Displaying publications 1 - 20 of 36 in total

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  1. Lwin OM, Giribabu N, Kilari EK, Salleh N
    J Dermatolog Treat, 2021 Dec;32(8):1039-1048.
    PMID: 32013660 DOI: 10.1080/09546634.2020.1721419
    PURPOSE: This study identifies the potential use of mangiferin gel to promote wound healing in diabetes mellitus (DM).

    MATERIALS AND METHODS: Male rats were rendered diabetes mellitus via intraperitoneal injection of streptozotocin and nicotinamide. Following diabetes development, wound was created at the back of the neck. 1% and 2% mangiferin gel and 1% silver sulphurdiazine (SS) gel (positive control) were applied to the wound for twenty-one (21) days. Fasting blood glucose (FBG) levels were weekly monitored. At the end of the treatment, rats were sacrificed and wound was excised and subjected for histopathological and molecular biological analysis.

    RESULTS: No changes to serum FBG levels was noted throughout the period of mangiferin treatment. Albeit, a significant decrease in the size of the wound with increased in the skin thickness of surrounding the wound were observed. Increased expression and distribution of EGF, FGF, TGF-β, VEGF, PI3K, MMP and Nrf2 and decreased expression and distribution of TNFα and NF-κB p65 were observed in diabetic wound treated with topical mangiferin.

    CONCLUSIONS: Mangiferin has potential to be used as an agent to promote wound healing in diabetic condition.

