Search

A novel series of N-[(4-oxo-2-substituted aryl-1,3-thiazolidineimino)-propyl]-2-chlorophenothiazines 4a-j were synthesised from N-[(arylidene hydrazino)-propyl]-2-chlorophenothiazines 3a-j. All the compounds were characterised by spectral data and elemental analysis and were evaluated for their antimicrobial activity against pathogenic strains and antitubercular activity against Mycobacterium tuberculosis. The screening results indicated that some of these compounds demonstrated moderate to very good antimicrobial and antitubercular activities. Molecular docking studies predict that the molecules bind at the substrate active site with high binding affinity values. [ABSTRACT FROM AUTHOR]

Polymeric nanocarriers formulation technologies have provided the pharmaceutical industry with new strategies for resolving issues associated with poorly soluble molecules. For new chemical entities, the technology has been of value when used as a screening tool during preclinical efficacy and/or safety studies. "Go/no go" decisions can be made rapidly with a formulation approach that is scaleable and marketable. During development, robust nanoparticle formulations can be post-processed into various types of patient-friendly dosage forms that provide maximal drug exposure. For marketed products requiring life-cycle management opportunities, nanoparticle formulation strategies provide a means to incorporate an old drug into a new drugdelivery platform, thus opening new avenues for addressing unmet medical needs. For the future, it is most likely that the drug-nanoparticle approaches that have been developed in the past decade would be complemented with the many new approaches for drug targeting and permeation enhancement that have, until now, been primarily academic and a research curiosity. In recent study, we found that calculation and comparison of partial solubility parameters of polymer and drug could be used as a reliable means to predict which polymer is most suitable for development of a micelle based formulation for a specific drug. [ABSTRACT FROM AUTHOR]

Depression is estimated to affect nearly 340 million people worldwide and 18 million people in the US at any given time making it the third most costly and disabling illness in the US. Duloxetine hydrochloride is one of the main antidepressant used as a selective serotonin and norepinephrine reuptake inhibitor (SSNRI) for oral administration. As it works on central nervous system (CNS), drug should be more available to the cells. To increase the efficacy and solubility drug can be formulated with polymers using nanoparticle as a drug carriers. In this work we propose and analysed different approaches to study measuring the size of nanoparticle and effect of these nanoparticles on the in vitro kinetics dissolution behaviour. The drug obeyed the Beers law over the range of 5-50 μg/ml at λmax 230 nm. Mixture of PEG 4000/PVP 44000 in 6.8 phosphate buffer was proposed as good discriminative dissolution media for duloxitine hydrochloride delayed release formulation. The quantidation of drug release was studied by UV-spectrophotometer at 230 nm. Nanoparticle size and morphology were determined by Scanning electron microscopy (SEM) and Transmission electron microscopy (TEM). By fitting the dissolution data in various kinetic models it was found out that the delayed release formulation of duloxitine hydrochloride obeyed the Higuchi model kinetics having linearity range 0.99 and the release component 'n' obtained by the Korsmyer Pappas model indicated release mechanism followed by the anomalous diffusion process. [ABSTRACT FROM AUTHOR]

The objective of the present study was to develop, optimise, and evaluate Alendronateloaded chitosan nanoparticles (NPs) for the treatment of osteoporosis and drug release kinetic study by using different mathematical kinetic models. NPs were prepared by the ionic gelation method and optimised for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP) and pH effect on particle size, polydispersity index (PDI), zeta potential and entrapment efficiency. The prepared nanoparticles were characterised using particle size analyser (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM) and fourier-transform infrared spectroscopy (FTIR). Formulated NPs were obtained in the average size ranging from 60 to 220 nm in TEM, SEM and DLS studies. The release profile was dependent on the dissolution medium. The proposed nanoparticles offer an interesting alternative for alendronate delivery via the oral route. Our results indicated that alendronate-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis. [ABSTRACT FROM AUTHOR]

