sushama talegaonkar | Jamia Hamdard (original) (raw)

Papers by sushama talegaonkar

Aaps Pharmscitech, Sep 9, 2009

Pharmaceutical Nanotechnology, 2019

Most of the active pharmaceutical ingredient used in the management of disease have poor water so... more Most of the active pharmaceutical ingredient used in the management of disease have poor water solubility and offer grueling problems in drug formulation development since low solubility is generally associated with poor dissolution characteristics which leads to poor oral bioavailability. The great challenge for the development of a pharmaceutical product is to create its new formulation and drug delivery system to limit solubility problems of existing drug candidate. Limited drug-loading capacity requires a large amount of carrier material to get appropriate encapsulation of the drug, which is another major challenge in the development of pharmaceutical product which could be resolved by developing nanocrystals (NCs). A significant research in the past few years has been done to develop NCs which helps in the delivery of poorly water soluble drugs via different routes. The technology could continue to thrive as a useful tool in pharmaceutical sciences for the improvement of drug s...

Pharmaceutics, 2019

While melanoma remains a challenge for oncologists, possibilities are being continuously explored... more While melanoma remains a challenge for oncologists, possibilities are being continuously explored to fight resistant metastatic melanoma more effectively. Eugenol is reported to inhibit survivin protein in breast cancer cells. Survivin is also overexpressed by melanoma cells, and is known to impart resistance to them against chemotherapy-induced apoptosis. To be able to fight resistant melanoma, we formulated hyaluronic acid (HA)-coated liposomes loaded with an effective combination of anti-melanoma agents (Dacarbazine and Eugenol), using a solvent injection method. Quality-by-Design (QbD) was applied to optimize and obtain a final formulation with the desired quality attributes, and within an acceptable size range. The optimized formulation was then subjected to performance analysis in cell lines. Coated-Dacarbazine Eugenol Liposomes were found to possess 95.08% cytotoxicity at a dacarbazine concentration of 0.5 µg/mL, while Dacarbazine Solution showed only 10.20% cytotoxicity at t...

European Journal of Pharmaceutics and Biopharmaceutics, 2007

Ramipril, potent anti-hypertensive agent has been used in the treatment of hypertensive disorders... more Ramipril, potent anti-hypertensive agent has been used in the treatment of hypertensive disorders. It has low bioavailability of 28-35% and short biological half-life (i.e. 2-4 hr). Thus this study attempts to evaluate chitosan-alginate nanoparticles as a novel drug delivery for Ramipril to sustain drug release and improve oral bioavailability. Nanoparticles were prepared by ionotropic pre-gelation technique using chitosan and sodium alginate polymers. Total nine formulations (F1 to F9) were prepared by varying the polymer concentrations. The nanoparticles were characterized for particle size, drug content, drug entrapment efficiency, zeta potential, surface morphology (TEM), percentage yield, in-vitro diffusion study, in-vivo bioavailability studies and stability studies. All prepared formulations were in the nanosize range of 190.5±6.15nm to 361.76±3.32 and with spherical morphology. The drug content and entrapment efficiency was found to maximum for F5 formulation, percentage yield was in the range of 53.72±2.04 to 77.91±0.565% which mainly depends upon polymer concentration. The zeta potential of optimised formulation F5 was found to be-34.2mV, showed good stability of nanoparticles during storage. The in-vitro drug release profile showed the suitability of nanoparticles for pH dependent and sustained release of Ramipril for prolonged time. Kinetic modelling revealed that the in-vitro drug release followed peppas model and non-fickian diffusion. From the in vivo studies it was predicted that oral bioavailability of Ramipril nanoparticles improved 2.17 times more than the pure drug. Stability studies carried out for optimized formulation F5 showed that the nanoparticles are more stable at 5±3°C.

