Development, characterization and in vitro-in vivo evaluation of Farnesol loaded niosomal gel for applications in oral candidiasis treatment.

OBJECTIVES: The aim of the study was to formulate and characterize the farnesol loaded niosomes comprising gel formulation and perform their in vitro-in vivo evaluation for applications in the treatment of oral candidiasis infections. METHODS: Various gelling systems were evaluated for their rheological and stability properties. The formulation was statistically optimized using experimental design method (Box-Behnken). Transmission electron microscopy (TEM) and Atomic force microscopy (AFM) were used to observe the niosomal surface morphology. Centrifugation method and dialysis method were used to find out the % entrapment efficiency (%EE) and in-vitro release of Farnesol, respectively. In-vitro antifungal effect and cell biocompatibility of the Farnesol loaded niosomal gel was also performed using Candida albicans (C. albicans) as the model organism and epithelial cell line (SW480) by MTT cytotoxicity assay. In-vivo skin irritation test was performed on rabbit skin. KEY FINDINGS: Farnesol loaded niosomes were integrated into polymeric gel solution. The optimized formulation demonstrated acceptable % EE (>80%) and an optimum particle size (168.8 nm) along with a sustained release and a long-term storage stability for up to a period of 6 months. TEM and AFM observations displayed a spherical niosome morphology. Farnesol niosomal gel showed a higher antifungal efficacy, ex-vivo skin permeation and deposition in comparison to plain farnesol solution. The niosomal gel also showed negligible cytotoxicity to normal cells citing biocompatibility and was found to be non-toxic and non-irritant to rabbit skin. CONCLUSIONS: This novel niosome loaded gel-based formulation could make the oral candidiasis healing process more efficient while improving patient compliance. With the optimized methodology used in this work, such formulation approaches can become an efficient, industrially scalable, and cost-effective alternatives to the existing conventional formulations.

Design, development and in-vitro/in-vivo evaluation of intranasally delivered Rivastigmine and N-Acetyl Cysteine loaded bifunctional niosomes for applications in combinative treatment of Alzheimer's disease.

The present investigation explores the potential of novel dual drug-loaded niosomes for nasal delivery of Rivastigmine (RIV) and N-Acetyl Cysteine (NAC) to the brain. The dual niosomes showed a particle size of 162.4 nm and % entrapment efficiencies of 97.7% for RIV and 85.9% for NAC. The niosomes were statistically validated using Box-Behnken experimental design (BBD) with good significance. Ultrastructural and chemical characterization of the niosomes using various analytical techniques like Fourier Transform Infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), Transmission electron microscopy (TEM) showcased drug-excipient compatibility and robust stability of 6 months in a liquid state at 4-8 °C. The dual drug-loaded niosomes showed a sustained drug release pattern up to 2 days. Acetylcholinesterase (AChE) and DPPH (1, 1-diphenyl-2- picrylhydrazyl) enzyme inhibition assays showed a better combinative effect than the free drug solutions. A 2-day nasal permeation proved the effectiveness and biocompatibility of the niosomes. In-vivo pharmacokinetic and organ biodistribution studies revealed a better drug profile and greater distribution of the niosomes in the brain compared to other organs, thereby indicating a direct nose-to-brain delivery of the niosomes.

Physicochemical and biological assessment of silver nanoparticles immobilized Halloysite nanotubes-based resin composite for dental applications.

OBJECTIVE: The purpose of this study was to investigate the effect of Silver nanoparticle immobilized Halloysite Nanotubes (HNT/Ag) fillers on physicochemical, mechanical, and biological properties of novel experimental dental resin composite in order to compare with the properties of corresponding composites containing conventional glass fillers. METHODS: Dental resin (Bis-GMA/TEGDMA with ratio 70/30) composites were prepared by incorporation of varied mass fraction of HNT/Ag. Experimental composites were divided into six groups, one control group and five experimental groups containing mass fraction 1 to 10.0 wt. % of HNT/Ag. Mechanical properties of the dental composites were recorded. Degree of conversion and depth of cure of the dental resin composites were assessed. Antimicrobial properties were assessed using agar diffusion test and evaluation of cytotoxicity were performed on NIH-3T3 cell line. RESULTS: The inclusion of mass fractions (1-5 wt. %) of the HNT/Ag in dental resins composites, significantly improved mechanical properties. While, addition of larger mass fractions (7.5 and 10 wt. %) of the HNT/Ag did not show further improvement in the mechanical properties of dental resins composites. Theses composites also demonstrated satisfactory depth of cure and degree of conversion. A significant antibacterial activity was observed on S. mutans. No significant cytotoxicity was found on NIH-3T3 cell lines. CONCLUSION: The incorporation of HNT/Ag in Bis-GMA/TEGDMA dental resins composites resulted in enhancement in mechanical as well as biological properties for dental applications. CLINICAL SIGNIFICANCE: HNT/Ag containing dental composite is proposed to be highly valuable in the development of restorative dental material for patients with high risk of dental caries.

Formulation, Characterization and In-vitro and In-vivo Evaluation of Capecitabine Loaded Niosomes.

BACKGROUND: Nanocarriers improve the efficacy of drugs by facilitating their specific delivery and protecting them from external environment resulting in a better performance against diseases. OBJECTIVE: In this study, it was aimed to improve the efficacy of capecitabine against colorectal cancer by its entrapment in niosomes. Ether injection method was used to prepare niosomes composed of span 20 and cholesterol. METHODS: Niosomes were evaluated by evaluating the entrapment efficiency, in-vitro drug release and cytotoxicity of capecitabine loaded niosomes. Niosomes were characterized by particle size analysis, transmission electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry for surface morphology and drug excipient interactions. RESULTS: High encapsulation efficiency (90.55%) was observed, which is anticipated to resolve the multi-drug resistance problem. Reported particle size was 180.9 + 5 nm with a negative zeta potential - 21 + 0.5 mV and the kinetic study showed a concentration-dependent release of the drug from the niosome. DSC study proved entrapment of the entire drug and its non-covalent bonding with the excipients. Cytotoxicity study of niosomes on CaCO2 cell line showed an improved IC50 value as compared to the free drug. CONCLUSION: Enhanced cytotoxicity observed in the results further supports the suitability of niosome as a nanocarrier for pharmaceutical drug delivery.

Physicochemical and biological assessment of flowable resin composites incorporated with farnesol loaded halloysite nanotubes for dental applications.

The aim of this study was to fabricate flowable resin composites, by incorporating Farnesol loaded Halloysite Nanotubes (Fa-HNT) as a filler and evaluate their physicochemical as well as biological properties. Chemical and morphological characterization of antibacterial filler, Fa-HNT were performed using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), Transmission Electron Microscope (TEM), Scanning Electron Microscope (SEM). The antibacterial filler was mixed into composite material consisting of methacrylate monomers and dental glass fillers at concentrations of 1-20% (wt./wt.). It was observed that addition of mass fractions of Fa-HNT causes enhancement of compressive strength as well as flexural modulus of the composite. However, it significantly decreases flexural strength and degree of conversion. A significant antibacterial activity of dental composite was observed with increase in the area of zone of inhibition against the strains of Streptococcus mutans (S. mutans). There was no cytotoxicity observed by Fa-HNT resin composites on NIH-3T3 (mouse embryonic fibroblast cells) cell lines. A favourable integration of antibacterial filler with significant mechanical properties was achieved at concentrations from 7 to 13 wt% of Fa-HNT in dental composites, which is desirable in dentistry.