    Matched MeSH terms: Niacinamide/therapeutic use
  2. Chellian J, Mak KK, Chellappan DK, Krishnappa P, Pichika MR
    Sci Rep, 2022 Dec 10;12(1):21393.
    PMID: 36496468 DOI: 10.1038/s41598-022-25739-5
    The antidiabetic effects of quercetin and metformin are well known. However, their synergistic effect in reversing the symptoms of diabetes-induced endothelial dysfunction remains unknown. In this study, we have investigated their synergistic effect in streptozotocin (STZ)-nicotinamide induced diabetic rats. Seventy-five rats were divided into five groups; normal control, diabetic control, treatment groups (10 mg/kg quercetin, 180 mg/kg metformin, and combined). The plasma glucose and lipid levels, liver enzymes, ex-vivo studies on aortic rings, histology of liver, kidney, pancreas, abdominal aorta and thoracic aorta, and immunohistochemical studies were carried out. The findings revealed that the combination of quercetin and metformin showed a greater antidiabetic effect than either drug, and rendered protection to the endothelium. The combination effectively reversed the hyperglycemia-induced endothelial dysfunction in diabetic rats. Furthermore, it also reversed the dysregulated expression of eNOS, 3-nitrotyrosine, VCAM-1, CD31 and SIRT-1. Overall, the present study's findings demonstrate that quercetin potentiates the activity of metformin to control the complications associated with diabetes.
    Matched MeSH terms: Niacinamide/metabolism
  3. Davoudi ET, bin-Noordin MI, Javar HA, Kadivar A, Sabeti B
    Pak J Pharm Sci, 2014 Jan;27(1):203-8.
    PMID: 24374450
    Cancer is among most important causes of death in recent decades. Whoever the renal cell carcinoma incidence is low but it seems it is more complicated than the other cancers in terms of pathophysiology and treatments. The purpose of this work is to provide an overview and also deeper insight to renal cell carcinoma and the steps which have been taken to reach more specific treatment and target therapy, in this type of cancer by developing most effective agents such as Sorafenib. To achieve this goal hundreds of research paper and published work has been overviewed and due to limitation of space in a paper just focus in most important points on renal cell carcinoma, treatment of RCC and clinical development of Sorafenib. The information presented this paper shows the advanced of human knowledge to provide more efficient drug in treatment of some complicated cancer such as RCC in promising much better future to fight killing disease.
    Matched MeSH terms: Niacinamide/analogs & derivatives*; Niacinamide/therapeutic use
  4. Bhullar M, Bhullar A, Arachchi NJ
    Ann Acad Med Singap, 2016 Oct;45(10):479-480.
    PMID: 27832225
    Matched MeSH terms: Niacinamide/adverse effects; Niacinamide/analogs & derivatives*
  5. Chia TS, Quah CK
    Acta Crystallogr B Struct Sci Cryst Eng Mater, 2017 Apr 01;73(Pt 2):285-295.
    PMID: 28362293 DOI: 10.1107/S2052520616019405
    Isonicotinamide-4-methoxybenzoic acid co-crystal (1), C6H6N2O·C8H8O3, is formed through slow evaporation from methanol solution and it undergoes a first-order isosymmetry (monoclinic I2/a ↔ monoclinic I2/a) structural phase transition at Tc= 142.5 (5) K, which has been confirmed by an abrupt jump of crystallographic interaxial angle β from variable-temperature single-crystal XRD and small heat hysteresis (6.25 K) in differential scanning calorimetry measurement. The three-dimensional X-ray crystal structures of (1) at the low-temperature phase (LTP) (100, 140 and 142 K) and the high-temperature phase (HTP) (143, 150, 200, 250 and 300 K) were solved and refined as a simple non-disordered model with final R[F2> 2σ(F2)] ≃ 0.05. The asymmetric unit of (1) consists of crystallographically independent 4-methoxybenzoic acid (A) and isonicotinamide (B) molecules in both enantiotropic phases. Molecule A adopts a `near-hydroxyl' conformation in which the hydroxyl and methoxy groups are positioned on the same side. Both `near-hydroxyl' and `near-carbonyl' molecular conformations possess minimum conformational energies with an energy difference of
    Matched MeSH terms: Niacinamide/chemistry*
  6. Eu-sen VO
