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  1. Rocke J, Evans C, Kumar BN
    Med J Malaysia, 2021 08;76(Suppl 4):27-30.
    PMID: 34558554
    No abstract provided.
  2. Chu M, Gopikrishna D, Rocke J, Kumar BN
    Med J Malaysia, 2021 08;76(Suppl 4):9-13.
    PMID: 34558550
    INTRODUCTION: It is clear that a proportion of patients continue to suffer long-lasting symptoms following acute infection with coronavirus disease 2019 (COVID-19). Persistent olfactory dysfunction is one of the commonest complaints reported in the condition colloquially known as long COVID (now known as post-acute sequelae of SARS-CoV-2 infection (PASC)). The prevalence, risk factors and clinical course of long COVID olfactory dysfunction are not yet well understood. At present, the main stay of treatment is olfactory training. Quantitative olfactory testing and impacts on patient quality of life have not been widely studied. This study describes our experiences at Wrightington, Wigan and Leigh Teaching Hospitals, UK (WWL) of establishing a COVID-19 smell clinic, along with preliminary data on patient demographics, baseline smell test scores and quality of life questionnaire scores before olfactory training.

    METHODS: We piloted a COVID-19 smell clinic. We recorded patient demographics and clinical characteristics then performed clinical assessment of each patient. Quantitative measurements of olfactory dysfunction were recorded using the University of Pennsylvania Smell Identification Test (UPSIT). We measured the impact of olfactory dysfunction on patient quality of life using the validated English Olfactory Disorders Questionnaire (eODQ).

    RESULTS: 20 patients participated in the clinic. 4 patients were excluded from analysis due to missing data. Median age was 35 years. 81% (n=13) of the participants were female. 50% (n=8) of patients suffered with a combination of anosmia/ageusia and parosmia, whilst 43% (n=7) of patients suffered with anosmia/ageusia without parosmia. Almost all the patients registered UPSIT scores in keeping with impaired olfaction. Patient scores ranged from 22 to 35, with the median score at 30. All patients reported that their olfactory dysfunction had an impact on their quality of life. The median eODQ score reported was 90, with scores ranging from 42 to 169 out of a maximum of 180.

    CONCLUSION: We have demonstrated that it is simple and feasible to set up a COVID-19 smell clinic. The materials are inexpensive, but supervised completion of the UPSIT and eODQ is time-consuming. Patients demonstrate reduced olfaction on quantitative testing and experience significant impacts on their quality of life as a result. More research is needed to demonstrate if olfactory training results in measurable improvements in smell test scores and quality of life.

  3. Sajeev Kumar B, Saraswathi R, Dhanaraj SA
    J Young Pharm, 2013 Sep;5(3):83-9.
    PMID: 24396247 DOI: 10.1016/j.jyp.2013.08.002
    OBJECTIVE: The objective of the present study is to formulate and characterize the properties of complexed glimepiride nanocrystals (GLP) by various techniques at different stages of its development, and to study the effect of PEG 20000 and P90G on particle size reduction and stability of nanocrystals.

    METHOD: Precipitated (GLP-PEG) and complexed NCs (GLP-PEG-P90G) of glimepiride were characterized for particle size, size distribution, zeta potential and stability assessment using photon correlation spectroscopy (PCS). The crystallinity was analyzed using differential scanning calorimetry (DSC) and X-ray powder diffraction spectroscopy (XRPD). The surface morphology and chemical stability were assessed by means of scanning electron microscopy (SEM) and infrared spectroscopy (FTIR).

    RESULTS: A formulation with drug-polymer ratio of 1:1 was most ideal in developing stable NCs as it exhibited smaller particle size and high stability. A high zeta potential was observed in all NCs after complexation indicating improved stability. DSC and XRPD studies showed no change in crystallinity after complexation. SEM analysis of complexed NCs showed presence of spherical shape particles (size below 1 μm) with a lipid coat on the surface. Stability studies on optimized formulation (F1) revealed no change in particle size during 3-month period. FTIR studies prove that the chemical identity of GLP was preserved in the samples and the formulation was stable.

