Gulshan Bansal - Academia.edu (original) (raw)

Papers by Gulshan Bansal

A protein precipitation method was developed and optimized for extraction of pentazocine from hum... more A protein precipitation method was developed and optimized for extraction of pentazocine from human serum, and subsequently a direct spectrofluorimetric method was developed and validated for the determination of the extracted drug. The extraction efficiency of the precipitation method employing TCA (10%) and dioxan was excellent (95-102%). The working conditions of spectrofluorimeter were optimized for accurate and sensitive quantification of the drug by varying slit widths and instrumental sensitivities. The excitation and emission wavelength were found to be 284 and 311 nm respectively. The method was found sensitive (LOQ and LOD being 0.025 and 0.01 ppm, respectively) and linear in the concentration range of 0.025 n 2.5 ppm (with correlation coefficient 0.9999). The method was sufficiently precise (% RSD 95% with % RSD of 1 at each concentration indicating the method to be sufficiently accurate. The method can be employed for the quantification of pentazocine in human serum for ...

An isocratic stability-indicating reversed phase liquid chromatography (RP-HPLC-UV) method for qu... more An isocratic stability-indicating reversed phase liquid chromatography (RP-HPLC-UV) method for quantitative determination of tapentadol HCl has been developed and validated as per the ICH guidelines. Tapentadol..

The Pharma Innovation, 2020

Plants are the backbone of traditional systems of medicine and are also revered for their contrib... more Plants are the backbone of traditional systems of medicine and are also revered for their contribution to development of modern drugs. The therapeutic potential of plants depends on the quality and quantity of phytoconstituents present. Plant growth and the biosynthesis of plant metabolites are greatly influenced by biotic and abiotic factors. Scientific investigations have shown that various abiotic stresses including salt stress, flooding, drought, fertilization, shade, soil types etc. influence plant growth and formation of active constituents. Thus, optimization of abiotic stresses may help in increasing levels of plant metabolites and thus enhancing the bioactivity. The present review summarizes the importance of various abiotic stresses on plant growth and production of bioactive constituents. Literature shows that plants respond to abiotic stresses by modifying their morphology, physiology and phytochemical nature. Changes in plant growth and their bioactive metabolites are reported with alteration in abiotic stresses. This knowledge however is not translated to the fields during cultivation of valuable medicinal plants. From this review the authors conclude that, alteration of environmental factors during growth/cultivation of medicinal plants may ensure supply of plants with increased marker content which ensures better activity.

Journal of AOAC INTERNATIONAL, 2008

A forced degradation study on glibenclamide was performed under conditions of hydrolysis, oxidati... more A forced degradation study on glibenclamide was performed under conditions of hydrolysis, oxidation, dry heat, and photolysis and a high-performance column liquid chromatographic-ultraviolet (HPLC-UV) method was developed to study degradation behavior of the drug under the forced conditions. The degradation products formed under different forced conditions were characterized through isolation and subsequent infrared/nuclear magnetic resonance/mass spectral analyses, or through HPLC/mass spectrometric (HPLC/MS) studies. The drug degraded in 0.1 M HCl and water at 85C toamajor degradation product, 5-chloro-2-methoxy-N-2-(4-sulfamoylphenyl)ethyl]benzamide (III), and to a minor product, 1-cyclohexyl-3-[[4-(2-aminoethyl)-phenyl]sulfonyl]urea (IV). Upon prolonged heating in the acid, the minor product IV disappeared, resulting in formation of 5-chloro-2-methoxy-benzoic acid (II) and an unidentified product (I). Heating of the drug in 0.1 M NaOH at 85C yielded II and IV as the major produc...

