Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Abstract

Abstract. In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0±1.4 μg/mL), compared to the pure SCE (8.12±0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6±0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2±4.7, % w/w) in comparison to the pure SCE (39.2±2.3, % w/w), or the physical mixture (42.8±2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8±3.7, % w/w), compared to the pure SCE (26.8±2.4, % w/w), or the physical mixture (33.0±2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents.

RETRACTED: Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells

“…In a previous study [46] it was reported that there was an increase in the vesicle size of avanafil invasomes with increasing Phospholipon concentration. In general, the results observed in our study were very much consistent with previously reported vesicular systems [47]. Three-dimensional (3D) response surface plots for the effect of the investigated variables on the vesicle size ( Figure 3) illustrate that ICA:Phospholipon ® 90H molar ratio exhibited the most significant effect on vesicle size.…”

Enhancement of the aqueous solubility and permeability of a poorly water soluble drug ritonavir via lyophilized milk-based solid dispersions

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Hippocampal amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid GluA1 (AMPAGluA1) receptor subunit involves in learning and memory improvement following treatment withCentella asiaticaextract in adolescent rats

“…It is a tropical plant from the Apiaceae family and is widely distributed in Southeast Asian countries, such as India, China, Sri Lanka, Malaysia, and Indonesia, as well as South Africa and Madagascar (Orhan, 2012). The major chemical constituents found in C. asiatica are triterpenoid derivatives, such as asiatic acid, madecassic acid, asiaticoside, and flavonoids (Saoji et al, 2016;Sari et al, 2014;Vasavi, Arun, & Rekha, 2016). This plant has been widely used in Ayurvedic, African, and Chinese traditional medicine (Giribabu, Srinivasarao, Swapna Rekha, Muniandy, & Salleh, 2014;Vasavi et al, 2016).…”