ABSTRACT
The preparation of microcapsules with a self-microemulsifying system (SMES) core using a vibrating nozzle technology was improved with regard to process reproducibility and core phase retention. The microcapsule shell was optimized for composition of the alginate-pectin (A/P) ratio and hydrophilic filling agent content. The best-shaped microcapsules with highest encapsulation efficiency for furosemide-loaded SMES were obtained from the shell-formation phase with an A/P ratio of 25:75, containing 10% lactose, which was hardened through a one-step process. Fluid-bed dried microcapsules were examined for their release characteristics and swelling behavior of the polymeric matrix. Incorporation of hydrophilic filling agents in the shell-formation phase was shown to be successful in limiting the leakage of the core phase during the microcapsule production and drying processes. Moreover, the addition of different fillers also allows the drug release profile from Ca-alginate/pectinate microcapsules with a self-microemulsifying core to be modified.
Subject(s)
Alginates/chemistry , Drug Compounding/methods , Drug Delivery Systems , Pectins/chemistry , Furosemide/chemistry , Glucuronic Acid/chemistry , Glycerides , Glycerol/analogs & derivatives , Glycerol/chemistry , Hexuronic Acids/chemistry , Lactose/chemistry , Mannitol/chemistry , Oleic Acids/chemistry , Organic Chemicals/chemistry , Sorbitol/chemistry , Trehalose/chemistry , Triglycerides/chemistryABSTRACT
Microcapsules with self-microemulsifying core were originated by the vibrating nozzle method. Alginate-pectin (A/P) ratio of the shell forming phase was optimized with regard to core phase retention and drug release kinetics from dried microcapsules. Well shaped microcapsules with high encapsulation efficiency were produced when an A/P composition of 25:75 was used. Microcapsules with higher pectin content exhibited faster drug release, which was additionally enhanced by the addition of sodium chloride to the shell phase.
Subject(s)
Capsules/chemistry , Desiccation , Diuretics/administration & dosage , Diuretics/chemistry , Drug Compounding/methods , Emulsions , Excipients , Furosemide/administration & dosage , Furosemide/chemistry , Kinetics , Pectins , Sodium Chloride , SolubilityABSTRACT
The primary goal of this study was to formulate Ca-pectinate microcapsules with self-microemulsifying core to enhance the solubility and permeability of BCS class IV drug furosemide. An Inotech IE-50R encapsulator equipped with a concentric nozzle was utilized to transform liquid self-microemulsifying system (SMES) to solid microcapsules. Self-microemulsifying core was optimized with respect to drug loading capacity and encapsulation efficiency and evaluated for its impact on furosemide permeability through rat small intestine and Caco-2 cell monolayers. Retention of the core phase was considerably improved (up to 70-80%) by optimization of the SMES and microcapsules' drying process. Incorporation of furosemide in self-microemulsifying core of microcapsules resulted in improved permeability and drug release characteristics in comparison to microspheres (without SMES in the core). The obtained results illustrate the prospective use of microcapsules with self-microemulsifying core for the delivery of compounds with poor biopharmaceutical properties via the oral route.
