Hema Chaudhary

Mechanism of Action of Flavonoids as Anti-inflammatory Agents: A Review

Flavonoids are polyphenolic compounds that occur ubiquitously in plants having a variety of biological effects both in vitro and in vivo. They have been found to have antimicrobial, antiviral, anti-ulcerogenic, cytotoxic, anti-neoplastic, mutagenic, antioxidant, antihepatotoxic, antihypertensive, hypolipidemic, antiplatelet and anti-inflammatory activities. Flavonoids also have biochemical effects, which inhibit a number of enzymes such as aldose reductase, xanthine oxidase, phosphodiesterase, Ca(+2)-ATPase, lipoxygenase, cycloxygenase, etc. They also have a regulatory role on different hormones like estrogens, androgens and thyroid hormone. They have been found to have anti-inflammatory activity in both proliferative and exudative phases of inflammation. Several mechanisms of action have been proposed to explain anti-inflammatory action of flavonoids. The aim of the present review is to give an overview of the mechanism of action of potential anti-inflammatory flavonoids.

Chemical penetration enhancers: a patent review

Background: Ever since transdermal drug delivery came into existence, it has offered great promises, although most of them are yet to be fulfilled owing to some intrinsic restrictions of the transdermal route. On the positive side, transdermal drug delivery systems present advantages including non-invasiveness, prolonged therapeutic effect, reduced side effects, improved bioavailability, better patient compliance and easy termination of drug therapy. The greatest hindrance in the percutaneous delivery is the obstruction property of the stratum corneum, the outermost layer of the skin, in addition to usual problems such as skin binding, skin metabolism, cutaneous toxicity and prolonged lag times. Objective: This paper reviews investigations on the feasibility and application of penetration enhancers as described in recent patents, which help in the selection of a suitable sorption promoter(s) for enhanced delivery of medicaments through the skin. Method: The patents granted under various categories of penetration enhancers have been discussed including fatty acids, terpenes, fatty alcohol, pyrrolidone, sulfoxides, laurocapram, surface active agents, amides, amines, lecithin, polyols, quaternary ammonium compounds, silicones, alkanoates and so on. Conclusion: Scores of promising chemicals have been harnessed for their skin permeation promoting capacity as mentioned earlier. In future, many more chemicals and putative enhancers are likely be documented and patented.

Optimization and Formulation Design of Gels of Diclofenac and Curcumin for Transdermal Drug Delivery by Box-Behnken Statistical Design

The aim of this study was to develop and optimize a transdermal gel formulation for Diclofenac diethylamine (DDEA) and Curcumin (CRM). A 3-factor, 3-level Box-Behnken design was used to derive a second-order polynomial equation to construct contour plots for prediction of responses. Independent variables studied were the polymer concentration (X(1)), ethanol (X(2)) and propylene glycol (X(3)) and the levels of each factor were low, medium, and high. The dependent variables studied were the skin permeation rate of DDEA (Y(1)), skin permeation rate of CRM (Y(2)), and viscosity of the gels (Y(3)). Response surface plots were drawn, statistical validity of the polynomials was established to find the compositions of optimized formulation which was evaluated using the Franz-type diffusion cell. The permeation rate of DDEA increased proportionally with ethanol concentration but decreased with polymer concentration, whereas the permeation rate of CRM increased proportionally with polymer concentration. Gels showed a non-Fickian super case II (typical zero order) and non-Fickian diffusion release mechanism for DDEA and CRM, respectively. The design demonstrated the role of the derived polynomial equation and contour plots in predicting the values of dependent variables for the preparation and optimization of gel formulation for transdermal drug release.

Optimization and formulation design of carbopol loaded Piroxicam gel using novel penetration enhancers

The aim of the study was to develop and optimize Piroxicam transdermal gel formulation using three-factor, three-level Box-Behnken design by deriving a second-order polynomial equation to construct contour plots for prediction of responses as three selected independent variables with ratio of carbopol 974 (X1), ratio of propylene glycol (PG) (X2) and ratio of ethanol (X3). The dependent variables studied were the skin permeation rate of piroxicam (Y1), viscosity of the gel (Y2) and pH of the gel (Y3). Response surface plots were drawn, statistical validity of the polynomials was established to find the compositions of optimized formulation which was evaluated using the vertical Franz-type diffusion cell. The permeation rate of piroxicam increased proportionally with ethanol concentration but decreased with polymer concentration. The design demonstrated the role of the derived polynomial equation and contour plots in predicting the values of dependent variables for the preparation and optimization of gel formulation.

Nano-transfersomes as a novel carrier for transdermal delivery

The aim of this study was to design and optimize a nano-transfersomes of Diclofenac diethylamine (DDEA) and Curcumin (CRM). A 3(3) factorial design (Box-Behnken) was used to derive a polynomial equation (second order) to construct 2-D (contour) and 3-D (Response Surface) plots for prediction of responses. The ratio of lipid to surfactant (X1), weight of lipid to surfactant (X2) and sonication time (X3) (independent variables) and dependent variables [entrapment efficiency of DDEA (Y1), entrapment efficiency of CRM (Y2), effect on particle size (Y3), flux of DDEA (Y4), and flux of CRM (Y5)] were studied. The 2-D and 3-D plots were drawn and a statistical validity of the polynomials was established to find the compositions of optimized formulation. The design established the role of the derived polynomial equation, 2-D and 3-D plots in predicting the values of dependent variables for the preparation and optimization of nano-transfersomes for transdermal drug release.

