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Dry powder inhalation of macromolecules using novel PEG-co-polyester microparticle carriers.
Tawfeek, Hesham M; Evans, Andrew R; Iftikhar, Abid; Mohammed, Afzal R; Shabir, Anjum; Somavarapu, Satyanarayana; Hutcheon, Gillian A; Saleem, Imran Y.
Afiliação
  • Tawfeek HM; School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, Liverpool, UK.
Int J Pharm ; 441(1-2): 611-9, 2013 Jan 30.
Article em En | MEDLINE | ID: mdl-23124106
This study investigated optimizing the formulation parameters for encapsulation of a model mucinolytic enzyme, α-chymotrypsin (α-CH), within a novel polymer; poly(ethylene glycol)-co-poly(glycerol adipate-co-ω-pentadecalactone), PEG-co-(PGA-co-PDL) which were then applied to the formulation of DNase I. α-CH or DNase I loaded microparticles were prepared via spray drying from double emulsion (w(1)/o/w(2)) utilizing chloroform (CHF) as the organic solvent, L-leucine as a dispersibility enhancer and an internal aqueous phase (w(1)) containing PEG4500 or Pluronic(®) F-68 (PLF68). α-CH released from microparticles was investigated for bioactivity using the azocasein assay and the mucinolytic activity was assessed utilizing the degradation of mucin suspension assay. The chemical structure of PEG-co-(PGA-co-PDL) was characterized by (1)H NMR and FT-IR with both analyses confirming PEG incorporated into the polymer backbone, and any unreacted units removed. Optimum formulation α-CH-CHF/PLF68, 1% produced the highest bioactivity, enzyme encapsulation (20.08±3.91%), loading (22.31±4.34 µg/mg), FPF (fine particle fraction) (37.63±0.97%); FPD (fine particle dose) (179.88±9.43 µg), MMAD (mass median aerodynamic diameter) (2.95±1.61 µm), and the mucinolytic activity was equal to the native non-encapsulated enzyme up to 5h. DNase I-CHF/PLF68, 1% resulted in enzyme encapsulation (17.44±3.11%), loading (19.31±3.27 µg/mg) and activity (81.9±2.7%). The results indicate PEG-co-(PGA-co-PDL) can be considered as a potential biodegradable polymer carrier for dry powder inhalation of macromolecules for treatment of local pulmonary diseases.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Portadores de Fármacos / Quimotripsina / Sistemas de Liberação de Medicamentos / Desoxirribonuclease I Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Portadores de Fármacos / Quimotripsina / Sistemas de Liberação de Medicamentos / Desoxirribonuclease I Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article