyfoot Street, Nottingham NG1 1GF, United Kingdom.
authors.forename: A
authors.initials: A
authors.lastname: Naylor
authors.affiliation: Critical Pharmaceuticals Limited BioCity, Pennyfoot Street, Nottingham NG1 1GF, United Kingdom.
authors.forename: M
authors.initials: M
authors.lastname: Whitaker
authors.affiliation: School of Pharmacy, University of Camerino, Via Sant'Agostino 1, Camerino, MC 62032, Italy.
authors.forename: G F
authors.initials: GF
authors.lastname: Palmieri
authors.affiliation: School of Pharmacy, University of Camerino, Via Sant'Agostino 1, Camerino, MC 62032, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Giorgioni
authors.affiliation: Department of Biomolecular Sciences, University of Urbino, Piazza Rinascimento 6, Urbino, PU 61029, Italy. Electronic address: luca.casettari@uniurb.it.
authors.forename: L
authors.initials: L
authors.lastname: Casettari
mesh_terms: D002245:Carbon Dioxide; D002626:Chemistry, Pharmaceutical; D025924:Chromatography, Supercritical Fluid; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005740:Gases; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D019344:Lactic Acid / Q000138:chemical synthesis*; D020442:Poloxamer / Q000138:chemical synthesis; D011091:Polyesters; D011092:Polyethylene Glycols / Q000138:chemical synthesis*; D011100:Polyglycolic Acid / Q000138:chemical synthesis; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000138:chemical synthesis*; D016062:Porosity; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods*; D014783:Viscosity
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005740:Gases; D011091:Polyesters; D011108:Polymers; D020442:Poloxamer; D002245:Carbon Dioxide; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid; D011092:Polyethylene Glycols; C033616:poly(lactide)
keywords: BSA; Biodegradable microparticles; Block copolymers; PGSS; scCO(2)