Two new allelochemicals (A) m.f. C35H44O23, m.p. 231-234oC [M+] 832 and (B) m.f. C33H40O21, m.p. 244-2460C, [M+] 772 have been isolated from ethanolic extract of the roots of plant Lagascea mollis Cav. along with two known compounds luteolin 7-O-β-D-glucopyranoside (C) and Isorhamentin (D). The structure of the two new allelochemicals have been characterised as 5,7,3'-trihydroxy-3,6,4'-trimethoxy flavone-5-O-β-D-glucopranosyl-7-O-α-L-rhamnopyranosyl(1→4)-O-α-L-arabinopyranoside (A) and 5, 7,3'5'-tetrahydroxy-3-methoxy flavone-7-O-β-D-galactopyranosyl-(1→4)-O-β-D-xylopyranosyl-5'-O-α-L-rahmnopyranoside (B) by various chemical degradations, colour reactions and spectral analysis. In this paper, the two new compounds A and B were screened against various bacteria and fungi and showed good results. Antioxidant activity of the two compounds A and B was evaluated by DPPH radical scavenging method. The result showed that both the compounds may be used as antioxidants agents. [ABSTRACT FROM AUTHOR]

Although the time that we live in is an age of creative technology and modernisation, infectious diseases, like Tuberculosis (TB), still remain to be one of the greatest health challenges worldwide. The objective of this study was to load first line antitubercular drug, isoniazid in chitosan nanoparticles in order to enhance its bioavailability and to reduce the dosing frequency. The isoniazid nanoparticles were prepared by ionic gelation method with addition of suitable polymer (chitosan) in acidic aqueous solution at various concentrations. The percentage yield obtained for the various formulations was 52-70%, which shows the suitability of ionic gelation technique for preparation of nanoparticles of isoniazid and the entrapment efficiency for the formulations F1-F5 was found to be in the range of 50-70% depending upon the polymer concentrations. It was observed that with an initial increase in polymer, i.e. chitosan concentration entrapment efficiency increases, however it dips as concentration of chitosan is increased further because of increased solution viscosity which decreases the loading capacity of nanoparticles. After the SEM studies, it was observed that the formulation F3 nanoparticles was the best being spherical and more regular in shape and size range between 124-220 nm. The F3 isoniazid nanoparticle formulation had a mean particle size of 1.81 nm and zeta potential (in mV) is 52.4. During the in vitro diffusion studies, it was observed that all the formulations show good control over the release of drug from the nanoparticles matrix. F3 formulation shows 87% drug release in 24 h. It was observed that F3 follows the Korsmeyer Peppas model (r2 value = 0.9864) indicating that the mechanism of drug release from the prepared F3 formulation is non-Fickian diffusion. [ABSTRACT FROM AUTHOR]

The development of Blood brain barrier (BBB) targeting technologies is a very active field of research and development. One goal is to develop chemically modified derivatives of central nervous system (CNS) drug (Alprazolam) chemically modified nanoparticulate of drugs, capable of crossing biological barriers, in particular the BBB. Nanocarrier drug delivery involves targeting CNS drugs enclosed in a particular PVP-44000 polymer. Drug nanoparticles have been shown to increase bioavailability and enhance drug exposure for oral and parenteral dosage forms. Nanoparticles of Alprazolam were prepared by nanoperception method. Polyvinylpyrrolidone (PVP) -44000 greatly enhanced the solubility of poorly water soluble drug, i.e. Alprazolam. Drug release follows zero order kinetics with Fickian diffusion. [ABSTRACT FROM AUTHOR]

The aim of the study was to develop and characterise raloxifene (RL-HCL)-loaded soy lecithin-chitosan (CS) nanoparticles (NPs) for the treatment of a commom bone disease osteoporosis. Raloxifene HCl is a poorly water soluble drug with poor bioavailability. Enhancement of the oral bioavailability of this drug was also the aim of our study. Biodegradable natural polymer chitosan and an anionic lipid soy lecithin were used to prepare raloxifene HCl-loaded hybrid nanoparticles for the efficient delivery of lipophilic drug raloxifene - HCl. The hybrid NPs were prepared by modified ionic interaction method and evaluated for particle size, zeta potential (ZP), entrapment efficiency and release kinetics study. The results indicated the NPs with the value of ZP to be +22.3 mV, particle sizes were in the range of 140-380 nm and the entrapment efficiency was 70.39%. The optimised formulation was prepared with CS: Soy lecithin ratio of 1:4 w/w and a stirring speed of 1500 rpm. The release study of drug for 45 h with 88.58% cumulative drug release and the optimised formulation showed the promising results of Ral-loaded SL-CS NPs. [ABSTRACT FROM AUTHOR]