    CONCLUSION: Solid-state characterization studies reveal that complexed GLP NCs are promising carriers for drug delivery and they can be safely and effectively used in design of various formulations. Also, PEG 20000 and P90G are excellent polymer and lipid for particle size reduction (nanonization) and stabilization of nanocrystals.

  4. Velmurugan C, Sundaram T, Sampath Kumar R, Vivek B, Sheshadrishekar D, Ashok Kumar BS
    Med J Malaysia, 2011 Mar;66(1):22-6.
    PMID: 23765138
    The hypoglycemic and hypolipidemic effect of Ethanolic extract of Ougeinia oojeinensis (200mg/kg) bark was evaluated with measurements including, Body weight, blood glucose level, urine glucose and biochemical parameters. The ethanolic extracts of the powdered bark was tested for its efficacy in alloxan-induced diabetic rats. Animals were induced for diabetes with Alloxan (150 mg/kg of body weight- i.p.) and treated orally with Ethanolic extract of Ougeinia oojeinensis. The extracts were also evaluated for acute oral toxicity studies and its effect on different biochemical parameters. The extracts showed significant (p<0.01) antihyperglycemic and hypolipidemic activity as compared to diabetic control. The extract shows beneficial effects on blood glucose and urine glucose level. It also reduces the elevated biochemical parameters such as triglycerides (TGL), low density lipoprotein (LDL), very low density lipoprotein (VLDL), Total Cholesterol (TC) and increased the reduced level of high density lipoprotein (HDL) and body weight, which might be due to presence of steroids, tannins, alkaloids and triterpenoids present in that extract. Thus ethanolic extract could serve as good oral hypoglycemic agents and seems to be promising for the development of phytomedicines for diabetes mellitus.
  5. Tamilvanan S, Kumar BA, Senthilkumar SR, Baskar R, Sekharan TR
    AAPS PharmSciTech, 2010 Jun;11(2):904-9.
    PMID: 20496017 DOI: 10.1208/s12249-010-9455-3
    The objectives of the present work were to prepare castor oil-based nano-sized emulsion containing cationic droplets stabilized by poloxamer-chitosan emulgator film and to assess the kinetic stability of the prepared cationic emulsion after subjecting it to thermal processing and freeze-thaw cycling. Presence of cryoprotectants (5%, w/w, sucrose +5%, w/w, sorbitol) improved the stability of emulsions to droplet aggregation during freeze-thaw cycling. After storing the emulsion at 4 degrees C, 25 degrees C, and 37 degrees C over a period of up to 6 months, no significant change was noted in mean diameter of the dispersed oil droplets. However, the emulsion stored at the highest temperature did show a progressive decrease in the pH and zeta potential values, whereas the emulsion kept at the lowest temperatures did not. This indicates that at 37 degrees C, free fatty acids were formed from the castor oil, and consequently, the liberated free fatty acids were responsible for the reduction in the emulsion pH and zeta potential values. Thus, the injectable castor oil-based nano-sized emulsion could be useful for incorporating various active pharmaceutical ingredients that are in size from small molecular drugs to large macromolecules such as oligonucleotides.
  6. Gupta S, Mishra KP, Kumar B, Singh SB, Ganju L
    J Ethnopharmacol, 2020 Oct 28;261:113022.
    PMID: 32569719 DOI: 10.1016/j.jep.2020.113022
    ETHNOPHARMACOLOGICAL RELEVANCE: Traditional plant-derived medicines have enabled the mankind in curing the wide spectrum of diseases throughout the ages. Andrographis paniculata (Burm.f.) Nees, is one of the traditional plant used as a folk medicine for the management of inflammation, arthritis, viral-bacterial infections and other ailments in India, China, Malaysia and other South-East Asian countries. Its major bioactive compound; andrographolide, a diterpenoid, also exerts cytoprotective properties and is reported to be effective in neuroprotection, hepatoprotection, etc. AIM: The study is aimed to explore the role of andrographolide in treatment of complete freund's adjuvant (CFA) induced arthritis.