Food Packaging, 2017

In this era of increasing demands and consequently improving technology, food packaging is not on... more In this era of increasing demands and consequently improving technology, food packaging is not only aimed to prevent food products from external dust and dirt particles, but also to perform several other functions, such as moisture control, oxygen scavenging, and a number of other actions including antimicrobial activity as well. But, with improving technology, which claims to fulfill most of the consumers’ requirements, health and environmental risks have been a major concern. Biodegradable polymers offer an environmental friendly alternative to these hazardous packaging materials. To impart active or smart properties to polymeric packaging films, polymers can be reinforced with nanomaterials. These so formed nanocomposites may exhibit one or more of the aforementioned properties of an active or smart packaging. This chapter deals with methods of preparation of polymeric nanocomposites, types and properties of nanoreinforcements, and details of few important biodegradable polymers that are commonly used for preparing nanocomposites for food packaging purposes. This chapter also gives an account of commercial active food packaging materials that are currently used in the market.

Nanoformulations in Human Health, 2020

A large majority of new chemical entities and many existing drug molecules exhibit poor aqueous s... more A large majority of new chemical entities and many existing drug molecules exhibit poor aqueous solubility, which may limit their potential use in developing drug formulations, with optimum bioavailability. One of the approaches to improve the solubility of a poorly water soluble drug and eventually its bioavailability is complexation with agents like humic acid (HA), fulvic acid (FA), β-cyclodextrin (β-CD), 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and caffeine (Caff). The current work emphasized at employing these agents to prepare different complexes and their in vitro/in vivo assessment. All the complexes evaluated for their complexation efficiency and authenticated by molecular modeling; conformational analysis, differential scanning calorimetry (DSC), X-ray diffraction (XRD), nuclear magnetic resonance (NMR) and mass spectroscopy. Furthermore, the complexes were assessed in an in vivo, rat vaginal model for their efficacy in treatment of vaginal candidiasis. Amongst the five tested complexes, fulvic acid-itraconazole complex yielded better solubility as well as in vivo efficacy and therefore may further be explored for developing a commercial formulation for treating vaginal candidiasis. Uniterms: Itraconazole/complexes/evaluation. Itraconazole/complexes/in vitro/in vivo performance. Vaginal candidiasis/treatment. Drugs/solubility. Drugs/formulation. A maioria das novas entidades químicas e muitas moléculas de fármacos existentes apresenta fraca solubilidade em água, o que pode limitar seu uso potencial no desenvolvimento de formulações com biodisponibilidade ideal. Uma das abordagens para melhorar a solubilidade de um fármaco pouco solúvel em água e, eventualmente, a sua biodisponibilidade é a complexação com agentes como o ácido húmico (HA), ácido fúlvico (FA), β-ciclodextrina (β-CD), 2-hidroxipropil-β-ciclodextrina (HP-β-CD) e cafeína (Caff). O presente trabalho baseia-se no uso desses agentes para preparar diferentes complexos e suas avaliações in vitro/in vivo. Todos os complexos foram avaliados quanto à eficiência de complexação por modelação molecular, análise conformacional, calorimetria de varredura diferencial (DSC), difração de raios-X (XRD), ressonância magnética nuclear (RMN) e espectroscopia de massas. Além disso, os complexos foram avaliados in vivo, em ratas, no tocante à sua eficácia no tratamento de candidíase vaginal. Entre os cinco complexos testados, o complexo de ácido fúlvico-itraconazol foi o que apresentou melhor solubilidade, bem como melhor eficácia in vivo e, portanto, pode ser explorado para o desenvolvimento de uma formulação comercial para o tratamento de candidíase vaginal. Unitermos: Itraconazol/complexos/avaliação. Itraconazol/complexos/desempenho in vitro/in vivo. Candidíase vaginal/tratamento. Fármacos/solubilidade. Fármacos/formulação. FIGURE 1-Molecular structure of itraconazole and different complexing agents (β-cyclodextrin, HP-β-cyclodextrin, caffeine, fulvic acid and humic acid)

The present investigation was aimed to establish a simple, accurate and highly sensitive validate... more The present investigation was aimed to establish a simple, accurate and highly sensitive validated stability-indicating liquid chromatographic method for imatinib mesylate. The purpose was to develop a method to detect nanogram quantity of the drug specific in development of nanoparticles. Imatinib mesylate was successfully analysed in a broad range from 50 to 50,000 ng/ml on Develosil® ODS-HG-5, Nomula chemical (50 mm×4.6 mm) analytical column, using 55:45 (v/v) aqueous (pH 8) to organic phase ratio (methanol and acetonitrile, 6:4) as the mobile phase, at a flow rate of 1.0 mL/min and detection at 267 nm with a good linearity (R2 > 0.9992). The method was validated for precision, accuracy, robustness, sensitivity and specificity. The method was further utilized to evaluate the fate of imatinib mesylate under various stress conditions including acid, alkaline, oxidation and photo degradation. The method was highly specific to determine pure drug from the degraded products. Further, it was inferred by the results that imatinib is less labile to alkaline and photo degradation.