Primaquine phosphate-loaded chitosan nanoparticles were prepared using the modified ionic gelation method. Chitosan is a naturally occurring biopolymer that can be easily functionalised to achieve desired outcomes. Chitosan nanoparticles are biodegradable, biocompatible, non-toxic and easily prepared. The different factors were studied in order to reveal their influence on the particle size, entrapment efficiency, zeta potential and in vitro release of the optimised nanoparticles such as the chitosan concentration and the amount of the crosslinker (TPP - sodium tri-polyphosphate). The primary focus of the study was concerned with the preparation of primaquine phosphate-loaded chitosan nanoparticles in order to improve drug tolerance and reduce the frequency of doses. Optimised nanoparticles were characterised for encapsulation efficiency using UV-vis. spectroscopy; particle size distribution, polydispersity index, and zeta potential using photon correlation spectroscopy; and in vitro drug release profile using UV-vis. spectroscopy. The sizes of nanoparticles of different formulation were 891, 152.3 and 233.8 nm, polydispersity index is 0.362, 0.272 and 0.188; encapsulation efficiency was 90, 95, and 97%, and zeta potential was 17.2, 22.3, and 34.2 mV, respectively. The in vitro release behaviour of the nanoparticles charged with the drug proved to follow a zero-order model. Ready nanoparticles were spherical and free-flowing. Infra-red (IR) spectra showed the stability of primaquine phosphate in optimised nanoparticles and the absence of drug-polymer interactions. Primaquine phosphate is a non-crystalline dispersion in chitosan nanoparticles, as determined by XRD results. [ABSTRACT FROM AUTHOR]

Alzheimer disease is the most common neurodegenerative disease of this century. It is associated with memory and cognitive impairment. There are two types of drugs approved by United State Food and Drug Administration (USFDA) for the treatment of Alzheimer's disease. The major problem with this disease is that the drugs are not able to cross Blood Brain Barrier effectively and higher dosage of the drug results several side effects such as vomiting, nausea, headache, etc. The aim of this work is to prepare Memantine-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles to reduce side effects. The approach of our research group is to improve drug transportation through the Blood Brain Barrier. The Memantine-loaded PLGA nanoparticles were prepared by modified nanoprecipitation method and characterised for Photo correlation spectroscopy (PCS) particle size distribution, Zeta potential, Entrapment efficiency. The average size and polydispersity index of polymeric nanoparticles was 83.7 nm and 0.328, respectively. The electron microscopic results of polymeric nanoparticles suggested that the particles are spherical in shape, smooth morphology and the preferred formulation follows the Hixson-Crowell model. The longer term clinical trial and attempts to increase their impact in treatment of anti-Alzheimer drug are highly needed. [ABSTRACT FROM AUTHOR]

Nowadays world is facing a severe global public health crisis pandemic COVID-19. Its symptoms are similar to common viral respiratory infections, i.e. cough cold, acute fever and difficulty in breathing. All countries have formulated guidelines, advisories and protocol for social distancing, diagnosis, and treatment according to the situation. Many countries have done the successful trials of Vaccine for this pandemic disease, while there is no effective medicine for all against COVID-19; it is advised to take preventive measures which boost our immunity in this time. Boosting the body's natural defence system (immunity) plays an important role in maintaining our optimum health. "The power of body which decreases the damaging power of the disease and stops the genesis of the disease is known as Immunity", this definition is according to the world's oldest healing (medicinal) system Indian Ayurveda. In human history medicinal plants have been applied for the treatment of many bacterial, viral and fungal diseases. These medicinal plants are used as modulators of the complex immune system because of the presence of the chemicals in the form of alkaloids, flavonoids, terpenoids, polysaccharides, lactones, and glycoside products, which are responsible to their immunomodulatory properties. In this article some commom immunomodulators are discussed which are prescribed for boosting immunity with special reference to respiratory health and helpful to protect against COVID-19. In current scenario when entire world is facing the greatest trouble due this viral infection, use of these specific immunomodulators can play an important role in fighting against COVID-19. [ABSTRACT FROM AUTHOR]

