A novel and multifunctional excipient for vaginal drug delivery

The present study explores the pharmaceutical potential of a natural organic matter (fulvic acid) for sustained release, acid buffering capacity and mucoadhesion in vaginal drug delivery. The antifungal drug, Itraconazole, was first converted into inclusion complexes with fulvic acid (1:1 & 1:2 molar ratio) and then characterized by Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FT IR) and Mass Spectroscopy. Results were also authenticated by conformational analysis. Solubility analysis of complexes yielded different thermodynamic parameters and explained the driving force for solubilisation when the pH was varied in an acidic range. MTT assays were also performed to assess the potential in vitro cell toxicity of the complexes in comparison to the neat drug. The complexes were then formulated into tablets and optimized for hardness, mucoadhesion and release profiles. The optimized tablets presented with satisfactory mucoadhesion, acid buffering and spreading ability. Moreover, the antifungal activity of the formulation was also increased due to improved aqueous solubility of the drug despite the larger size of the complex. The study also indicated the potential use of fulvic acid as a functional excipient in the preparation of a vaginal drug delivery system (VDDS)

Development and validation of stability indicating liquid chromatographic (RP-HPLC) method for estimation of ubidecarenone in bulk drug and formulations using quality by design (QBD) approach

A novel, accurate, precise and economical stability indicating Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) method, was developed and validated for the quantitative determination of ubidecarenone (UDC) in bulk drug, UDC marketed formulation and UDC loaded cubosomes (CBMs) nanocarriers through Response surface methodology (RSM) design with three factors and three levels was performed to optimize the chromatographic variables followed by forced degradation studies of UDC were performed to detect degradation peak. RP-HPLC separation was achieved using mobile phase consisting of Acetonitrile:Tetrahydrofuran:Deionised water in the ratio 55:42:3 and a flow rate of 1.0 mL/min was optimized with a standard retention time (Rt) of 2.15 min, through experiment. The method was found linear in the concentration range of 5-100 µg/mL with a regression coefficient of 0.999. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 3.04 µg/mL and 9.11 µg/mL, respectively

Enhancement of oral bioavailability of doxorubicin through surface modified biodegradable polymeric nanoparticles

Abstract Background Doxorubicin hydrochloride (DOX·HCl), an anthracycline glycoside antibiotic, exhibits low oral bioavailability due to active efflux from intestinal P-glycoprotein receptors. The oral administration of DOX remains a challenge hence; no oral formulation for DOX is marketed, till date. Aim of the study To improve the oral bioavailability of DOX through, preparation of a nanoformulation i.e. PEGylated-doxorubicin(DOX)-loaded-poly-lactic-co-glycolic acid (PLGA)-Nanoparticles (NPs) and to develop and validate an ultra-high performance liquid chromatography electrospray ionization-synapt mass spectrometric bioanalytical method (UHPLC/ESI-QTOF–MS/MS) for plasma (Wistar rats) DOX quantification. Materials and methods For chromatography, Waters ACQUITY UPLC™ along with a BEH C-18 column (2.1 mm × 100 mm; 1.7 μm), mobile phase conditions (acetonitrile: 0.1% formic acid::1:1 v/v) and flow rate (0.20 ml/min) was used. For analyte recovery from rat plasma, a liquid–liquid extraction method (LLE), using Acetonitrile: 5 mM ammonium acetate in a ratio of 6:4 v/v at pH 3.5, was used. Results Nanoformulation with a particle size (183.10 ± 7.41 nm), zeta potential (− 13.10 ± 1.04 mV), drug content (42.69 ± 1.97 µg/mg) and a spherical shape and smooth surface was developed. An elution time of 1.61 and 1.75 min along with a transition at m/z 544.42/397.27 and 528.46/321.41 were observed for DOX and internal standard (IS) Daunorubicin, respectively. In addition, a linear dynamic range with r2 ≥ 0.9985 over a concentration range of 1.00–2500.0 ng/ml was observed for different processes and parameters used in the study. Similarly a marked improvement i.e. 6.8 fold was observed, in PEGylated-DOX-PLGA-NPs as compared to DOX-S, in pharmacokinetics studies. Conclusion The promising approach of PEGylated-DOX-PLGA-NPs may provide an alternate to intravenous therapy for better patient care

A novel and multifunctional excipient for vaginal drug delivery

The present study explores the pharmaceutical potential of a natural organic matter (fulvic acid) for sustained release, acid buffering capacity and mucoadhesion in vaginal drug delivery. The antifungal drug, Itraconazole, was first converted into inclusion complexes with fulvic acid (1:1 & 1:2 molar ratio) and then characterized by Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FT IR) and Mass Spectroscopy. Results were also authenticated by conformational analysis. Solubility analysis of complexes yielded different thermodynamic parameters and explained the driving force for solubilisation when the pH was varied in an acidic range. MTT assays were also performed to assess the potential in vitro cell toxicity of the complexes in comparison to the neat drug. The complexes were then formulated into tablets and optimized for hardness, mucoadhesion and release profiles. The optimized tablets presented with satisfactory mucoadhesion, acid buffering and spreading ability. Moreover, the antifungal activity of the formulation was also increased due to improved aqueous solubility of the drug despite the larger size of the complex. The study also indicated the potential use of fulvic acid as a functional excipient in the preparation of a vaginal drug delivery system (VDDS)

Gold nanoparticles in theranostic oncology: current state-of-the-art

INTRODUCTION: In recent years, extensive multidisciplinary investigations have been carried out in the area of cancer nanotechnology. Gold nanoparticles (GNPs) have emerged as promising carrier for delivery of various pay-loads into their target. In view of their unique physicochemical and optical properties, GNPs have been exploited for multimodality imaging, tumor targeting, and as transporter of various therapeutics. Additionally, GNPs have been used as photothermal therapeutics against cancer. AREAS COVERED: This review will focus on recent progress in the field of gold nanomaterials in cancer therapy and diagnosis. Moreover, concern about the toxicity of gold nanomaterials is addressed. EXPERT OPINION: GNPs present versatile scaffolds for efficient delivery of cancer chemotherapeutics. Tuneable chemistry of the GNPs contributes to their ever increasing use in oncology research. The promises of a functional cancer therapy using GNPs have been extensively demonstrated, although the materials are still in their infancy stage and not surfaced to meet clinical standards

Emerging advances in cancer nanotheranostics with graphene nanocomposites: opportunities and challenges

International audienceAs an inorganic nanomaterial, graphene nanocomposites have gained much attention in cancer nanotechnology compared with the other inorganic nanomaterial in recent times. Although a relatively new drug carrier, it has been extensively explored as a potential chemotherapeutic carrier and theranostic because of its numerous physicochemical properties, including, capability of multiple pay load, functionalization for drug targeting and photothermal effect. Despite potential benefit, its translation from bench to bed-side in cancer therapy is challenged due to its toxicity concern. Here, we discussed the present progress and future possibilities of graphene nanocomposites as a cancer theranostic. Moreover, the paper also exemplifies the effects of graphene/graphene oxide on tissues and organ functions in order to understand the extent and mechanism of toxicity