International Journal of Drug Regulatory Affairs, 2018

Oral route is one of the most accepted and convenient mode of drug administration, however low or... more Oral route is one of the most accepted and convenient mode of drug administration, however low oral bioavailability of many drugs is a major concern which limits their oral administration. Optimum solubility and permeation of a drug across the intestinal epithelium is a prerequisite to reach the systematic circulation in the active form for effective action at the desired site. Physicochemical properties of the drug, physiological factors and pharmacokinetic factors are mainly responsible for their low solubility, low permeability and high metabolism which in turn into low oral bioavailability of the drug molecules. In this review, various factors which affect bioavailability of drugs and possible approaches to overcome this problem have been discussed. The review identifies various areas for research that can be focused for improving oral bioavailability of therapeutic molecules for different classes of drugs, thus making the oral route of administration of the drugs more effectiv...

Biomolecules, 2019

Wood-based cellulose nanofibrils (CNF) offer an excellent scaffold for drug-delivery formulation ... more Wood-based cellulose nanofibrils (CNF) offer an excellent scaffold for drug-delivery formulation development. However, toxicity and haemocompatibility of the drug carrier is always an important issue. In this study, toxicity-related issues of CNF were addressed. Different doses of CNF were orally administered to Drosophila and different tests like the developmental cycle, trypan blue exclusion assay, larva crawling assay, thermal sensitivity assay, cold sensitivity assay, larval light preference test, climbing behaviour, nitroblue tetrazolium (NBT) reduction assay, adult phenotype, and adult weight were conducted to observe the impact on its development and behaviour. A haemocompatibility assay was done on the blood taken from healthy Wistar rats. In Drosophila, the abnormalities in larval development and behaviour were observed in the behavioural assays. However, the cytotoxic effect could not be confirmed by the gut staining and level of reactive oxygen species. The larvae develop...

Drug Development and Industrial Pharmacy, 2019

To determine the phase of Calcium phosphate synthesized nanoparticles were subjected to EDS analy... more To determine the phase of Calcium phosphate synthesized nanoparticles were subjected to EDS analysis for elemental detection (Figure.3S).. The EDS spectra were recorded using an EDX system (X-act 10mm2 silicon drift detector, Oxford Instruments Plc, UK) coupled with the

Journal of cancer research and clinical oncology, Jan 9, 2018

Melanoma is the most serious form of skin cancer causing most of the skin cancer-related deaths. ... more Melanoma is the most serious form of skin cancer causing most of the skin cancer-related deaths. The incidence of melanoma has risen so dramatically over past few years that no other solid or blood malignancy comes close to it in terms of increased incidence. The main problem associated with the treatment of melanoma is low response rate to the existing treatment modalities, which in turn is due to the incomplete response by chemotherapeutic agents and inherent resistance of melanoma cells. Conventional therapeutic strategies, as well as, recent literature on melanoma have been thoroughly studied. This review summarizes the base of anti-melanoma treatment with conventional chemotherapeutic drugs, followed by an account of recent studies which explored the potential of nanotechnology and newer strategies and agents in melanoma treatment. Although melanoma is curable if detected in its early localized form, metastatic melanoma continues to be a therapeutic challenge. Metastatic melano...