Natural Product Research, 2019

Stability study on Gymnema sylvestre extract under WHO recommended accelerated and long-term cond... more Stability study on Gymnema sylvestre extract under WHO recommended accelerated and long-term conditions for 6 and 30 months, respectively was carried out by taking gymnemagenin as a marker and by evaluating antidiabetic activity through different models. Gymnemagenin was not detected in any stability sample indicating that gymnemic acids (GAs) remain stable in the extract under the test conditions. The extract and its GA rich fraction exhibited mild α-glucosidase inhibitory activity (18-27%) that remained intact during the study. Neither hypoglycemic nor anti-hyperglycemic effect was induced by the extract in normal rats in oral glucose tolerance test. The extract and GA rich fraction showed significant antidiabetic activity in alloxan-induced diabetic rats that remained intact in all stability samples. Based on these findings, a shelf-life of at least 30 months is suggested for G. sylvestre extract under long-term conditions, and gymnemagenin as a marker for shelf-life assessment of products derived from the plant.

Medicinal Research Reviews, 2019

Inducible nitric oxide synthase (iNOS), which is expressed in response to bacterial/proinflammato... more Inducible nitric oxide synthase (iNOS), which is expressed in response to bacterial/proinflammatory stimuli, generates nitric oxide (NO) that provides cytoprotection. Overexpression of iNOS increases the levels of NO, and this increased NO level is implicated in pathophysiology of complex multifactorial diseases like Parkinson's disease, Alzheimer's disease, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel disease. Selective inhibition of iNOS is an effective approach in treatment of such complex diseases. l‐Arginine, being a substrate for iNOS, is the natural lead to develop iNOS inhibitors. More than 200 research reports on development of nitric oxide synthase inhibitors by different research groups across the globe have appeared in literature so far. The first review on iNOS, in 2002, discussed the iNOS inhibitors under two classes that is, amino acid and non‐amino acid derivatives. Other review articles discussing specific chemical classes of iNOS inhibit...

Environmental science and pollution research international, Jan 23, 2018

Industrial and municipal solid wastes, noise, pesticides, fertilizers and vehicular emission are ... more Industrial and municipal solid wastes, noise, pesticides, fertilizers and vehicular emission are visible pollutants responsible for environmental contamination and ill-effects on health of all living systems. But, environmental contamination due to drugs or medicines used for different purposes in humans and animals goes unseen largely and can affect the health of living system severely. During the last few decades, the usage of drugs has increased drastically, resulting in increased drug load in soil and water. Contraceptive and fertility drugs are extensively and effectively used in humans as well as animals for different purposes. Usage of these reproductive drugs in humans is increased manifold to manage reproductive problems and/or for birth control with changing lifestyles. These drugs are excreted in urine and faeces as metabolite or conjugated forms, leading to contamination of water, milk and animal produce, which are consumed directly by humans as well as animals. These dr...

Medicinal Chemistry Research, 2017

Two series of novel derivatives have been designed by coupling medicinally important coumarin and... more Two series of novel derivatives have been designed by coupling medicinally important coumarin and benzimidazole nuclei through different linkers. These compounds have been predicted to be potent antiinflammatory and anthelmintic by in silico studies using PASS (prediction of activity spectra for substances) software. The compounds are synthesized and evaluated for the predicted activities as well as for their in vitro antioxidant potential. Compounds of first series (4a-4f) are found good to moderate anti-inflammatory agents. Among these, compounds 4b and 4f exhibited maximum anti-inflammatory activity (45% inhibition), which is equivalent to the activity of indomethacin (48% inhibition) after 3 h (peak inflammatory response time). Compounds of second series (5a-5f) exhibit anthelmintic activity. Amongst these, compound 5f has mortality activity marginally higher than albendazole (10-11 s). Compound 5e is found to be the most potent antioxidant with remarkable EC 50 value (0.08 µM/mL), which is though a little less than that of ascorbic acid (0.03 µM/mL). In addition, a comparative analysis of calculated Lipinski's parameters reveals that all test compounds have the propensity to be orally bioavailable. Based on these findings, compounds 4b, 4f, 5e, and 5f are identified as new leads to develop potent anti-inflammatory, anthelmintic, and antioxidant compounds.