Taguchi design for optimization and development of antibacterial drug-loaded PLGA nanoparticles.

This research report was to develop Cefixime loaded polylactide-co-glycolide (PLGA) nanoparticles using modified precipitation method. TEM analysis indicated formation of well-formed, smooth, spherical nanoparticles with no aggregates whereas XRD recommended dispersion of drug in PLGA carrier system in amorphous form. The polymer and stabilizer concentration and organic to aqueous ratio were found to be significant factors for nanoparticles and their optimization using Taguchi design (L9). The design formulations showed entrapment efficiency (EE), particle size and poly-dispersity index (PDI) ranging 68.31 ± 1.74%, 159.8-157.7 nm and 0.126-0.149, respectively indicated small and stable nanoparticles with good homogeneity and encapsulation. The design optimized formulation drug release and permeation studies demonstrated that it is four times sustained release behavior and 1.74 times better permeation than free drug. The result of microbiological assay also suggested that optimized formulation has significant antibacterial activity against intracellular multidrug resistance (MDR) of Salmonella typhi.

Effect of Physicochemical Properties of Biodegradable Polymers on Nano Drug Delivery

This review article is to explore the utilization of biodegradable polymers and their associated physicochemical properties in nano drug delivery (NDD). The main hub of the pharma industry is involved in the development of innovative biodegradable and biocompatible polymers which have targeting ability and a predictable release profile of an incorporated active pharmaceutical ingredient (API) or therapeutic agents. Moreover, the pharmaceutical and biological efficiency of the nano drug delivery system varies with the inherent properties of the polymer. The foremost, important physicochemical properties of biodegradable polymers include molecular weight, hydrophobicity, surface charge, crystallinity, composition of the co-polymer, glass transition temperature, and the nature of coating material. Nevertheless, these properties can be manipulated to modify the kinetics of the delivery system by selecting an optimum polymer (based on physicochemical properties) for a specific purpose.

Nano-Carrier for Accentuated Transdermal Drug Delivery

This research objective was to design a nano-carrier for Glibenclamide (GBD) by loading it in to nano-transfersomes to provide an accentuated transdermal drug delivery for Non-Insulin Dependent Diabetes Mellitus (NIDDM) The nanotransfersomes were prepared by sonication method and optimized using a statistically three-factor three-level Factorial Design (Box-Behnken design). A second order equation (polynomial) was originated and construct contour plots (2- D) for prediction the responses and characterized by various parameters (i.e. entrapment efficiency, vesicle shape & size, zeta potential, degree of deformability, permeation and skin irritation study). The skin permeation of optimized formulation (GNTs2) was found to be significantly higher (enhancement ratio is 10.44) than the drug in solution and also further confirmed by fluorescence microscopy using due i.e. Rhodamine B. Hence, drug loaded nano-transfersomes accentuates its transdermal flux and can be used as a nano-vehicle for NIDDM.

Optimization & design of isradipine loaded solid lipid nanobioparticles using rutin by Taguchi methodology.

Our research objective was to optimize and design nano-biosystem of Isradipine (IDP) via novel bioenhancer (Rutin) loaded solid-lipid nanobioparticles (ANbp) using Taguchi design (TgD) methodology. Firstly, preliminary screening of solid lipid nanoparticles (SLNps) formulation core factors (A, B & C; Lipoids, poly-acid, sonication time respectively at fixed dose of model drug were assessed on entrapment efficiency & particle size; R1 & R2) by performed experimentally of three factor three levels orthogonal L27 array. Consequently, signal to noise (S/N) ratio plot of responses were drawn to predict better quality fitted-levels of significant factor for eminence optimization. Further, optimized quality spaces composition was used via enhancer (Rutin) to design advanced bio-formulation (ANbp) and done its evaluation (entrapment efficiency, particle size, drug release & kinetics). As designed, ANbp results showed better sustained (86.54% as compared to control SLNps 94.48% in 24h) release, kinetics & stability behavior with good entrapment efficiency (97.58%) and desired smaller particle size (108nm). Therefore, statistically (TgD) optimization strategy would be considered to design nano-drug delivery system with bio-agent in-order to improve oral bioavailability of antihypertensive agents.

Radiopharmaceutical: Revolutionary Agents for Diagnosis

Radiopharmaceuticals play an imperative role in clinical nuclear medicine by providing a tool to better understand human disease and develop effective treatments. This is the base to use these radioactive substances in diagnosis. Radiopharmaceuticals are radioactive agents that consist of either a gamma or a positron-emitting radionuclide bound to ligands which have been used extensively in the field of nuclear medicine as non-invasive diagnostic imaging agents to provide both functional and structural information about organs and diseased tissues. Diagnostic radioactive pharmaceuticals can be used to examine blood flow to the brain, functioning to the liver, lungs, heart, kidneys, to assess bone growth and to confirm other diagnostic procedures. Another important use is to predict the effects of surgery and assess changes since treatment. They may be given to the patient in several ways, e.g. orally, parenterally, or placed into the eye or the bladder. Todays clinical practice of nuclear medicine revolves primarily around the use of systemically administered gamma- or positron-emitting radiopharmaceuticals as diagnostic tools for imaging the human body.