Titre du document / Document title

The preparation and evaluation of poly(ε-caprolactone) microparticles containing both a lipophilic and a hydrophilic drug

Auteur(s) / Author(s)

HOMBREIRO PEREZ M. ⁽¹⁾ ; ZINUTTI C. ⁽¹⁾ ; LAMPRECHT A. ⁽²⁾ ; UBRICH N. ⁽¹⁾ ; ASTIER A. ⁽¹⁾ ; HOFFMAN M. ⁽¹⁾ ; BODMEIER R. ⁽³⁾ ; MAINCENT P. ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Laboratoire de Pharmacie Galénique et Biopharmacie, Université de Nancy 1, 5 rue A. Lebrun, BP 403, 54001 Nancy, FRANCE
⁽²⁾ Institut für Biopharmazie und Pharmazeutische Technologie, Universität des Saarlandes, Im Stadwald, 66123 Saarbrücken, ALLEMAGNE
⁽³⁾ College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, ALLEMAGNE

Résumé / Abstract

An original dosage form for oral delivery based on the encapsulation of both, lipophilic and hydrophilic drugs, in poly(ε-caprolactone) (PCL) microparticles prepared either by the oil-in-water (o/w) or the water-in-oil-in-water (w/o/w) solvent evaporation method was developed. Microparticles were characterized in terms of morphology, size, encapsulation efficiency and drug release. The physical state of the drugs and the polymer was determined by scanning electron microscopy (SEM), X-ray powder diffractometry, and differential scanning calorimetry (DSC). Nifedipine (calcium antagonist) and propranolol HCI (β-blocker), used for the treatment of hypertension, were chosen as lipophilic and hydrophilic drugs. The microparticles were spherical with diameters in the range of 191-351 μm by the o/w-method, and in the range of 302-477 μm by the w/o/w-method. The encapsulation efficiency (EE) was 91% for nifedipine and 37% for propranolol HCI with the o/w-method, and 83% for nifedipine and 57% for propranolol HCI with the w/o/w-method. DSC and X-ray diffraction studies showed that PCL maintained its semi-crystalline structure, while the drugs were either dispersed or dissolved in the polymer. In vitro release studies revealed a controlled release of nifedipine and propranolol HCI from microparticles prepared by the o/w-method; a burst release of propranolol HCI was observed from microparticles prepared by the w/o/w-method. In conclusion, microparticles containing both a hydrophilic and a lipophilic drug were successfully prepared.

Revue / Journal Title

Journal of controlled release   ISSN 0168-3659   CODEN JCREEC 

Source / Source

2000, vol. 65, n^o3, pp. 429-438 (32 ref.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1984) (Revue)

Mots-clés anglais / English Keywords

Nifedipine ; Propranolol ; Antihypertensive agent ; Pharmaceutical technology ; Dosage form ; Drug carrier ; Control release polymer ; Water oil water emulsion ; Oil water emulsion ; Release ; Active ingredient ; In vitro ; Polycaprolactone ; Encapsulation ; Particle size ; Capsule ; Dihydropyridine derivatives ; Tablet ;

Mots-clés français / French Keywords

Nifédipine ; Propranolol ; Antihypertenseur ; Technologie pharmaceutique ; Forme pharmaceutique ; Vecteur médicament ; Polymère vecteur ; Emulsion eau huile eau ; Emulsion huile eau ; Libération ; Principe actif ; In vitro ; Caprolactone polymère ; Encapsulation ; Dimension particule ; Capsule ; Dihydropyridine dérivé ; Comprimé ; Microparticule ;

Mots-clés espagnols / Spanish Keywords

Nifedipino ; Propranolol ; Antihipertensivo ; Tecnología farmacéutica ; Forma farmacéutica ; Vector medicamento ; Polímero vector ; Emulsión agua aceite agua ; Emulsión aceite agua ; Liberación ; Principio activo ; In vitro ; Caprolactona polímero ; Encapsulación ; Dimensión partícula ; Cápsula ; Dihidropiridine derivado ; Tableta ;

Localisation / Location

INIST-CNRS, Cote INIST : 20704, 35400008688245.0090