    Med J Malaya, 1969 Sep;24(1):18-20.
    PMID: 4243836
    Matched MeSH terms: Niacinamide/therapeutic use
  7. Zolkeflee NKZ, Wong PL, Maulidiani M, Ramli NS, Azlan A, Mediani A, et al.
    Biochem Biophys Res Commun, 2024 May 14;708:149778.
    PMID: 38507867 DOI: 10.1016/j.bbrc.2024.149778
    The increasing prevalence of lean diabetes has prompted the generation of animal models that mimic metabolic disease in humans. This study aimed to determine the optimum streptozotocin-nicotinamide (STZ-NA) dosage ratio to elicit lean diabetic features in a rat model. It also used a proton nuclear magnetic resonance (1H NMR) urinary metabolomics approach to identify the metabolic effect of metformin treatment on this novel rat model. Three different STZ-NA dosage regimens (by body weight: Group A: 110 mg/kg NA and 45 mg/kg STZ; Group B: 180 mg/kg NA and 65 mg/kg STZ and Group C: 120 mg/kg NA and 60 mg/kg STZ) were administered to Sprague-Dawley rats along with oral metformin. Group A diabetic rats (A-DC) showed favorable serum biochemical analyses and a more positive response toward oral metformin administration relative to the other STZ-NA dosage ratio groups. Orthogonal partial least squares-discriminant analysis (OPLS-DA) revealed that glucose, citrate, pyruvate, hippurate, and methylnicotinamide differentiating the OPLS-DA of A-MTF rats (Group A diabetic rats treated with metformin) and A-DC model rats. Subsequent metabolic pathway analyses revealed that metformin treatment was associated with improvement in dysfunctions caused by STZ-NA induction, including carbohydrate metabolism, cofactor metabolism, and vitamin and amino acid metabolism. In conclusion, our results identify the best STZ-NA dosage ratio for a rat model to exhibit lean type 2 diabetic features with optimum sensitivity to metformin treatment. The data presented here could be informative to improve our understanding of non-obese diabetes in humans through the identification of possible activated metabolic pathways in the STZ-NA-induced diabetic rats model.
    Matched MeSH terms: Niacinamide/adverse effects
  8. Che Hamzah AM, Chew CH, Al-Trad EI, Puah SM, Chua KH, A Rahman NI, et al.
    Sci Rep, 2024 Feb 12;14(1):3485.
    PMID: 38347106 DOI: 10.1038/s41598-024-54182-x
    Despite the importance of methicillin-resistant Staphylococcus aureus (MRSA) as a priority nosocomial pathogen, the genome sequences of Malaysian MRSA isolates are currently limited to a small pool of samples. Here, we present the genome sequence analyses of 88 clinical MRSA isolates obtained from the main tertiary hospital in Terengganu, Malaysia in 2016-2020, to obtain in-depth insights into their characteristics. The EMRSA-15 (ST22-SCCmec IV) clone of the clonal complex 22 (CC22) lineage was predominant with a total of 61 (69.3%) isolates. Earlier reports from other Malaysian hospitals indicated the predominance of the ST239 clone, but only two (2.3%) isolates were identified in this study. Two Indian-origin clones, the Bengal Bay clone ST772-SCCmec V (n = 2) and ST672 (n = 10) were also detected, with most of the ST672 isolates obtained in 2020 (n = 7). Two new STs were found, with one isolate each, and were designated ST7879 and ST7883. From the core genome phylogenetic tree, the HSNZ MRSA isolates could be grouped into seven clades. Antimicrobial phenotype-genotype concordance was high (> 95%), indicating the accuracy of WGS in predicting most resistances. Majority of the MRSA isolates were found to harbor more than 10 virulence genes, demonstrating their pathogenic nature.
    Matched MeSH terms: Niacinamide/analogs & derivatives*
  9. Tan SC, Rajendran R, Bhattamisra SK, Krishnappa P, Davamani F, Chitra E, et al.
    J Pharm Pharmacol, 2023 Aug 01;75(8):1034-1045.
    PMID: 37402616 DOI: 10.1093/jpp/rgad063
    OBJECTIVES: Madecassoside (MAD) is a triterpenoid constituent of Centella asiatica (L.) Urb., an ethnomedical tropical plant, extracts of which were shown to reduce blood glucose in experimental diabetes. This study examines MAD for its anti-hyperglycaemic effects and tests the hypothesis that it reduces the blood glucose in experimentally induced diabetic rats by protecting the β-cells.

