Synthesis and bioactivity assessment of Coccinia grandis L. extract encapsulated alginate nanoparticles as an antidiabetic drug lead.

AIM: This study aimed to prepare, characterise, and evaluate the antidiabetic activity of Coccinia grandis (L.) extracts encapsulated alginate nanoparticles. METHODS: Alginate nanoparticles were prepared using the ionic gelation method and characterised by encapsulation efficiency %w/w, loading capacity %w/w, particle size analysis, zeta potential, Fourier transform infra-red spectroscopy (FTIR), and scanning electron microscopy (SEM). In vitro antidiabetic activity was also evaluated. RESULTS: Encapsulation efficiency %w/w, loading capacity %w/w, mean diameter, zeta potential of C. grandis encapsulated alginate nanoparticles ranged from 10.51 ± 0.51 to 62.01 ± 1.28%w/w, 0.39 ± 0.04 to 3.12 ± 0.11%w/w, 191.9 ± 76.7 to 298.9 ± 89.6 nm, -21.3 ± 3.3 to -28.4 ± 3.4 mV, respectively. SEM and FTIR confirmed that particles were in nano range with spherical shape and successful encapsulation of plant extracts into an alginate matrix. The antidiabetic potential of aqueous extract of C. grandis encapsulated alginate nanoparticles (AqCG-ANP) exhibited inhibition in α-amylase, α-glucosidase and dipeptidyl peptidase IV enzymes of 60.8%c/c, 19.1%c/c, and 30.3%c/c, respectively, compared to the AqCG. CONCLUSION: The AqCG-ANP exerted promising antidiabetic potential as an antidiabetic drug lead.

Bael (Aegle marmelos L. Correa) fruit extracts encapsulated alginate nanoparticles as a potential dietary supplement with improved bioactivities.

Nanoencapsulated bael fruit (Aegle marmelos L. Correa (Family: Rutaceae)) extracts reveal novel prospects in the development of dietary supplements with improved biological activities in the field of the food industry. The main objectives of this study were to prepare and characterize aqueous, ethanol, 50% ethanol, and 50% acetone extracts of bael fruit encapsulated alginate nanoparticles and investigate the effect of encapsulation on in vitro release of polyphenols, antidiabetic, antioxidant, and anti-inflammatory activities, and their stability. Bael fruit extracts encapsulated alginate nanoparticles were prepared using the ionic gelation method. Characterization, in vitro release profiles of polyphenols, determination of antidiabetic, anti-inflammatory, antioxidant activity, and accelerated stability were conducted. The results of the characterization confirmed the successful encapsulation of extracts of bael fruit in the alginate matrix. The aqueous extract of bael fruit encapsulated alginate nanoparticles exhibited a more controlled slow-release profile, accounting for 21.82% ± 1.17% and 48.14% ± 0.52% of polyphenols at solutions of pH 1.2 and pH 6.8, respectively. In general, the results of the bioactivity assessment suggested that nanoencapsulation could facilitate the enhancement of its antidiabetic, antioxidant, and anti-inflammatory properties. The results of thermogravimetric analysis and thin layer chromatography fingerprint showed the stability of aqueous bael fruit extract encapsulated alginate nanoparticles at 27 and 4°C over a month. In summary, the results of this study revealed the potency of nanoencapsulated aqueous extract of bael fruit to develop a dietary supplement with improved antidiabetic, antioxidant, and anti-inflammatory activities. PRACTICAL APPLICATION: The encapsulation of bael fruit extracts into a nanocarrier enhances bioactivities and promotes the controlled release of bioactive compounds. This could be useful in the future food industry, based on scientifically proven data, and inspire the market by means of the development of dietary supplements. Overall, the results would facilitate the formulation of novel commercially elegant nanoencapsulated dietary supplements with improved potential to manage a healthy life.

A new liposomal nanocarrier for co-delivery of gedunin and p-glycoprotein siRNA to target breast cancer stem cells.

Gedunin is a secondary metabolite found in neem tree. Since the first discovery of this compound, its bio-active properties have been continuously evaluated. However, the low hydrophobicity of gedunin decreases its bioavailability and pharmacokinetic profile. In the present investigation, a new liposomal nanocarrier for co-delivery of gedunin and P-glycoprotein (P-gp) siRNA [siRNA coated liposomal gedunin (Lipo-Ged-siRNA)] was developed to improve the anti-proliferative activity of gedunin. Characteristics of prepared Lipo-Ged-siRNA demonstrated promising effects. Lipo-Ged-siRNA showed greater anti-proliferative effects (IC50-8.5 µg/mL) followed by pure gedunin (IC50- 40.2 µg/mL) in breast cancer stem cells (bCSCs). Immunofluorescence analysis demonstrated reduced expression of P-gp following exposure to Lipo-Ged-siRNA. Furthermore, Lipo-Ged-siRNA affected the expression of ABCB1, Cyclin D1, Bax, p53, and surviving genes in bCSCs.