Nanotechnology is the study of extremely small structures, having size of 0.1 to 100 nm. Nanomedicine is a relatively new field of science and technology. Brief explanation of various types of pharmaceutical nanosystems is given. Classification of nanomaterials based on their dimensions is given. An application of nanotechnology in various fields such as health and medicine, electronics, energy and environment, is discussed in detail. Applications of nanoparticles in drug delivery, protein and peptide delivery, cancer are explained. Applications of various nanosystems in cancer therapy such as carbon nanotube, dendrimers, nanocrystal, nanowire, nanoshells, etc. are given. The advancement in nanotechnology helps in the treatment of neuro degenerative disorders such as the Parkinson's and Alzheimer's disease. Applications of nanotechnology in tuberculosis treatment, the clinical application of nanotechnology in operative dentistry, in ophthalmology, in surgery, visualisation, tissue engineering, antibiotic resistance, immune response are discussed in this article. Nanopharmaceuticals can be used to detect diseases at much earlier stages. [ABSTRACT FROM AUTHOR]

Tuberculosis (TB) is a preventable and curable disease, and its control is a highly cost-effective health intervention. However, diagnostic delay and inadequate treatment contribute to the severity and mortality of the disease as well as the risk of transmission and development of drug resistance. Despite the fact that TB disproportionately impacts low- and middle- income countries, it does not spare any country in the world including those in the European Union/European Economic Area where more than 4000 of people still die for the disease every year. The recent epidemic of COVID-19 highlights how a rapid spread of a serious epidemic could severely affect healthcare systems in the world. Shortages of Personal Protective Devices, mechanical ventilators, and worse, beds in intensive care units are a serious sign that health system cannot adapt rapidly to a health emergency. Risk factors associated with COVID-19, the viral pneumonia originating in Wuhan,China, in Dec 2019, require clarification so that medical resources can be prioritised for those at highest risk of severe COVID-19 complications. Infection with M. tuberculosis (MTB), the pathogen that causes TB and latently infects ~25% of the global population, may be a risk factor for SARS-CoV-2 infection and severe COVID-19 pneumonia. On the contrary, TB is a 'silent' epidemic. In this review both pandemics are compared to ensure that while tackling the new one (COVID-19) we should not forget the existing one (tuberculosis). [ABSTRACT FROM AUTHOR]

Malaria is an endemic disease caused by a protozoan parasite which is transmitted by female Anopheles mosquitoes around tropical and sub-tropical world. The main factor concerning the spreading of this disease is the increase in the number of drug-resistant parasites. To affect drug resistance, drug delivery systems for biodegradable polymers for the loading of anti-malarial drugs were developed. The formulated polymer loaded anti-malarial drugs nanoparticles are multifunctional features such as good biocompatibility, high percentage drug encapsulation, reduced drug toxicity, targeted drug, controlled release of therapeutic and diagnostic agents. Nanosize particles are expected to reduce the dose of the drug and kinetics of development of resistance in Parasite. Kinetics plays a key role in the study of what the body dose for a drug so these areas of study move towards pharmacokinetics. To evaluate the mechanism of drug release from the matrix tablet data obtained from the drug release studies were analysed according to zero order model, Higuchi model, and Korsmeyer-Peppas model, respectively. Thus obtained biodegradable polymer loaded drug nanoparticles were characterided by using DLS, Zeta analysis, SEM, TEM, AFM and identified by FT-IR, and UV-spectroscopy. In this review, we aim to provide insights into the design and improvement of targeted polymeric drug nanoparticles and to highlight the challenges correlate with the novel class of therapeutics, including the attention of nanoparticles design optimisation, improvement and biopharmaceutical properties. Additionally, we highlight some recent examples from the literature and novel concepts in both the design and use of targeted polymer loaded drug nanoparticles. [ABSTRACT FROM AUTHOR]

Alzheimer's disease is a neurodegenerative disease characterised by the presence of amyloid plaques and taupathies in the brain, which is the cause of dementia. At present only few drugs are approved by United State Food and Drug Administration (USFDA) for the treatment of the Alzheimer's disease. The drug delivery of these drugs should be such that they can cross blood brain barrier and be efficiently delivering the drug to the brain. This review paper is based on the concept of surface to size ratio and reports that establish a relation between drug bioavailability to the size of particles. It is evident that smaller the particle size more will be the surface area in turn more will be the catalytic activity and in this paper we review some important methods for the preparation and characterisation of anti-Alzheimer's drug loaded polymeric nanoparticles and the different mathematical models used to determine the kinetics of anti-Alzheimer's drug nano particles from drug delivery systems such as, zero order, first order, Hixson-Crowell, Higuchi, Korsemeyer-Peppas, etc. [ABSTRACT FROM AUTHOR]