Abstract
Gentian (Gentiana lutea L., Gentianaceae) root extract (GRE) is used for the treatment of gastrointestinal disorders. However, its bioactive potential is limited in conventional forms due to the low bioavailability and short elimination half-life of the dominant bioactive compound, gentiopicroside. The aim of study was to encapsulate GRE in the lipid-based gastroretentive delivery system that could provide high yield and encapsulation efficiency, as well as the biphasic release of gentiopicroside from the tablets obtained by direct compression. Solid lipid microparticles (SLM) loaded with GRE were prepared by freeze-drying double (W/O/W) emulsions, which were obtained by a multiple emulsion–melt dispersion technique, with GRE as the inner water phase, Gelucire® 39/01 or 43/01, as lipid components, with or without the addition of porous silica (Sylysia® 350) in the outer water phase. Formulated SLM powders were examined by SEM and mercury intrusion porosimetry, as well as by determination of yield, encapsulation efficiency, and flow properties. Furthermore, in vitro dissolution of gentiopicroside, the size of the dispersed systems, mechanical properties, and mucoadhesion of tablets obtained by direct compression were investigated. The results have revealed that SLM with the macroporous structure were formulated, and, consequently, the powders floated immediately in the acidic medium. Formulation with porous silica (Sylysia® 350) and Gelucire® 43/01 as a solid lipid was characterized with the high yield end encapsulation efficiency. Furthermore, the mucoadhesive properties of tablets obtained by direct compression of that formulation, as well as the biphasic release of gentiopicroside, presence of nanoassociates in dissolution medium, and optimal mechanical properties indicated that a promising lipid-based gastroretentive system for GRE was developed.
Highlights
Yellow gentian (Gentiana lutea L., Gentianaceae) root is officially listed in the European and many national Pharmacopoeias [1]
The objective of this study was to develop a lipid-based gastroretentive delivery system loaded with the gentian extract that could provide high yield and encapsulation efficiency, as well as the biphasic release of gentiopicroside from tablets obtained by direct compression of powder obtained by the freeze-drying of double emulsions with gentian extract as the inner water phase and Gelucire® 39/01 or 43/01, as lipid components, without the addition of organic solvents
An effective method for the encapsulation of gentian extract into solid lipid microparticles was developed by freeze-drying double (W/O/W) emulsions with solid lipid, i.e., Gelucire® 39/01 or 43/01, with polyglycerol ployricinoleate as lipophilic emulsifier and lecithin as a hydrophilic emulsifier
Summary
Yellow gentian (Gentiana lutea L., Gentianaceae) root is officially listed in the European and many national Pharmacopoeias [1]. In order to improve the bioavailability and effectiveness, as well as patient compliance, it is necessary to enable the release of an initial, effective dose of gentian extract, followed by further sustained release at the place of action (stomach). This would allow improved absorption of the gentian extract active compounds. Solid lipid microparticles have been applied as a carrier for the bioactive compound site-specific delivery [8] This type of carrier provides good in vivo tolerability, adequate stability, and increased bioavailability, with quite low production costs and feasibility of large-scale production [9]. It is known that the formulation of double emulsions could be a challenging task because of their low thermodynamic stability [12]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
