Cytocompatible chitosan-graft-mPEG-based 5-fluorouracil-loaded polymeric nanoparticles for tumor-targeted drug delivery.

Biodegradable materials like chitosan (CH) and methoxy polyethylene glycol (mPEG) are widely being used as drug delivery carriers for various therapeutic applications. In this study, copolymer (CH-g-mPEG) of CH and carboxylic acid terminated mPEG was synthesized by carbodiimide-mediated acid amine reaction. The resultant hydrophilic copolymer was characterized by Fourier transform infrared spectroscopy and 1H NMR studies, revealing its relevant functional bands and proton peaks, respectively. Blank polymeric nanoparticles (B-PNPs) and 5-fluorouracil loaded polymeric nanoparticles (5-FU-PNPs) were formulated by ionic gelation method. Furthermore, folic acid functionalized FA-PNPs and FA-5-FU-PNPs were prepared for folate receptor-targeted drug delivery. FA-5-FU-PNPs were characterized by particle size, zeta potential, and in vitro drug release studies, resulting in 197.7 nm, +29.9 mv, and sustained drug release of 88% in 24 h, respectively. Cytotoxicity studies were performed for FA-PNPs and FA-5-FU-PNPs in MCF-7 cell line, which exhibited a cell viability of 80 and 41%, respectively. In vitro internalization studies were carried out for 5-FU-PNPs and FA-5-FU-PNPs which demonstrated increased cellular uptake of FA-5-FU-PNPs by receptor-mediated transport. Significant (p < .01) reduction (1.5-fold) of reactive oxygen species (ROS) accumulation was observed in lipopolysaccharides-stimulated RAW264.7 macrophages, revealing its potent antioxidant property. From the obtained results, it is concluded that folic acid functionalization of 5-FU-PNPs is an ideal approach for sustained and targeted drug delivery, thereby influencing better therapeutic effect.

Aerosolized hyaluronic acid decorated, ferulic acid loaded chitosan nanoparticle: A promising asthma control strategy.

Vibrating mesh nebulizers are recognized as the most efficient actuation technique over conventional inhalers for drug deposition. This study explored hyaluronic acid (HA) decorated, ferulic acid (FA) loaded chitosan (CS) nanoparticle (FACHA) aerosolized using vibrating mesh nebulizer as strategic combination of drug, nanocarrier and delivery device for effective asthma control. FACHA exhibited spherical morphology with suitable size (164.2 ± 9.7 nm), zeta potential (24.0 ± 0.5 mV), entrapment efficiency (EE%) (65.0 ± 1.5), loading capacity (LC%) (18.5 ± 0.4) and mass median aerodynamic diameter (MMAD) of 1.81 ± 0.15 µm, ascertaining efficient drug deposition. In vivo inhalation toxicity assessment confirmed safety, while, FACHA prophylaxis mitigated inflammation, airway hypersensitivity and remodelling in ovalbumin (OVA) induced mice models. The results thus accentuated the role of pro-pulmonary surface chemistry conferred by HA functionalization that improved 1) thermal stability (thermogravimetric analysis - TGA) and 2) therapeutic efficacy of FA, by facilitating better interaction and transportation across mucus barrier, which otherwise suffers poor bioavailability and rapid metabolism.

Cellular imaging and folate receptor targeting delivery of gum kondagogu capped gold nanoparticles in cancer cells.

In this study, the green synthesis of gum kondagogu capped gold nanoparticles (GK-GNPs) was prepared using a naturally available polysaccharide. The anionic gum capped GK-GNPs enabled the successful coupling of folic acid (FA) and fluorescein isothiocyanate (FITC) to produce a fluorescently labelled GNP (F2-GNP). F2-GNPs were further characterized using different physicochemical methods Cellular viability, cellular imaging, and targeted delivery of F2-GNPs were further evaluated in both folate receptor positive (MCF-7) and folate receptor negative (A549) cancer cells. Physicochemical characterization revealed a nanoparticle with a small size (37 nm), smooth surface (surface charge of -23.7 mV), crystallinity of gold nanoparticles and existence of gum kondagogu in the F2-GNPs. Cellular uptake of F2-GNPs indicated a greater affinity towards folate receptor positive cells. This study shows that the F2-GNPs is as an effective nanocarrier for targeted drug delivery and cellular imaging via folate receptors.

Recent Trends of Biocompatible and Biodegradable Nanoparticles in Drug Delivery: A Review.

A vast amount of research on nanoparticles has been conducted in recent years with versatile applications in the field of drug delivery systems. Nanoparticles are designed as a carrier molecule to deliver drugs in a sustained and stimuli response manner. Recent advances in nanotechnology have led to the development of long circulating nanoparticles with high encapsulation efficiency. This article focuses on the properties such as biocompatibility and biodegradability, which are considered as essential criteria for nanoparticles to be successfully used as a carrier molecule in drug delivery systems. Physicochemical characterization of the nanoparticles such as size and size distribution, surface morphology, zeta potential and surface chemistry has a significant role in the successful formulation and applications in drug delivery systems. Mostly, the size and surface characteristics of nanoparticles enable enhanced intracellular accumulation in tumor cells through passive targeting mechanisms and rapid development of nanoengineering, and aid towards attaining active targeting delivery by co-functionalization of nanoparticles using appropriate targeting ligands. This article reviews the recent progress and development of employing different biocompatible and biodegradable nanoparticles in drug delivery systems. It also briefly recaps the important methods available to evaluate its biocompatibility, the mechanism of biodegradability and clearance properties of NPs.