    MATERIALS AND METHODS: The influx of immune cells, release of pro-inflammatory cytokines and subsequent accumulation of synovial fluid (swelling) and pain manifest into the disease. The present study used CFA induced Balb/c mice model and treated them intraperitoneally with andrographolide and dexamethasone (used as a positive control) on alternate days for six days. After 6 days, blood and peritoneal macrophages were collected to evaluate the expression of various arthritic markers and paw edema was measured on all days.

    RESULTS: The in vitro and ex vivo experiments showed that andrographolide treated animal group had reduced paw edema, cell cytotoxicity and nitric oxide production than dexamethasone treated animal group. Further, the study revealed the mechanistic role of andrographolide in treatment of arthritis by suppressing battery of molecules like COX-2, NF-κB, p-p38, CD40, TNF-α, IL-1β and IL-6 involved in arthritis.

    CONCLUSION: The study showed the potent anti-arthritic effects of andrographolide and warrants further investigations on andrographolide for the development of safe and effective anti-arthritic drug.

  7. Chandirasekar R, Kumar BL, Jayakumar R, Uthayakumar V, Jacob R, Sasikala K
    Clin Chim Acta, 2015 Jan 15;439:77-83.
    PMID: 25307208 DOI: 10.1016/j.cca.2014.10.005
    BACKGROUND: Rheumatoid arthritis is the commonest inflammatory joint disease, affecting nearly 1% of the adult population worldwide. Early and accurate diagnosis and prognosis of rheumatoid arthritis (RA) have become increasingly important. In the present study, we aimed to elucidate the relationships between hematological, biochemical, immunological and cytogenetic parameters in rheumatoid arthritis patients and healthy normal controls.
    METHODS:The study group comprised of 126 RA patients and equal number of healthy normal control subjects. The blood wa s collected and analyzed for biochemical, immunological, enzymatic and cytogenetic parameters.
    RESULTS: Results of the present study indicated that 20% of RA patient's hematological, 31% of biochemical and 70% immunological parameters had a significant difference from the controls and reference range. The RF and anti-CCP antibody levels were also positive in 70% of RA patients. A significant increase in minor chromosomal abnormalities was also observed in patients as compared to controls.
    CONCLUSION: The knowledge about autoimmune diseases is very low among the South Indian population. The present study has thus helped in understanding the RA disease in a better way based on a pattern of various clinical markers of the disease condition which might help in planning therapeutic intervention strategies and create awareness about the disease management among RA patients of the population studied.
    KEYWORDS: Anti-cyclic citrullinated peptide (anti-CCP); Rheumatoid arthritis (RA); Rheumatoid factor (RF)
  8. Kumar B, Kumar L, Kumar A, Kumari R, Tagar U, Sassanelli C
    Environ Dev Sustain, 2023 May 17.
    PMID: 37362997 DOI: 10.1007/s10668-023-03361-3
    Developing markets are using sustainable development potential to reach zero-carbon goals. Due to the limitation of natural resources, companies need to use environmentally friendly manufacturing to develop a circular economy (CE). Green finance (GF) and the CE are linked in a systematic and complex approach; therefore, it was essential to employ the coupling coordination-level framework to explain their relationship and feedback. Any study linking green financing and CE together has been found. The objective of this research is to explore this twofold domain and determine its main characteristics. To address this objective, a comprehensive review of the literature was conducted, supplemented by a bibliometric analysis. The results confirm that GF has the potential to help society, sustainability, and the prevention to climate shifts, investing in the CE. There are many hurdles to overcome, including inadequate knowledge about CE and GF, ambiguous definitions, a lack of coherence between legal frameworks on CE and green financing, unclear laws, and a lack of financially viable motivation for investors and financial institutions that are ready to promote in sustainability. This study explores CE and GF domains. Managers may readily increase their understanding of methods, strategies, and technical solutions beneficial to assist their operations toward a green economy depending on various CE and GF elements. Finally, based on a categorization of GF types, the assessment identifies future investment potential consequences of green financing in the CE.