Journal of AOAC INTERNATIONAL, 2017

The present work relates to the development and validation of reversed-phase HPLC–UV-photodiode a... more The present work relates to the development and validation of reversed-phase HPLC–UV-photodiode array methods for the estimation of two drugs in blood serum: dronedarone hydrochloride (DDN), a class III antiarrhythmic drug, and duloxetine hydrochloride (DLX), an antidepressant. Chromatographic analysis of DLX was carried out on a Nucleodur C18 column (250 × 4.6 mm, 5 μm) using ammonium acetate buffer (32 mM, pH 5.5) and acetonitrile (40 + 60, v/v; flow rate of 1.0 mL/min; detection wavelength of 290 nm) as the mobile phase. A Waters XTerra C18 column (250 × 4.6 mm, 5 μm) was used for the chromatographic analysis ofDDN using an acetonitrile–ammonium formate buffer (20 mM, pH 3.0, with formic acid; 45 + 55, v/v; flow rate 1.0 mL/min) as the mobile phase. Pentazocine and bupropion HCl were used as the internal reference standards for DLX and DDN, respectively. Excellent linearity was observed for DLX (r2 = 0.9996; concentration range 0.2–10.0 μg/mL) and DDN (r2 = 0.9997; concn. range 2...

Medicinal Plants - International Journal of Phytomedicines and Related Industries, 2015

Leaves of Nyctanthes arbor -tr istis have been traditionally used as anti-cancer drug, but there ... more Leaves of Nyctanthes arbor -tr istis have been traditionally used as anti-cancer drug, but there is no report to support this tradi tional claim. The present study is undertaken to establish the anti-cancer activi ty of the N. arbortristis, and to identify the most active anticancer fraction(s) f rom its different extracts. Leaves of N. arbor -tr istis were extracted with solvents of varied polari ty (toluene, chloroform, ethylacetate and aqueous ethanol (HA), and subsequently evaluated for their anti-cancer activity against HL60 cell lines using MTT assay method. The toluene and HA extracts were fractionated through column chromatography and successive solvent extractions, respectively. All extracts, except ethyl acetate extract, exhibited potent anti-cancer activity. Four fractions of the toluene extract were found maximal ly potent whereas the petroleum ether f raction of HA was found responsible for anti-cancer activity of HA extract. I t is concluded that the plant can serve as an excel lent source of potent and probably new anti-cancer lead(s), which can be further modif ied chemically to produce a series of compounds for development of potent and safe anti-cancer drugs.

Anti-Cancer Agents in Medicinal Chemistry, 2015

Journal of Pharmaceutical Analysis, 2015

Forced degradation study on doxorubicin (DOX) was carried out under hydrolytic condition in acidi... more Forced degradation study on doxorubicin (DOX) was carried out under hydrolytic condition in acidic, alkaline and neutral media at varied temperatures, as well as under peroxide, thermal and photolytic conditions in accordance with International Conference on Harmonization (ICH) guidelines Q1(R2). It was found extremely unstable to alkaline hydrolysis even at room temperature, unstable to acid hydrolysis at 80°C, and to oxidation at room temperature. It degraded to four products (O-I-O-IV) in oxidative condition, and to single product (A-I) in acid hydrolytic condition. These products were resolved on a C 8 (150 mm Â 4.6 mm, 5 mm) column with isocratic elution using mobile phase consisting of HCOONH 4 (10 mM, pH 2.5), acetonitrile and methanol (65:15:20, v/v/v). Liquid chromatography-photodiode array (LC-PDA) technique was used to ascertain the purity of the products noted in LC-UV chromatogram. For their characterization, a six stage mass fragmentation (MS 6) pattern of DOX was outlined through mass spectral studies in positive mode of electrospray ionization (þESI) as well as through accurate mass spectral data of DOX and the products generated through liquid chromatography-time of flight mass spectrometry (LC-MS-TOF) on degraded drug solutions. Based on it, O-I-O-IV were characterized as 3-hydroxy-9-desacetyldoxorubicin-9-hydroperoxide, 1-hydroxy-9-desacetyldoxorubicin-9-hydroperoxide, 9-desacetyldoxorubicin-9-hydroperoxide and 9-desacetyldoxorubicin, respectively, whereas A-I was characterized as deglucosaminyl doxorubicin. While A-I was found to be a pharmacopoeial impurity, all oxidative products were found to be new degradation impurities. The mechanisms and pathways of degradation of doxorubicin were outlined and discussed.

