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Abstract

Nonhardened gelatin-acacia microcapsules were studied for encapsulation of microdroplets of oil solution containing a lipophilic drug as core material and ready disintegration with release of micro oil droplets in the gastrointestinal tract. Probucol and S-312-d, a Ca-channel blocker, were employed as model lipophilic drugs. Glyceryl tricaprylate and tricaprate mixture solutions containing these drugs were encapsulated according to the complex coacervation method and were recovered as free-flowing powders without any hardening (cross-linking) step. The microcapsules obtained were disintegrated, and the emulsion was reproduced within 3 min at 37 degrees C in the first or second test solution defined in the Japanese Pharmacopeia XII. When the microcapsules were stored as a powder at room temperature in a closed bottle, no significant change in their appearance or disintegration time upon rehydration was observed even after 1 year. Oral bioavailabilities of model drugs from the microcapsules were tested in rats and dogs and compared with those from other conventional formulations. Gastrointestinal absorption of both probucol and S-312-d from the microcapsules was remarkably more efficient than that from other formulations such as powders, granules, or oil solution. The proposed method for microencapsulation could be useful for powdering drug-containing oil solutions or O/W emulsions while maintaining excellent bioavailability.

Stabilization mechanism of oil-in-water emulsions by β-lactoglobulin and gum arabic

“…Finally in protocol 3, emulsions were prepared with a b-lg solution, and then diluted by a GA solution. Note that this latter procedure can be used for oil encapsulation via interfacial coacervation [33]. Emulsification procedure was the same as the one described above (rotor-stator and high pressure homogenizers) and emulsion dilution was performed by simple hand reversal shaking to minimize system destructuring.…”

“…Over the last decade, proteins and polysaccharides and their complexes have emerged in the pharmaceutical field mainly for microencapsulation [32][33][34]. However, to our knowledge, there is currently no marketed pharmaceutical emulsion stabilized by a combination of protein and polysaccharide.…”

Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

“…As the major route of elimination is the bile and feces, renal clearance is very low (2%) 13,14. In one study, gelatin-acacia microcapsules were prepared by using a special coacervation method and were studied for encapsulating microdroplets of oil solution containing PB; this resulted in better bioavailability 15. PB’s low and variable oral bioavailability, and its nonlinear distribution and clearance, contribute to the variability in its pharmacokinetic (PK) and pharmacodynamic properties, as well as its adverse effects 16,17.…”

Nanotechnology: A Valuable Strategy to Improve Bacteriocin Formulations

“…Carbohydrates are naturally occurring organic substances that serve both structural and storage functions (Ghazarian et al, 2011 ). They are biodegradable, biocompatible substances, with highly stable properties, and thus have attracted much attention for their applications in the food, biomedical and environmental fields (Chen and Soucie, 1985 ; Jizomoto et al, 1993 ; Richardson et al, 1999 ; Melamu and Von Blottnitz, 2009 ). Chitosan, a natural biopolymer produced by the deacetylation of chitin, is one of the most commonly used polysaccharides for fabrication of nanoparticles (Nitta and Numata, 2013 ).…”