    METHODS: Diabetes was induced using streptozotocin (60 mg/kg, i.v.) followed by nicotinamide (210 mg/kg, intraperitoneal (i.p.)). MAD (50 mg/kg) was administered orally for 4 weeks, commencing 15 days after induction of diabetes; resveratrol (10 mg/kg) was used as a positive control. Fasting blood glucose, plasma insulin, HbA1c, liver and lipid parameters were measured, along with antioxidant enzymes and malondialdehyde as an index of lipid peroxidation; histological and immunohistochemical studies were also undertaken.

    KEY FINDINGS: MAD normalized the elevated fasting blood glucose levels. This was associated with increased plasma insulin concentrations. MAD alleviated oxidative stress by improving enzymatic antioxidants and reducing lipid peroxidation. Histopathological examination showed significant recovery of islet structural degeneration and an increased area of islets. Immunohistochemical staining showed increased insulin content in islets of MAD-treated rats.

    CONCLUSIONS: The results demonstrate an antidiabetic effect of MAD associated with preservation of β-cell structure and function.

    Matched MeSH terms: Niacinamide/pharmacology
  10. Chow PK, Poon DY, Khin MW, Singh H, Han HS, Goh AS, et al.
    PLoS One, 2014;9(3):e90909.
    PMID: 24614178 DOI: 10.1371/journal.pone.0090909
    The safety and tolerability of sequential radioembolization-sorafenib therapy is unknown. An open-label, single arm, investigator-initiated Phase II study (NCT0071279) was conducted at four Asia-Pacific centers to evaluate the safety and efficacy of sequential radioembolization-sorafenib in patients with hepatocellular carcinoma (HCC) not amenable to curative therapies.
    Matched MeSH terms: Niacinamide/adverse effects; Niacinamide/analogs & derivatives*; Niacinamide/therapeutic use
  11. Sampath Kumar NS, Sarbon NM, Rana SS, Chintagunta AD, Prathibha S, Ingilala SK, et al.
    AMB Express, 2021 Mar 01;11(1):36.
    PMID: 33646462 DOI: 10.1186/s13568-021-01194-9
    Psidium guajava L. (guava) is predominantly grown throughout the world and known for its medicinal properties in treating various diseases and disorders. The present work focuses on aqueous extraction of bioactive compounds from the guava leaf and its utilization in the formulation of jelly to improve the public health. The guava leaf extract has been used in the preparation of jelly with pectin (1.5 g), sugar (28 g) and lemon juice (2 mL). The prepared guava leaf extract jelly (GJ) and the control jelly (CJ, without extract) were subjected to proximate, nutritional and textural analyses besides determination of antioxidant and antimicrobial activities. GJ was found to contain carbohydrate (45.78 g/100 g), protein (3.0 g/100 g), vitamin C (6.15 mg/100 g), vitamin B3 (2.90 mg/100 g) and energy (120.6 kcal). Further, the texture analysis of CJ and GJ indicated that both the jellies showed similar properties emphasizing that the addition of guava leaf extract does not bring any change in the texture properties of jelly. GJ exhibited antimicrobial activity against various bacteria ranging from 11.4 to 13.6 mm. Similarly, GJ showed antioxidant activity of 42.38% against DPPH radical and 33.45% against hydroxyl radical. Mass spectroscopic analysis of aqueous extract confirmed the presence of esculin, quercetin, gallocatechin, 3-sinapoylquinic acid, gallic acid, citric acid and ellagic acid which are responsible for antioxidant and antimicrobial properties.
    Matched MeSH terms: Niacinamide
  12. Zarina Thasneem Zainudeen, Ilie Fadzilah Hashim, Intan Juliana Abd Hamid
    MyJurnal
    Chronic granulomatous disease (CGD) is defined as an inherited phagocyte disorder causing defective superoxide generation and intracellular killing. Reduced or missing burst activity of nicotinamide dinucleotide phosphate (NADPH) oxide complex is observed in this inborn defect that usually manifests itself during the first two years of life. It can be inherited either by X-linked inheritance or autosomal recessive inheritance. Most patients with CGD develop failure to thrive, severe bacterial adenitis, abscesses, osteomyelitis or hyperinflammaory manifestations. (Copied from article).