  9. Chandirasekar R, Kumar BL, Sasikala K, Jayakumar R, Suresh K, Venkatesan R, et al.
    PMID: 24769293 DOI: 10.1016/j.mrgentox.2014.04.007
    Inexpensive forms of tobacco are widely used in developing countries such as India. We have evaluated genotoxicity endpoints (chromosome aberrations, micronucleus frequency, comet assay) and polymorphisms of the XRCC1 and p53 genes among smokers and smokeless tobacco (SLT) users in rural Tamilnadu, South India. Cytogenetic, DNA damage and SNP analyses were performed on peripheral blood samples; micronucleus frequency was measured in peripheral blood and buccal mucosa exfoliated cells. Both categories of tobacco users had elevated levels of genotoxic damage. SNP analysis of tobacco users revealed that 17% carry the XRCC1 gln399gln genotype and 19% carry the p53 pro72pro genotype. Both genotypes are associated with increased risk of cancer.
  10. Kumar BS, Saraswathi R, Kumar KV, Jha SK, Venkates DP, Dhanaraj SA
    Drug Deliv, 2014 May;21(3):173-84.
    PMID: 24102185 DOI: 10.3109/10717544.2013.840690
    Novel LNCs (lipid nanocrystals) were developed with an aim to improve the solubility, stability and targeting efficiency of the model drug glibenclamide (GLB). PEG 20000, Tween 80 and soybean lecithin were used as polymer, surfactant and complexing agent, respectively. GLB nanocrystals (NCs) were prepared by precipitation process and complexed using hot and cold melt technique. The LNCs were evaluated by drug loading, saturation solubility (SL), optical clarity, in vitro dissolution, solid state characterization, in vivo and stability analysis. LNCs exhibited a threefold increase in SL and a higher dissolution rate than GLB. The percentage dissolution efficiency was found to decrease with increase in PEG 20000. The average particle size was in the range of 155-842 nm and zeta potential values tend to increase after complexation. X-ray powder diffractometry and differential scanning calorimetry results proved the crystallinity prevailed in the samples. Spherical shaped particles (<1000 nm) with a lipid coat on the surface were observed in scanning electron microscopy analysis. Fourier transform infrared results proved the absence of interaction between drug and polymer and stability study findings proved that LNCs were stable. In vivo study findings showed a decrease in drug concentration to pancreas in male Wistar rats. It can be concluded that LNCs are could offer enhanced solubility, dissolution rate and stability for poorly water soluble drugs. The targeting efficiency of LNCs was decreased and further membrane permeability studies ought to be carried out.
  11. Gupta M, Gulati M, Kapoor B, Kumar B, Kumar R, Kumar R, et al.
    J Ethnopharmacol, 2021 Jul 15;275:114115.
    PMID: 33852947 DOI: 10.1016/j.jep.2021.114115
    ETHNOPHARMACOLOGICAL RELEVANCE: Elaeagnus conferta Roxb. (Elaeagnaceae) is a subtropical shrub mainly native to India, Vietnam, Malaysia and South China, whose various parts are used for treatment of diabetes, gastric ulcers, pain, oxidative stress and pulmonary disorders. Though the other parts of the plant have been reported for their ethnic use i.e. fruits as astringent locally and for cancer systemically, leaves for body pain and flowers for pain in chest and the seeds are mentioned as edible, there is no report per se on the medicinal use of seeds. Based on the fact that seeds of closely resembling species i.e. Elaeagnus rhamnoides has demonstrated significant anti-gastroulcerative property, the probability of the seeds of E. conferta possessing similar activity seemed quite significant.

