In-vivo sustained release of nanoencapsulated ferulic acid and its impact in induced diabetes.

Diabetes mellitus (DM) is one of the most common lifestyle diseases, caused due to endocrine disorder. DM is commonly associated with hyperglycemia, a condition which is generally followed by an overproduction of free radicals leading to tissue oxidative stress. Currently, the focus of medical fraternity lies in developing therapeutic drugs based on natural origin in order to reduce the hyperglycemia associated toxicity. Ferulic acid (FA) is a ubiquitous hydroxycinnamic acid displaying an array of therapeutic properties, including anti-diabetic effect which could be attributed to its potent antioxidant capacity. However, due to low bioavailability and clinical efficacy of FA, its biomedical applications remained limited. In the present study, FA encapsulated chitosan nanoparticles (FANPs) were synthesized through ionotropic gelation process with an aim to enhance FA bioavailability. The plasma release and urinary excretion profiles of FANPs were compared with that of free FA using healthy Wistar albino rats as a model system. The encapsulated FA displayed extended plasma retention time and maximum plasma concentration was recorded at 60 min which implied four times enhancement of Tmax compared to free FA. The elimination of compound from the animal body also displayed a similar pattern where the peak urinary excretion of FA from nanoformulations. FANPs were also tested for their anti-hyperglycemic effects in streptozotocin (STZ) induced diabetes in Wistar albino rats and were found to attenuate the diabetes-associated symptoms. FANPs caused an enhancement in body weight, decrease in blood glucose level along with a regulatory effect on blood lipid profile of diabetic rats. Positive impact of FANPs in improving the hyperglycemic condition prevalent in diabetic rats might provide new avenues for the treatment of DM and help avoid secondary complications associated with the synthetic drugs.

Efficacy of ferulic acid encapsulated chitosan nanoparticles against Candida albicans biofilm.

Candida albicans, an opportunistic fungal pathogen is a major causative agent of superficial to systemic life-threating biofilm infections on indwelling medical devices. These biofilms acts as double edge swords owing to their resistance towards antibiotics and immunological barriers. To overcome this threat ferulic acid encapsulated chitosan nanoparticles (FA-CSNPs) were formulated to assess its efficacy as an antibiofilm agent against C. albicans. These FA-CSNPs were synthesized using ionotropic gelation method and observed through field emission scanning electron microscopy (FESEM) and fluorescent microscopy. Assessment of successful encapsulation and stability of ferulic acid into chitosan nanoparticles was made using Fourier transform infrared spectrum (FTIR), (1)H NMR and thermal analyses. Synthesized FA-CSNPs, were found to be cytocompatible, when tested using Human Embryonic Kidney (HEK-293) cell lines. XTT assay revealed that FA-CSNPs reduced the cell metabolic activity of C. albicans upto 22.5% as compared to native ferulic acid (63%) and unloaded CSNPs (88%) after 24 h incubation. Disruption of C. albicans biofilm architecture was visualized by FESEM. Results highlighted the potential of FA-CSNPs to be used as an effective alternative to the conventional antifungal therapeutics.

Antiproliferative activity of ferulic acid-encapsulated electrospun PLGA/PEO nanofibers against MCF-7 human breast carcinoma cells.

Ferulic acid (FA) is a polyphenolic phytonutrient which possesses strong antiproliferative effect; however, it has limited therapeutic applications due to its physiochemical instability and low bioavailability at the tumor site. In present study, these shortcomings associated with FA were overcome by fabricating FA-encapsulated poly(D,L-lactide-co-glycolide)/polyethylene oxide (PLGA/PEO) blend nanofibers using electrospinning technique. FESEM and fluorescence microscopic analysis imitates the smooth morphology and even distribution of FA within the polymeric nanofibers at optimum 2 wt% concentration of FA. The average diameters were recorded to be 150 ± 47.4 and 200 ± 79 nm for PLGA/PEO and FA-encapsulated PLGA/PEO nanofibers, respectively. The encapsulation, compatibility, and physical state of FA within the nanofibers were further confirmed by FTIR, TGA and XRD analysis. In vitro drug delivery studies demonstrated initial burst liberation of FA within 24 h followed by a sustained release for the subsequent time. MTT assay revealed the effectiveness of FA-encapsulated nanofibers against human breast carcinoma cells (MCF-7) cells as compared to control. FESEM and fluorescence microscopic analysis further confirmed the apoptotic effect of FA-encapsulated PLGA/PEO nanofibers against MCF-7. These fabricated nanofibers hold enormous potential to be used as a therapeutic agent for various biomedical applications.

Production of microbial surfactants from oily sludge-contaminated soil by Bacillus subtilis DSVP23.

The indigenous microbial community utilizing aliphatic, aromatic, and polar components from the oily sludge as sole source of carbon and energy was selected from the soil samples of Ankleshwar, India for biosurfactant production. Evaluation of biosurfactant production was done using screening assays such as surface tension reduction, hemolytic activity, emulsification activity, drop-collapse assay, and cell surface hydrophobicity studies. Maximum biosurfactant (6.9 g/l) production was achieved after 5 days of growth from Bacillus subtilis DSVP23 which was identified by 16S RNA technique (NCBI GenBank accession no. EU679368). Composition of biosurfactant showed it to be lipopeptide in nature with 15.2% protein content and 18.0% lipid content. Functional group analysis was also done by using Fourier transform infrared spectroscopy which showed it to be a protein-bound lipid thereby imparting them special properties. Analysis by matrix-assisted laser desorption/ionization time-of-flight mass spectrometric and nuclear magnetic resonance revealed that the major constituents of lipopeptide are leucine and isoleucine. Gas chromatographic analysis data indicated that oily sludge components of chain length C12-C30 and aromatic hydrocarbons were degraded effectively by B. subtilis DSVP23 after 5 days of incubation. These results collectively points toward the importance of B. subtilis DSVP23 as a potential candidate for bioremediation studies.