    Matched MeSH terms: Niacinamide
  13. Suraiami, M., Mohd Fairulnizal, M.N., Norhayati, M.K., Zaiton, A., Norliza, A.H., Wan Syuriahti, W.Z., et al.
    Malays J Nutr, 2014;20(3):417-427.
    MyJurnal
    Introduction: This study aimed to determine the nutrient content of cornflakes and muesli, ready-to-eat cereal products available in the Malaysian market. Cornflakes and muesli were chosen due to their popularity as a breakfast meal especially in urban areas. Methods: A total of six brands each for cornflakes and muesli were purchased from supermarkets in the Klang Valley using stratified random sampling. All samples were analysed using AOAC official methods of analysis. The validity of the test data was monitored with the application of internal quality controls in line with the requirements of ISO 17025. Results: Proximate analysis revealed significantly higher mean levels of carbohydrate (86.94 ± 0.59 mg/lOOg), minerals such as iron (8.48±1.72 mg/lOOg) and sodium (674.83±102.99 g/lOOg), B3 as niacinamide (25.87 ± 6.14 g/lOOg) and sucrose (5.10 ± 0.90 mg/lOOg) in cornflakes than in muesli. However, muesli contained significantly more mean moisture (10.23 ± 0.72 mg/lOOg), protein (10.07 ± 0.79 mg/lOOg), total dietary fibre (12.49 ± 1.44 mg/lOOg), magnesium (113.22 ± 7.93 mg/lOOg), zinc (1.65 ± 0.16 mg/lOOg), copper (0.25 ± 0.02 mg/lOOg), total sugar (18.75 ± 2.05 mg/lOOg), glucose (7.70±1.77 mg/lOOg) and fructose (8.68±1.76 mg/lOOg) than cornflakes. Most of the fatty acids analysed were not detected or of low value in both the cereal products. Conclusion: The nutrient analysis of cornflakes and muesli suggests that both ready-to-eat cereals are nutritionally good choice as breakfast for consumers as it provides carbohydrate, minerals, fibre and vitamins. The data provides additional information to the Malaysian Food Composition Database.
    Matched MeSH terms: Niacinamide
  14. Wang Y, Molin DG, Sevrin C, Grandfils C, van den Akker NM, Gagliardi M, et al.
    Int J Pharm, 2016 Apr 30;503(1-2):150-62.
    PMID: 26965198 DOI: 10.1016/j.ijpharm.2016.03.002
    Poly(d,l-lactic acid) biodegradable microspheres, loaded with the drugs cisplatin and/or sorafenib tosylate, were prepared, characterized and studied. Degradation of the microspheres, and release of cisplatin and/or sorafenib tosylate from them, were investigated in detail. Incubation of the drug-carrying microspheres in phosphate buffered saline (pH=7.4) revealed slow degradation. Nevertheless, significant release of cisplatin and sorafenib tosylate from microspheres loaded with both drugs was apparent in vitro; this can be attributed to their porous structure. Supernatants from microspheres loaded with both drugs showed strong toxic effects on cells (i.e. endothelial cells, fibroblast cells and Renca tumor cells) and potent anti-angiogenic effect in the matrigel endothelial tube assay. In vivo anti-tumor effects of the microspheres were also observed, in a Renca tumor mouse model. The poly(d,l-lactic acid) microspheres containing both cisplatin and sorafenib tosylate revealed highest therapeutic efficacy, probably demonstrating that combined local administration of cisplatin and sorafenib tosylate synergistically inhibits tumor growth in situ. In conclusion, this study demonstrates the applicability of biodegradable poly(d,l-lactic acid) microspheres loaded with cisplatin and sorafenib tosylate for local drug delivery as well as the potential of these microspheres for future use in transarterial chemoembolization.
    Matched MeSH terms: Niacinamide
  15. Giribabu N, Roslan J, Rekha SS, Salleh N
    Int J Cardiol, 2016 Nov 01;222:850-65.
    PMID: 27522389 DOI: 10.1016/j.ijcard.2016.07.250
    BACKGROUND: We hypothesized that consumption of Vitis vinifera seed by diabetics could help to ameliorate myocardial damage. Therefore, in this study, we investigated effects of V. vinifera seed methanolic extract (VVSME) on parameters related to myocardial damage in diabetes with or without myocardial infarction (MI).