    AIM OF THE STUDY: Phytochemical investigation and assessment of pharmacological mechanism(s) involved in anti-ulcer effect of methanolic extract of the seeds of E. conferta.

    MATERIALS AND METHODS: Bioactive phytoconstituents were isolated by column chromatography. These were identified by spectroscopic techniques including infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) and mass spectrometry. Methanolic extract (MEC) of the seeds was prepared by cold maceration and its anti-ulcerogenic potential was evaluated using indomethacin (50 mg/kg) and water immersion stress models in male rats. The animals were pre-treated with different doses of MEC (400 and 800 mg/kg) and the therapeutic effect was compared with standard drug i.e. ranitidine (RANT; 50 mg/kg). The ameliorative effects of MEC were investigated on gastric juice pH, total acidity, free acidity and ulcer index. The assays of malionaldehyde (MDA), catalase (CAT), superoxide dismutase (SOD), glutathione (GSH) and pro-inflammatory cytokines i.e. interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α) were carried out to find out the possible mechanism(s) of protection. Further, histopathological changes were also studied.

    RESULTS: Chromatography studies and further confirmation by spectroscopic techniques revealed the presence of four different compounds in MEC i.e oleic acid (1), stearic acid (2), ascorbic acid (3) and quercetin (4). MEC exhibited anti-ulcerogenic effect in dose dependent manner which may be attributed to suppression of pro-inflammatory cytokines (IL-6, TNF-α) and MDA (112.7%), and up-regulation of protective factors such as CAT (90.48%), SOD (92.77%) and GSH (90.01%). Ulcer inhibition, reduction in total and free acidity and increase in gastric juice pH were observed in MEC treated rats as compared to disease control animals. Histopathological findings confirmed decreased cell infiltration, less epithelial cell damage and regeneration of gastric mucosa in dose dependent manner.

    CONCLUSIONS: The anti-ulcer effect of MEC may be attributed to its ability to scavenge free radicals and anti-inflammatory property via suppression of TNF-α and IL-6, thus offers a complete and holistic approach for management of peptic ulcer.

