title: Polyester-based microparticles of different hydrophobicity: the patterns of lipophilic drug entrapment and release.
abstract: The paper is devoted to the investigation of the effect of polyester hydrophobicity and ability for crystallisation on lipophilic drug loading and release from microparticles fabricated on the base of these polymers. Poly(l-lactic acid), poly(d, l-lactic acid) and poly (lactic acid-co-glycolic acid) were synthesised by ring-opening polymerisation using stannous octoate as catalyst, while poly(caprolactone) (PCL) and poly(ω-pentadecalactone) (PPDL) formation was catalysed by lipase. The particles were formed via single emulsion evaporation/diffusion method. The particles obtained were studied using SEM, XRD and DSC methods. The degradation of particles based on different polyesters, entrapment and release of a model hydrophobic drug (risperidone®) were thoroughly studied. The effect of particles hydrophobicity and crystallinity on these parameters was of most interest. The drug entrapment is greater for the hydrophobic polymers. Drug release was more rapid from crystalline particles (PLLA, PCL, PPDL), than from amorphous PDLLA and PLGA ones.
authors.affiliation: a Institute of Chemistry , Saint-Petersburg State University , St. Petersburg , Russia ;
authors.forename: Viktor
authors.initials: V
authors.lastname: Korzhikov
authors.affiliation: b Institute of Macromolecular Compounds, Russian Academy of Sciences , St. Petersburg , Russia.
authors.forename: Ilia
authors.initials: I
authors.lastname: Averianov
authors.affiliation: b Institute of Macromolecular Compounds, Russian Academy of Sciences , St. Petersburg , Russia.
authors.forename: Evgeniia
authors.initials: E
authors.lastname: Litvinchuk
authors.affiliation: a Institute of Chemistry , Saint-Petersburg State University , St. Petersburg , Russia ;
authors.forename: Tatiana B
authors.initials: TB
authors.lastname: Tennikova
mesh_terms: D014150:Antipsychotic Agents / Q000008:administration & dosage* / Q000737:chemistry; D003460:Crystallization; D003692:Delayed-Action Preparations / Q000737:chemistry*; D018492:Dopamine Antagonists / Q000008:administration & dosage* / Q000737:chemistry; D065546:Drug Liberation; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D019344:Lactic Acid / Q000737:chemistry; D018942:Macrolides / Q000737:chemistry; D011091:Polyesters / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D018967:Risperidone / Q000008:administration & dosage* / Q000737:chemistry; D020298:U937 Cells
chemical_list: D014150:Antipsychotic Agents; D003692:Delayed-Action Preparations; D018492:Dopamine Antagonists; D018942:Macrolides; D011091:Polyesters; C571591:omega-pentadecalactone; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C016240:polycaprolactone; D011100:Polyglycolic Acid; D019344:Lactic Acid; C033616:poly(lactide); D018967:Risperidone
keywords: Biodegradable particles; drug encapsulation; drug release; risperidone