    METHODS: Streptozotocin-nicotinamide induced diabetic rats received oral VVSME for 28days. MI was induced by intraperitoneal injection of isoproterenol on last two days. Prior to sacrifice, blood was collected and fasting blood glucose (FBG), glycated hemoglobin (HbA1c), lipid profile and insulin levels were measured. Levels of serum cardiac injury marker (troponin-I and CK-MB) were determined and histopathological changes in the heart were observed following harvesting. Levels of oxidative stress (LPO, SOD, CAT, GPx and RAGE), inflammation (NF-κB, TNF-α, IL-1β and IL-6) and cardiac ATPases (Na(+)/K(+)-ATPase and Ca(2+)-ATPase) were determined in heart homogenates. LC-MS was used to identify constituents in the extracts.

    RESULTS: Consumption of VVSME by diabetic rats with or without MI improved the metabolic profiles while decreased the cardiac injury marker levels with lesser myocardial damage observed. Additionally, VVSME consumption reduced the levels of LPO, RAGE, TNF-α, Iκκβ, NF-κβ, IL-1β and IL-6 while increased the levels of SOD, CAT, GPx, Na(+)/K(+)-ATPase and Ca(2+)-ATPase in the infarcted and non-infarcted heart of diabetic rats (p<0.05). LC-MS analysis revealed 17 major compounds in VVSME which might be responsible for the observed effects.

    CONCLUSIONS: Consumption of VVSME by diabetics helps to ameliorate damage to the infarcted and non-infarcted myocardium by decreasing oxidative stress, inflammation and cardiac ATPases dysfunctions.