  12. Dash B, Rout SS, Lovaraju A, Charan Kumar B, Bharati A, Ganesh T, et al.
    Mar Pollut Bull, 2021 Oct;171:112775.
    PMID: 34375747 DOI: 10.1016/j.marpolbul.2021.112775
    The present study examines historical perspectives of the macrobenthic community in response to different phases of anthropogenic perturbations in Kakinada Bay, a tropical embayment on the east coast of India. Multivariate analysis of the snapshot data (1958-2017) revealed considerable changes in the Bay environment following a breakwater construction across the Bay mouth in 1997. Subsequently, port expansion activities, industrialization, urbanization, and geomorphic alterations in the Godavari delta brought deterrent changes in the Bay. The fluctuations over the years in hydrographical and sediment characteristics increased environmental heterogeneity and caused significant spatio-temporal shifts in the macrobenthic community between 1995-1996 and 2016-2017. The observed variabilities were suggestive of anthropogenic perturbations of the system with future repercussions on Bay ecosystem functioning. Overall, this study provides evidence on the long-term impact of anthropogenic activities on coastal marine communities and stresses the importance of macrobenthos as bioindicators of such changes in tropical systems.
  13. Kaur J, Gulati M, Gowthamarajan K, Vishwas S, Kumar Chellappan D, Gupta G, et al.
    Med Hypotheses, 2021 Sep 14;156:110679.
    PMID: 34555619 DOI: 10.1016/j.mehy.2021.110679
    Colon cancer is characterised by the persistent change in bowel habits due to the formation of polyps (cancerous) in the inner lining of the colon. Clinically, there are several anticancer drugs available to treat colon cancer. Oxaliplatin (third generation platinum drug) is widely prescribed anticancer drug due to its broad range anticancer properties and low toxicities over cisplatin and carboplatin. Currently, use of oxaliplatin as adjuvant chemotherapy represents a standard care for the treatment of advanced colon cancer. Despite this, its rapid degradation in systemic circulations upon administration, lack of tumor specificity, and low bioavailability limits its anticancer potential. On the other hand, vanillic acid (VA) has shown anticancer potential in colon cancer by targeting mTOR/Ras pathway, HIF-1α inhibition, NF-ĸB, and Nrf2 that regulate cell growth, cell survival, proliferation and adaptation to cancer microenvironment. Normal oral delivery of these two drugs offers non-specific drug release in gastrointestinal tract that leads to unwanted toxicity and very less amount of drug become available for colonic site. Therefore, loading of these two drugs in polysaccharide based functionalized polymeric micelles (FPMs) can offer selective targeting at colonic site and could offer better therapeutic efficacy at much lesser doses of drugs. Therefore, a new hypothesis has been proposed that the combination of vanillic acid with oxaliplatin co-loaded in FPMs could provide colon targeting ability with enhanced potency and safety profile by targeting multiple pathways than current adjuvant chemotherapies available in the market for the treatment of colon cancer.
  14. Girisha SK, Kushala KB, Nithin MS, Puneeth TG, Naveen Kumar BT, Vinay TN, et al.
    Transbound Emerg Dis, 2021 Mar;68(2):964-972.
    PMID: 33448668 DOI: 10.1111/tbed.13793
    Infectious spleen and kidney necrosis virus (ISKNV), a member of family iridoviridae, reported for the first time in a wide range of ornamental fish species in India. Significant mortalities during the year 2018-19 were reported from a number of retailers in the region with various clinical signs. The samples of moribund, dead and apparently healthy ornamental fishes were collected from retailers, located in three districts of Karnataka, India. Out of 140 fish samples, 16 samples (11.42%) representing 10 different fish species were found positive to ISKNV by OIE listed primers and same samples were reported to amplify the major capsid protein (MCP) gene of ISKNV. Further, sequence analysis of MCP gene showed that all strains detected in this study were closely related to other documented isolates from different countries with an identity ranging from 98.76% to 100%. Further, they clustered in the clade of ISKNV, during the phylogenetic analysis. The sequence similarity was high (99.94%) to ISKNV strains from Japan, Australia and Malaysia. This is the first report of an ISKNV infection in India. Moreover, out of 10 ISKNV-positive fish species, three species were reported positive to ISKNV for the first time in the world. Further, the in vitro experiment showed the growth of virus in Asian sea bass cell line, which is a natural host of ISKNV. Therefore, considering the lethal nature of megalocytiviruses to infect a vast range of species, proper biosecurity measures need to be taken to control these emerging pathogens.