Current Drug Delivery, 2018

Bendamustine HCl, an antineoplastic drug, has a very short life of about 40 minutes which necessi... more Bendamustine HCl, an antineoplastic drug, has a very short life of about 40 minutes which necessitates administration of large doses which leads to increased side effects as well as costs. The present work describes the fabrication, optimization, and evaluation of bioactive hydroxyapatite nanoparticles to achieve sustained delivery of bendamustine HCl. Hydroxyapatite nanoparticles (NPs) were prepared by the wet chemical precipitation method by reacting a calcium and phosphate precursor and the reaction was optimized via Box-Behnken DOE. The drug was loaded on particles by physical adsorption. Various analytical studies were performed on the fabricated nanoparticles in addition to biodistribution studies to establish the physicochemical and biological characteristics of the designed formulation. pH of the reactant solution was found to have a more profound effect on the particle size and size distribution in comparison to reactant concentration. The particles were found to have a spherical morphology by SEM. Size of the blank and drug-loaded nanoparticles was found to be 130±20 nm by TEM. Energy Dispersive X-ray Spectroscopy (EDS) studies confirmed the presence of hydroxyapatite as the dominant phase while DSC studies indicated the presence of the drug in its amorphous form after its adsorption on NPs. Tissue distribution studies further suggested that the majority of drug concentration was released in blood rather than the other organs implying low organ toxicity. Bendamustine loaded hydroxyapatite nanoparticles were successfully optimized and fabricated. Favorable results were obtained in in vitro, in vivo, and analytical studies.

Pharmaceutical research, Jan 5, 2018

The present investigation was aimed at developing Teriflunomide (TEF) and Methotrexate (MTX) load... more The present investigation was aimed at developing Teriflunomide (TEF) and Methotrexate (MTX) loaded hydroxyapatite nanoparticles and increasing tolerability towards combination therapy against rheumatoid arthritis by reducing hepatotoxicity. Drug-loaded HAp-NPs were synthesized by wet-chemical precipitation method and optimized by Box-Behnken experimental design. The developed NPs were subjected to in vitro and in vivo characterization. In-vivo pharmacodynamics and biochemical studies were performed on adjuvant- induced arthritis model treated with different formulations; MTX-TEF-SOL, TEF-HAp-NP, MTX-HAp-NP, TEF-MTX-HAp-NP, FOLITRAX-10 and AUBAGIO. The size of the optimized formulations, TEF-HAp-NP and MTX-HAp-NP, was found to be 224.3 ± 83.80 nm and 268.3 ± 73.86 nm with drug loading 53.11 ± 0.84% and 67.04 ± 1.12% respectively. In vitro release of TEF from TEF-HAp-NP (70.41 ± 1.22%) and MTX from MTX-HAp-NP (82.43 ± 1.31%) up to 24 h revealed sustained release pattern. Results of t...

Recent Patents on Inflammation & Allergy Drug Discovery, 2017

The CD44 receptor is a cell surface glycoprotein, which mediates many physiological and pathologi... more The CD44 receptor is a cell surface glycoprotein, which mediates many physiological and pathological activities. Its key role is to provide defence against inflammatory reactions by cellular transmigration and cell signalling. In pathological conditions, it gives destructive outcomes by mediating migration of pathogenic cells to vital organs resulting in tissue and organ damage. It binds to several ligands principally the hyaluronan. This review explores CD44 structure, functions, and its potential as a disease indicator and therapeutic target. From a thorough literature review on the CD44 receptor, several patents of targeting approaches have been identified and herewith reviewed which recommend CD44-binding proteins, CD44-binding antibodies, antibody fragments, pharmaceutical compositions, as well as nucleic acids as a targeting moiety. Applicability of CD44 overexpression and its targeting has now been extensively utilized in the disease diagnosis and real-time bio imaging of pathologic cells. A thorough understanding of CD44-receptor structure, expression and diverse functions towards different cell types would offer an opportunity to develop better therapeutic approaches in near future by overcoming all the shortcomings of toxicity and efficacy. The present review includes recent patents of CD44 receptor targeting approaches that have been presented in the different agencies: European (EP), US, and World Intellectual Property Organization (WIPO) and a general analysis of the future developments and trends in this emerging area.