Journal of Acute Disease, 2014

To study acute and sub-acute toxicity study of Clerodendrum inerme (C. inerme), Jasminum mesnyi (... more To study acute and sub-acute toxicity study of Clerodendrum inerme (C. inerme), Jasminum mesnyi (J. mesnyi) Hance and Callistemon citrinus (C. citrinus). Methods: The acute toxicity test was conducted in Swiss albino mice. The extracts of C. inerme, J. mesnyi Hance and C. citrinus was administered in single dose of 0.5, 1.0, 2.0, 3.0, 4.0 and 5.0 g/kg and observed for behavioral changes and mortality, if any. In sub-acute toxicity study, Wistar rats of either sex were administered 1/5th of the maximum tolerated dose, p.o. for 4 weeks. Rats were observed weekly for any change in their body weight, food and water intake during 28 d of the treatment. At the end of 28 d, blood samples of the rats were collected for hematological and biochemical study. Results: In acute toxicity study, all four extracts of three plants were found to be well tolerated up to the dose of 2 000 mg/kg. These produced neither mortality nor any change in the behavior in mice. In sub-acute toxicity study, all four extracts of three plants at the LD 50 dose level did not produce any significant alteration in hematological and biochemical parameters in rats. Conclusions: The results demonstrated that there is a wide margin of safety for the therapeutic use of each of the four extracts of three plants. The findings also corroborated the traditional use of these extracts.

Acta Pharmaceutica Sinica B, 2014

Inspired from occurrence of anti-inflammatory activity of 3-substituted coumarins and antiulcer a... more Inspired from occurrence of anti-inflammatory activity of 3-substituted coumarins and antiulcer activity of various 2-substituted benzimidazoles, novel compounds have been designed by coupling coumarin derivatives at 3-position directly or through amide linkage with benzimidazole nucleus at 2-position. The resultant compounds are expected to exhibit both anti-inflammatory and antioxidant activities along with less gastric toxicity profile. Two series of coumarin-benzimidazole derivatives (4a-e and 5a-e) were synthesized and evaluated for anti-inflammatory activity and antioxidant activity. Compounds 4c, 4d and 5a displayed good anti-inflammatory (45.45%, 46.75% and 42.85% inhibition, respectively, versus 54.54% inhibition by indomethacin) and antioxidant (IC 50 of 19.7, 13.9 and 1.2 mmol/L, respectively, versus 23.4 mmol/L for butylatedhydroxytoluene) activities. Evaluation of ulcer index and in vivo biochemical estimations for oxidative stress revealed that compounds 4d and 5a remain safe on gastric mucosa and did not induce oxidative stress in tissues. Calculation of various molecular properties suggests the compounds to be sufficiently bioavailable.

Bioorganic & Medicinal Chemistry, 2014

Naturally occurring coumarins, having wide spectrum of activities such as antioxidant, antiinflam... more Naturally occurring coumarins, having wide spectrum of activities such as antioxidant, antiinflammatory, anticancer, MAO-B inhibitory and antimicrobial, are frequently used by the researchers to develop novel synthetic and semisynthetic coumarin based therapeutic agents. Many of these agents are hybrid molecules, which are designed through concept of molecular hybridization and have shown multiple pharmacological activities. This multifunctional attribute of these hybrid compounds makes them potential drug candidates for the treatment of multifactorial diseases such as cancer, Alzheimer's disease, metabolic syndromes, AIDS, malaria, and cardiovascular diseases. The present review compiles research reports on development of different coumarin hybrids, classify these on the basis of their therapeutic uses and propose structure-activity relationships. It is intended to help medicinal chemist in designing and synthesizing novel and potent hybrid compounds for the treatment of different disorders.

