title: Factors influencing the erosion rate and the drug release kinetics from organogels designed as matrices for oral controlled release of a hydrophobic drug.
abstract: This article proposes solid-like systems from sunflower oil structured with a fibrillar network built by the assembly of 12-hydroxystearic acid (12-HSA), a gelator molecule for an oil phase. The resulting organogels were studied as oral controlled release formulations for a lipophilic drug, Efavirenz (EFV), dissolved in the oil. The effects of the gelator concentration on the thermal properties of the organogels were studied by Differential Scanning Calorimetry (DSC) and showed that drug incorporation did not change the sol-gel-sol transitions. The erosion and drug release kinetics from organogels under conventional (filling gelatin capsules) or multiparticulate (beads obtained by prilling) dosage forms were measured in simulated gastric and intestinal fluids. EFV release profiles were analyzed using model-dependent (curve-fitting) and independent approaches (Dissolution Efficiency DE). Korsmeyer-Peppas was the best fitting release kinetic model based on the goodness of fit, revealing a release mechanism from organogels loaded with EFV different from the simple drug diffusion release mechanism obtained from oily formulations. From organogels, EFV probably diffuses through an outer gel layer that erodes releasing oil droplets containing dissolved EFV into the aqueous medium.
authors.affiliation: a Mines Albi, CNRS, Centre RAPSODEE, Campus Jarlard, Université De Toulouse , Albi CT Cedex , France .
authors.forename: Sarah Regina
authors.initials: SR
authors.lastname: Pereira Camelo
authors.affiliation: b Laboratoire Des I.M.R.C.P. , Université Paul Sabatier , Toulouse , France , and.
authors.forename: Sophie
authors.initials: S
authors.lastname: Franceschi
authors.affiliation: b Laboratoire Des I.M.R.C.P. , Université Paul Sabatier , Toulouse , France , and.
authors.forename: Emile
authors.initials: E
authors.lastname: Perez
authors.affiliation: c Faculty of Sciences Pharmaceutiques , CIRIMAT INPT-CNRS-UPS, Université Toulouse , Toulouse , France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Girod Fullana
authors.affiliation: a Mines Albi, CNRS, Centre RAPSODEE, Campus Jarlard, Université De Toulouse , Albi CT Cedex , France .
authors.forename: Maria Inês
authors.initials: MI
authors.lastname: Ré
mesh_terms: D000284:Administration, Oral; D000480:Alkynes; D048588:Benzoxazines / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003521:Cyclopropanes; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D005780:Gelatin / Q000737:chemistry; D005782:Gels / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D010938:Plant Oils / Q000737:chemistry; D012995:Solubility; D000074242:Sunflower Oil
chemical_list: D000480:Alkynes; D048588:Benzoxazines; D003521:Cyclopropanes; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005782:Gels; D010938:Plant Oils; D000074242:Sunflower Oil; D005780:Gelatin; C098320:efavirenz
keywords: Efavirenz; lipid formulation; multiparticulate dosage form; oral drug delivery; organogel; poorly soluble drugs; prilling process; release profile models