Data in Brief, 2017

Currently, the third generation aromatase inhibitors are the drugs of choice for treatment of ear... more Currently, the third generation aromatase inhibitors are the drugs of choice for treatment of early and advanced breast cancer in postmenopausal women. The negative impact of these drugs on bone health is the significant limiting factor during this therapy. Here we report the effect of two aromatase inhibitors viz. letrozole and exemestane alone and in combination with raloxifene on lumbar vertebrae and femoral diaphysis after one month of treatment but no discernible effects were observed on bone when tested by micro CT and strength test except in trabecular number which was reduced in lumbar vertebrae following letrozole and exemestane. Further studies with letrozole and exemestane should be done at higher doses for longer duration of time to check whether effects are observed in other parameters as well. The data is an extension of our published work in Mol. Cell Endocrinology (A. Kalam, S. Talegaonkar, D. Vohora, 2017) [1] describing letrozole-induced bone loss on femoral epiphysis and its reversal by raloxifene.

Journal of Young Pharmacists, 2016

Objective: The present work aims to develop and validate stability indicating a novel liquid chro... more Objective: The present work aims to develop and validate stability indicating a novel liquid chromatography method with applicability i.e. to study the pharmacokinetics factor as well as estimate Tamoxifen (TMX) in bio-analytes, using Ultra High Pressure Liquid Chromatography/ Mass Spectrometry (UPLC-ESI-Q-TOF-MS/MS) in plasma. Methods: A bioanalytical method based on UPLC-ESI-Q-TOF-MS/MS has been developed and validated for the quantitative determination of TMX in female mice plasma using Clomiphine as an Internal Standard (IS). After Liquid-liquid extraction (LLE), analyte and IS, chromatographic separation was achieved on ACQUITY UPLC BEH C18 Waters column with dimensions; 100 mm × 2.1 mm; 1.7 µm, isocratic mobile phase (Acetonitrile:2 mM ammonium formate: 90:10; v/v), and a flow rate of 0.25 mL min-1. Results: The transitions occurred at m/z 372.1→178.1 and m/z 407.1 → 100.1 for TMX and IS, respectively. Liquidliquid extraction technique (LLE) using ethyl acetate was applied in order to optimize the recovery of analytes in mice plasma. The run and retention time of TMX were 6.0 and 2.63 minutes, respectively while the linear dynamic range established was 1.002-4001.07 ng/ml (r 2 >0.998 ± 0.0003). Intra-assay and inter-assay accuracy (% RSD) was found in the range; 2.43-3.49. Conclusion: The proposed LC-MS/MS assay method is simple, rapid and sensitive for the determination of TMX in mice plasma for pharmacokinetic studies. Analytes were stable under various conditions i.e. autosampler, freeze-thaw, at room temperature, and under deep freeze conditions.

Colloids and surfaces. B, Biointerfaces, Jan 17, 2016

The present work evaluates the synergistic anticancer efficacy of bioactive Hydroxyapatite (HA) n... more The present work evaluates the synergistic anticancer efficacy of bioactive Hydroxyapatite (HA) nanoparticles (HA NPs) loaded with Bendamustine HCl. Hydroxyapatite is a material with an excellent biological compatibility, a well-known fact which was also supported by the results of the Hemolytic studies and a high IC50 value observed in the MTT assay. HA NPs were prepared by the chemical precipitation method and loaded with the drug via physical adsorption. In-vitro release study was performed, which confirmed the sustained release of the drug from the drug loaded HA NPs. MTT assay, Cell Uptake and FACS studies on JURKAT E6.1 cell line and in-vivo pharmacokinetic studies in Wistar rats revealed that the drug loaded HA NPs could be easily internalized by the cells and release drug in a sustained manner. The drug loaded HA NPs showed cytotoxicity similar to the drug solution at 1/10th of the drug content, which indicates a possible synergism between the activity of the anticancer drug...

Structure and Chemistry, 2016

International Journal of Pharmaceutics, 2016

A stability analysis has also been carried out according to ICH guidelines (Q1AR2) and shelf life... more A stability analysis has also been carried out according to ICH guidelines (Q1AR2) and shelf life was found to be 1year and 4 months for the prepared formulation. Thus the results of present studies indicated that mPEG-PLGA-RIS-HA NPs has a great potential for sustained delivery of RIS for the treatment and prevention of osteoporosis and to minimize the adverse effects of RIS typically induced by its oral administration.