Medicinal Chemistry Research, 2012

Numerous research reports have indicated the coumarin nucleus as a potential candidate for develo... more Numerous research reports have indicated the coumarin nucleus as a potential candidate for development of anti-inflammatory drugs. Various phytoconstituents such as umbelliferone, scopoletin, columbiatnetin, visniadin, marmin, and many more derived from coumarin nucleus are found to have potent anti-inflammatory as well as antioxidant activities. A large number of coumarin derivatives have also been designed, synthesized, and evaluated to have mild-to-very potent anti-inflammatory activity through different mechanisms. However, despite the continuing efforts in search of these drugs, no major breakthrough has been achieved so far. In the present review, a critical analysis of various reports on naturally as well as the synthetically derived coumarin derivatives having anti-inflammatory activity has been carried out and a structural-activity relationship around the coumarin nucleus has been proposed to assist the medicinal chemists in rationally designing the anti-inflammatory drugs.

Medicinal Chemistry, 2014

A series of novel 2-substituted benzimidazole analogs has been designed and synthesized by connec... more A series of novel 2-substituted benzimidazole analogs has been designed and synthesized by connecting the benzimidazole nucleus with variedly substituted chalcone moieties through an amino linker. The designed analogs were predicted for their biological activity profile through the computer software PASS. The compounds were predicted to have potent anthelmintic activity. These were synthesized and the activity of each compound was evaluated experimentally at the concentrations of 0.1, 0.2, and 0.5 % in terms of mortality time and paralysis time for the helminthes. The experimentally observed activity was found to comply with the PASS predicted activity. All compounds showed dose-dependent activities. The compounds with an electron releasing group at the para position on phenyl ring in the chalcone moiety (8 and 9) were the most active in comparison to those bearing electron withdrawing groups. The corresponding ortho analogs (4 and 5) also revealed good paralytic and lethal activities. The higher activities of 8 and 9 may be attributed to the favorable electronic interactions of the electron releasing groups present at para position of the phenyl ring. Comparative analysis of the Lipinski's parameters and the activities of the compounds revealed all the compounds to comply with the Lipinski's rule of five. Further an optimum hydrophilicity and total polar surface area in the range of 65-80 of the molecule are required for the potent activity, but Molar refractance is not found to have any significant role in determining the anthelmintic activity.

Journal of Thermal Analysis and Calorimetry, 2014

Liposomes and niosomes are known to be efficient vehicles for localized and systemic delivery of ... more Liposomes and niosomes are known to be efficient vehicles for localized and systemic delivery of particularly lipophilic drugs resulting in their improved bioavailability, targeted delivery, and fewer side effects. These systems consist of bilayered membrane structures comprising amphiphilic molecules like phosphatidylcholine (liposomes) and nonionic surfactants (niosomes). Itraconazole (ITZ) is a widely used insoluble antifungal agent, which is known to be poorly absorbed from available marketed dosage forms. For countering the bioavailability related problem of oral ITZ products, vesicular systems like liposomes and niosomes could provide a rational approach. Drug–excipient interaction is being considered as an essential first step in development of any drug delivery system nowadays. Therefore, the present work describes the evaluation of drug–excipient interactions of ITZ with selected excipients used for development of liposomes and niosomes. Analytical techniques like differential scanning calorimetry, Fourier transform infrared spectroscopy, optical microcopy, and X-ray powder diffraction analysis were utilized for assessing the drug–excipient interactions. Isothermal stress testing was also performed to quantitatively measure the percent change in initial drug content from ITZ–excipient blends kept under stress conditions. The excipients included phospholipids (Phospholipon 90G®, Phospholipon 90H®), surfactants (Span 40 and Span 60), vesicular membrane stabilizer (cholesterol), and a solubilizer (3-hydroxypropyl-betacyclodextrin).