  15. Mir MI, Hameeda B, Quadriya H, Kumar BK, Ilyas N, Kee Zuan AT, et al.
    Front Nutr, 2021;8:781764.
    PMID: 35096930 DOI: 10.3389/fnut.2021.781764
    A diverse group of rhizobacteria persists in the rhizospheric soil, on the surface of roots, or in association with rice plants. These bacteria colonize plant root systems, enhance plant growth and crop yield. Indigenous rhizobacteria are known to promote soil health, grain production quality and serve as sustainable bioinoculant. The present study was aimed to isolate, identify and characterize indigenous plant growth promoting (PGP) diazotrophic bacteria associated with the rhizosphere of rice fields from different areas of Jammu and Kashmir, India. A total of 15 bacteria were isolated and evaluated for various PGP traits, antagonistic activity against phytopathogens, production of hydrolytic enzymes and biofilm formation under in-vitro conditions. The majority of the isolated bacteria were Gram-negative. Out of 15 bacterial isolates, nine isolates produced IAA (12.24 ± 2.86 to 250.3 ± 1.15 μg/ml), 6 isolates exhibited phosphate solubilization activity (36.69 ± 1.63 to 312.4 ± 1.15 μg/ml), 7 isolates exhibited rock phosphate solubilization while 5 isolates solubilized zinc (10-18 mm), 7 isolates showed siderophore production, 8 isolates exhibited HCN production, 6 isolates exhibited aminocyclopropane-1-carboxylate (ACC) deaminase activity, 13 isolates exhibited cellulase activity, nine isolates exhibited amylase and lipase activity and six isolates exhibited chitinase activity. In addition, 5 isolates showed amplification with the nifH gene and showed a significant amount of nitrogenase activity in a range of 0.127-4.39 μmol C2H4/mg protein/h. Five isolates viz., IHK-1, IHK-3, IHK-13, IHK-15 and IHK-25 exhibited most PGP attributes and successfully limited the mycelial growth of Rhizoctonia solani and Fusarium oxysporum in-vitro. All the five bacterial isolates were identified based on morphological, biochemical and 16S rDNA gene sequencing study, as Stenotrophomonas maltophilia, Enterobacter sp., Bacillus sp., Ochrobactrum haematophilum and Pseudomonas aeruginosa. Rice plants developed from seeds inoculated with these PGP strains individually had considerably higher germination percentage, seed vigor index and total dry biomass when compared to control. These findings strongly imply that the PGP diazotrophic bacteria identified in this work could be employed as plant growth stimulators in rice.
  16. Corrie L, Kaur J, Awasthi A, Vishwas S, Gulati M, Saini S, et al.
    Pharmaceutics, 2022 Nov 06;14(11).
    PMID: 36365213 DOI: 10.3390/pharmaceutics14112395
    The study was initiated with two major purposes: investigating the role of isomalt (GIQ9) as a pharmaceutical carrier for solid self-nanoemulsifying drug delivery systems (S-SNEDDSs) and improving the oral bioavailability of lipophilic curcumin (CUN). GIQ9 has never been explored for solidification of liquid lipid-based nanoparticles such as a liquid isotropic mixture of a SNEDDS containing oil, surfactant and co-surfactant. The suitability of GIQ9 as a carrier was assessed by calculating the loading factor, flow and micromeritic properties. The S-SNEDDSs were prepared by surface adsorption technique. The formulation variables were optimized using central composite design (CCD). The optimized S-SNEDDS was evaluated for differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), microscopy, dissolution and pharmacokinetic studies. The S-SNEDDS showed a particle size, zeta potential and PDI of 97 nm, -26.8 mV and 0.354, respectively. The results of DSC, XRD, FTIR and microscopic studies revealed that the isotropic mixture was adsorbed onto the solid carrier. The L-SNEDDS and S-SNEDDS showed no significant difference in drug release, indicating no change upon solidification. The optimized S-SNEDDS showed 5.1-fold and 61.7-fold enhancement in dissolution rate and oral bioavailability as compared to the naïve curcumin. The overall outcomes of the study indicated the suitability of GIQ9 as a solid carrier for SNEDDSs.
  17. Faizan S, Wali AF, Talath S, Rehman MU, Sivamani Y, Nilugal KC, et al.
    Eur J Med Chem, 2024 Sep 05;275:116607.
    PMID: 38908102 DOI: 10.1016/j.ejmech.2024.116607