    Matched MeSH terms: Niacinamide/toxicity
  16. Marafi F, Sasikumar A, Aldaas M, Esmail A
    Clin Nucl Med, 2021 Jan;46(1):e65-e67.
    PMID: 33181733 DOI: 10.1097/RLU.0000000000003354
    A 46-year-old man with end-stage renal disease and renal cell carcinoma underwent F-FDG PET/CT for initial staging followed by F-PSMA-1007 PET/CT. Unlike F-FDG, which undergoes renal clearance, F-PSMA-1007 undergoes hepatobiliary clearance and thus generates superior quality images. F-PSMA-1007 PET/CT showed intense tracer-avid left renal mass lesion (FDG nonavid); lytic bone lesions (FDG avid) and single liver lesion (FDG nonavid). This case highlights the superiority of F-PSMA-1007 over F-FDG PET/CT in identifying primary lesion as well as metastatic sites in case of renal cell carcinoma even in the presence of end-stage renal disease.
    Matched MeSH terms: Niacinamide/analogs & derivatives*
  17. Vattam KK, Raghavendran H, Murali MR, Savatey H, Kamarul T
    Hum Exp Toxicol, 2016 Aug;35(8):893-901.
    PMID: 26429928 DOI: 10.1177/0960327115608246
    In the present study, thirty six male Sprague Dawley rats were randomly divided into six groups and were injected with varying doses of alloxan (Ax) and nicotinamide (NA). The serum levels of glucose, insulin, and adiponectin were measured weekly up to 4 weeks.
    Matched MeSH terms: Niacinamide/administration & dosage; Niacinamide/toxicity*
  18. Panda BP, Krishnamoorthy R, Bhattamisra SK, Shivashekaregowda NKH, Seng LB, Patnaik S
    Sci Rep, 2019 11 22;9(1):17331.
    PMID: 31758056 DOI: 10.1038/s41598-019-53996-4
    Drug delivery and therapeutic challenges of gliclazide, a BCS class II drug used in type 2 diabetes mellitus (T2DM) can be overcome by exploring smarter carriers of second-generation nanocrystals (SGNCs). A combined method of emulsion diffusion, high-pressure homogenization and solvent evaporation method were employed in the preparation of gliclazide loaded poly (D, L-lactide-co-glycolide) (PLGA) SGNCs. Taguchi experimental design was adopted in fabrication of Gliclazide SGNc using Gliclazide -PLGA ratio at 1:0.5, 1:0.75, 1:1 with stabilizer (Poloxamer-188, PEG 4000, HPMC E15 at 0.5, 0.75, 1% w/v). The formulated gliclazide of SGNCs were investigated for physicochemical properties, in vitro drug release, and in vivo performance studies using type-2 diabetes rat model. The formulation (SGNCF1) with Drug: PLGA 1: 0.5 ratio with 0.5% w/v Poloxamer-188 produced optimized gliclazide SGNCs. SGNCF1 showed spherical shape, small particle size (106.3 ± 2.69 nm), good zeta potential (-18.2 ± 1.30 mV), small PDI (0.222 ± 0.104) and high entrapment efficiency (86.27 ± 0.222%). The solubility, dissolution rate and bioavailability of gliclazide SGNCs were significantly improved compared to pure gliclazide. The findings emphasize gliclazide SGNCs produce faster release initially, followed by delayed release with improved bioavailability, facilitate efficient delivery of gliclazide in T2DM with better therapeutic effect.
    Matched MeSH terms: Niacinamide/adverse effects
  19. Roslan J, Giribabu N, Karim K, Salleh N
    Biomed Pharmacother, 2017 Feb;86:570-582.
    PMID: 28027533 DOI: 10.1016/j.biopha.2016.12.044
    Quercetin is known to possess beneficial effects in ameliorating diabetic complications, however the mechanisms underlying cardioprotective effect of this compound in diabetes is not fully revealed. In this study, quercetin effect on oxidative stress, inflammation and apoptosis in the heart in diabetes were investigated. Normal and streptozotocin-nicotinamide induced adult male diabetic rats received quercetin (10, 25 and 50mg/kg/bw) orally for 28days were anesthetized and hemodynamic parameters i.e. systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate (HR) were measured. Blood was collected for analyses of fasting glucose (FBG), insulin and cardiac injury marker levels (troponin-C, CK-MB and LDH). Following sacrificed, heart was harvested and histopathological changes were observed. Heart was subjected for analyses of oxidative stress marker i.e. lipid peroxidation and activity and expression levels of anti-oxidative enzymes i.e. SOD, CAT and GPx. Levels of inflammation in the heart were determined by measuring nuclear factor (p65-NF-κB), tumor necrosis factor (TNF-α), interleukins (IL)-1β and IL-6 levels by using enzyme-linked immunoassay (ELISA). Distribution and expression levels of TNF-α and Ikk-β (inflammatory markers), caspase-3, caspase-9, Blc-2 and Bax (apoptosis markers) in the heart were identified by immunohistochemistry and Western blotting respectively.
    Matched MeSH terms: Niacinamide/pharmacology
  20. Madan JR, Pawar KT, Dua K
    Int J Pharm Investig, 2015 Apr-Jun;5(2):114-20.
    PMID: 25838997 DOI: 10.4103/2230-973X.153390
    Low aqueous solubility is a major problem faced during formulation development of new drug molecules. Lurasidone HCl (LRD) is an antipsychotic agent specially used in the treatments of schizophrenia and is a good example of the problems associated with low aqueous solubility. Lurasidone is practically insoluble in water, has poor bioavailability and slow onset of action and therefore cannot be given in emergency clinical situations like schizophrenia. Hence, purpose of this research was to provide a fast dissolving oral dosage form of Lurasidone. This dosage form can provide quick onset of action by using the concept of mixed hydrotropy. Initially, solubility of LRD was determined individually in nicotinamide, sodium citrate, urea and sodium benzoate at concentration of 10, 20, 30 and 40% w/v solutions using purified water as a solvent. Highest solubility was obtained in 40% sodium benzoate solution. In order to decrease the individual hydrotrope concentration mixed hydrotropic agents were used. Highest solubility was obtained in 15:20:5 ratio of Nicotinamide + sodium benzoate + sodium citrate. This optimized combination was utilized in the preparation of solid dispersions by using distilled water as a solvent. Solid dispersions were evaluated for X-ray diffraction, differential scanning calorimetry and Fourier-transform infrared to show no drug-hydrotropes interaction has occurred. This solid dispersion was compressed to form fast dissolving tablets. Dissolution studies of prepared tablets were done using USP Type II apparatus. The batch L3 tablets show 88% cumulative drug release within 14 min and in vitro dispersion time was 32 min. It was concluded that the concept of mixed hydrotropic solid dispersion is novel, safe and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs. The miraculous enhancement in solubility and bioavailability of Lurasidone is clear indication of the potential of mixed hydrotropy to be used in future for other poorly water-soluble drugs in which low bioavailability is a major concern.
    Matched MeSH terms: Niacinamide
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