Formulation and statistical optimization of gastric floating alginate/oil/chitosan capsules loading procyanidins: in vitro and in vivo evaluations.

The aim of the present work was to develop gastric floating capsules containing oil-entrapped beads loading procyanidins. The floating beads were prepared by ionotropic gelation method using sodium alginate, CaCl2 and chitosan. The effect of three independent parameters (concentration of sodium alginate, CaCl2 and chitosan) on entrapment efficiency were analyzed by Box-Behnken design. The floating beads were evaluated for surface morphology, particle size, density, entrapment efficiency, buoyancy, release behavior in vitro and floating ability in vivo. The prepared beads were grossly spherical in shape and the mean size was approximately 1.54±0.17mm. The density was 0.97g/cm3. And the optimal conditions were as follows: concentration of sodium alginate, CaCl2 and chitosan were 33.75mg/mL, 9.84mg/mL and 9.05mg/mL, respectively. The optimized formulation showed entrapment efficiency of 88.84±1.04% within small error-value (0.65). The release mechanism of floating capsules followed Korsmeyer-Peppas model (r2=0.9902) with non-Fickian release. The gastric floating capsules exhibited 100% floating percentage in vitro and they could float on the top of gastric juice for 5h in vivo. Therefore, the floating capsules are able to prolong the gastroretentive delivery of procyanidins.

Preparation of enteric-coated microcapsules of astaxanthin oleoresin by complex coacervation.

Astaxanthin oleoresin (AO) has a number of beneficial physiological functions. However, its sensitivity to light, heat, oxygen and gastric fluids has limited its application. In this paper, we describe the preparation of AO enteric microcapsules by coacervation to improve its stability and enteric solubility, and evaluate their efficacy by measuring the drug loading, encapsulation efficiency, optical microscopic appearance, stability, in vitro release and bioavailability. The results obtained showed that the AO enteric microcapsules possessed a high encapsulation efficiency (85.9%), a satisfactory in vitro release profile, and the ability of the microencapsulated AO to resist the effects of light, heat and oxygen was improved by 2.2-fold, 3.1-fold and 2.4-fold, respectively, during storage. In addition, the bioavailability of AO microcapsules was approximately 1.29-fold higher than AO, which is important for pharmaceutical applications and as a functional food.