    Dihydropyrimidines are widely recognized for their diverse biological properties and are often synthesized by the Biginelli reactions. In this backdrop, a novel series of Biginelli dihydropyrimidines were designed, synthesized, purified, and analyzed by FT-IR, 1H NMR, 13C NMR, and mass spectrometry. Anticancer activity against MCF-7 breast cancer cells was evaluated as part of their cytotoxicity in comparison with the normal Vero cells. The cytotoxicity of dihydropyrimidines ranges from moderate to significant. Among the 38 dihydropyrimidines screened, compounds 16, 21, and 39 exhibited significant cytotoxicity. These 3 compounds were subjected to flow cytometry studies and EGFRwt Kinase inhibition assay using lapatinib as a standard. The study included evaluation for the inhibition of EGFR and HER2 expression at five different concentrations. At a concentration of 1000 nM compound 21 showed 98.51 % and 96.79 % inhibition of EGFR and HER2 expression. Moreover, compounds 16, 21 and 39 significantly inhibited EGFRwt activity with IC50 = 69.83, 37.21 and 76.79 nM, respectively. In addition, 3D-QSAR experiments were conducted to elucidate Structure activity relationships in a 3D grid space by comparing the experimental and predicted cytotoxic activities. Molecular docking studies were performed to validate the results by in silico method. All together, we developed a new series of Biginelli dihydropyrimidines as dual EGFR/HER2 inhibitors.
  18. Awasthi A, Gulati M, Kumar B, Kaur J, Vishwas S, Khursheed R, et al.
    Biomed Res Int, 2022;2022:1659338.
    PMID: 35832856 DOI: 10.1155/2022/1659338
    Diabetic wound (DW) is a secondary application of uncontrolled diabetes and affects about 42.2% of diabetics. If the disease is left untreated/uncontrolled, then it may further lead to amputation of organs. In recent years, huge research has been done in the area of wound dressing to have a better maintenance of DW. These include gauze, films, foams or, hydrocolloid-based dressings as well as polysaccharide- and polymer-based dressings. In recent years, scaffolds have played major role as biomaterial for wound dressing due to its tissue regeneration properties as well as fluid absorption capacity. These are three-dimensional polymeric structures formed from polymers that help in tissue rejuvenation. These offer a large surface area to volume ratio to allow cell adhesion and exudate absorbing capacity and antibacterial properties. They also offer a better retention as well as sustained release of drugs that are directly impregnated to the scaffolds or the ones that are loaded in nanocarriers that are impregnated onto scaffolds. The present review comprehensively describes the pathogenesis of DW, various dressings that are used so far for DW, the limitation of currently used wound dressings, role of scaffolds in topical delivery of drugs, materials used for scaffold fabrication, and application of various polymer-based scaffolds for treating DW.
  19. Sharma DS, Wadhwa S, Gulati M, Kumar B, Chitranshi N, Gupta VK, et al.
    Int J Biol Macromol, 2023 Jan 01;224:810-830.
    PMID: 36302483 DOI: 10.1016/j.ijbiomac.2022.10.168
    Diabetic retinopathy (DR) is one of the chronic complications of diabetes. It includes retinal blood vessels' damage. If untreated, it leads to loss of vision. The existing treatment strategies for DR are expensive, invasive, and need expertise during administration. Hence, there is a need to develop a non-invasive topical formulation that can penetrate deep to the posterior segment of retina and treat the damaged retinal vessels. In addition, it should also provide sustained release. In recent years, novel drug delivery systems (NDDS) have been explored for treating DR and found successful. In this study, chitosan (CS) modified 5-Fluorouracil Nanostructured Lipid Carriers (CS-5-FU-NLCs) were prepared by modified melt emulsification-ultrasonication method and optimized by Box-Behnken Design. The size, polydispersity index, zeta potential and entrapment efficiency of CS-5-FU-NLCs were 163.2 ± 2.3 nm, 0.28 ± 1.52, 21.4 ± 0.5 mV and 85.0 ± 0.2 %, respectively. The in vitro drug release and ex vivo permeation study confirmed higher and sustained drug release in CS-5-FU-NLCs as compared to 5-FU solution. HET-CAM Model ensured the non-irritant nature of CS-5-FU-NLCs. In vivo ocular studies of CS-5-FU-NLCs confirmed antiangiogenic effect of 5-FU by CAM model and diabetic retinopathy induced rat model, indicating successful delivery of 5-FU to the retina.
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