Abstract
The purpose of this study was to develop new formulation for an improved oral delivery of Vitex agnus-castus (VAC) extract. After the optimization and validation of analytical method for quali-quantitative characterization of extract, nanoemulsion (NE) was selected as lipid-based nanocarrier. The composition of extract-loaded NE resulted in triacetin as oil phase, labrasol as surfactant, cremophor EL as co-surfactant and water. NE contains until 60 mg/mL of extract. It was characterized by DLS and TEM analyses and its droplets appear dark with an average diameter of 11.82 ± 0.125 nm and a polydispersity index (PdI) of 0.117 ± 0.019. The aqueous solubility of the extract was improved about 10 times: the extract is completely soluble in the NE at the concentration of 60 mg/mL, while its solubility in water results less than 6 mg. The passive intestinal permeation was tested by using parallel artificial membrane permeation assay (PAMPA) and the permeation across Caco-2 cells after preliminary cytotoxicity studies were also evaluated. NE shows a good solubilizing effect of the constituents of the extract, compared with aqueous solution. The total amount of constituents permeated from NE to acceptor compartment is greater than that permeated from saturated aqueous solution. Caco-2 test confirmed PAMPA results and they revealed that NE was successful in increasing the permeation of VAC extract. This formulation could improve oral bioavailability of extract due to enhanced solubility and permeability of phytocomplex.
Highlights
In the last years, the use of herbal medicines has been increased due to their therapeutic effects and fewer adverse effects as compared with the modern medicines
NE contains until 60 mg/mL of extract. It was characterized by dynamic light scattering (DLS) and TEM analyses and its droplets appear dark with an average diameter of 11.82 ± 0.125 nm and a polydispersity index (PdI) of 0.117 ± 0.019
The passive intestinal permeation was tested by using parallel artificial membrane permeation assay (PAMPA) and the permeation across Caco-2 cells after preliminary cytotoxicity studies were evaluated
Summary
The use of herbal medicines has been increased due to their therapeutic effects and fewer adverse effects as compared with the modern medicines. Drug delivery systems represent good tools to formulate herbal drugs and to enhance their bioavailability. The novel formulations have remarkable advantages over conventional formulations of natural compounds and extracts, which include increase of solubility, bioavailability, stability, enhancement of intracellular uptake, modification of pharmacokinetics and bio-distribution, sustained delivery. The strategy of drug delivery systems has been applied to Many synthetic drugs and to phytopharmaceuticals, including both isolated compounds and purified extracts (Porter et al, 2008; Sermkaew et al, 2013; Bergonzi et al, 2013, 2014; Righeschi et al, 2014; Esfanjani & Jafari, 2016; Isacchi et al, 2016).
Sign-in/Register to view highlights & summary 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 callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