Journal of the Brazilian Chemical Society, 2011

Cinco produtos de degradação (I-V) do hidrobromidrato de citalopram (CTL) foram formados sob cond... more Cinco produtos de degradação (I-V) do hidrobromidrato de citalopram (CTL) foram formados sob condições diferentes de degradação forçada. Os produtos I e II foram formados sob condições hidrolíticas, enquanto que os produtos III-V sob condições fotolíticas. Os produtos II e IV foram encontrados como impurezas conhecidas, citalopram carboxamida e citolopram-N-óxido, respectivamente. O produto I foi encontrado como sendo uma nova impureza, que foi caracterizada como 3-hidroxicitalopram N-óxido. A droga e todos os cinco produtos de degradação foram resolvidos de uma maneira otimizada em uma coluna C 8 com fase móvel composta de acetonitrila e tampão acetato de amônia (pH* 4,5) na vazão de 0,50 mL min-1. O método foi linear, preciso com RSD < 3 (desvio padrão relativo) e exato com recuperação de 88-97% no intervalo de concentração 5-500 mg mL-1 de citalopram. Os limites de determinação (LOD) e de quantificação (LOQ) foram 1 mg mL-1 e 5 mg mL-1 , respectivamente. A análise por arranjo de fotodiodo de uma solução da droga degradada contendo a droga e todos os cinco produtos de degradação revelou picos isolados, puros. Sendo assim, o método pode ser sugerido como estável. Five degradation products (I-V) of citalopram hydrobromide (CTL) were formed under different forced degradation conditions. Products I and II were formed under hydrolytic conditions while product III-V were formed under photolytic conditions. Products II and IV were found known impurities as citalopram carboxamide and citalopram N-oxide, respectively. Product I was found to be a new impurity which was characterized as 3-hydroxycitalopram N-oxide. The drug and all five degradation products were optimally resolved on a C 8 column with mobile phase composed of acetonitrile and ammonium acetate buffer (pH* 4.5) flowing at a rate of 0.50 mL min-1. The method was linear, precise RSD < 3 (relative standard deviation) and accurate (recovery being 88-97%) in the concentration range of 5-500 mg mL-1 of citalopram. The limits of detection (LOD) and of quantitation (LOQ) were 1 mg mL-1 and 5 mg mL-1 , respectively. The photodiode array (PDA) analysis of the degraded CTL solution containing the CTL and all five degradation products revealed each peak to be pure. Hence, the method was suggested to be stability-indicating.

Journal of Pharmaceutical and Biomedical Analysis, 2008

Degradation products of glimepiride formed under different forced conditions have been characteri... more Degradation products of glimepiride formed under different forced conditions have been characterized through LC-UV-PDA and LC-MS studies. Glimepiride was subjected to forced decomposition under the conditions of hydrolysis, oxidation, dry heat and photolysis, in accordance with the ICH guideline Q1A(R2). The reaction solutions were chromatographed on reversed phase C8 (150 mm x 4.6mm i.d., 5 microm) analytical column. In total, five degradation products (I-V) were formed under various conditions. The drug degraded to products II and V under acid and neutral hydrolytic conditions while products I, III and IV were formed under the alkaline conditions. The products II and V were also observed on exposure of drug to peroxide. No additional degradation product was shown up under photolytic conditions. All the products, except I, could be characterized through LC-PDA analyses and study of MS fragmentation pattern in both +ESI and -ESI modes. Product I could not be identified, as it did not ionize under MS conditions. The products II, III and V matched, respectively, to impurity B (glimepiride sulfonamide), impurity J and impurity C (glimepiride urethane) listed in European Pharmacopoeia. The product IV was a new degradation product, characterized as [[4-[2-(N-carbamoyl)aminoethyl]phenyl]sulfonyl]-3-trans-(4-methylcyclohexyl) urea. The degradation pathway of the drug to products II-V is proposed, which is yet unreported.