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Formulation and evaluation of gels containing coconut? kernel extract for topical application

Asian Journal of Pharmaceutical Sciences 2018年第5期13卷 415-424页

作者： Wantanwa Krongrawa Sontaya Limmatvapirat Nushjira Pongnimitprasert Paranee Meetam Chutima Limmatvapirat department of Pharmaceutical Technology Faculty of Pharmacy Silpakorn University department of Pharmacology and Toxicology Faculty of Pharmacy Silpakorn University department of biopharmacy Faculty of Pharmacy Silpakorn University department of Pharmaceutical Chemistry Faculty of Pharmacy Silpakorn University

The biological activity of coconut( Cocos nucifera L.) extracts from its kernels and various parts was reported by many previous studies, it is therefore believable that the extracts of its kernels might show some activities in topical formulations. Among several kernel extracts, the TC06 extract prepared by soaking the steamed coconut kernels in hot water showed the highest total phenolic content(6.98 ± 0.30 mg GAE/g extract) and the strongest antioxidant activity as determined using FRAP and DPPH methods with a reducing power value of 4.12 ± 0.16 mg AAE/g of extract and an SC 50 value of 2.38 ± 0.14 mg/ml, respectively. In addition, this extract did not display any cytotoxic effects in the concentration range of 50–3200 μg/ml. Meanwhile, it revealed cytoprotective effects against t-BHP-induced cytotoxicity in HaCaT cells at concentrations higher than 400 μg/ml. The results of phytochemical investigations including a chemical color test, TLC, 1 H NMR and FTIR suggested that the TC06 extract was mainly composed of flavonoids and terpenoids. Furthermore, the concentrations of heavy metals including As, Cd, Hg, and Pb in the TC06 extract were below permissible limits. According to the solubility, the TC06 extract was incorporated into gels using Carbopol Ultrez 21 as a gelling agent. The formulated gel containing 3%(w/w) TC06 extract was stable at 4 °C and 25 °C with 75% RH throughout the storage period. It was found that the Carbopol Ultrez 21-based hydroalcoholic gel containing an aqueous extract of coconut kernels exhibited antioxidant activities in the two assays and showed a sufficient consistency, a pleasing color, and a non-oily perception during the period of observation.

关键词： Coconut kernel Extract Gel Antioxidant activity Phytochemical screening

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Influence of solvent mixtures on HPMCAS-celecoxib microparticles prepared by electrospraying

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Asian Journal of Pharmaceutical Sciences 2018年第6期13卷 584-591页

作者： Adam Bohr Yingya Wang Moritz Beck-Broichsitter Mingshi Yang department of Pharmacy Faculty of Health and Medical SciencesUniversity of Copenhagen department of Pharmaceutics and biopharmacy Philipps-Universitat Chemical and Pharmaceutical Development Bayer AG Wuya College of Innovation Shenyang Pharmaceutical University

Hypromellose acetate succinate(HPMCAS) microparticles containing the poorly-water soluble drug celecoxib(CEL) were prepared by electrospraying intended for oral drug delivery. Various solvent mixtures with different solubility for CEL and HPMCAS were used to induce changes in the polymer structural conformation of the microparticles. The performance of the prepared microparticles was evaluated by studying the solid state from, particle size and morphology, radial drug distribution and drug release. CEL was amorphous in all electrosprayed HPMCAS microparticles. The particle size and morphology was dependent on the solubility of HPMCAS in the solvent mixture used with poorer solvents resulting in smaller microparticles with rougher appearance. The CEL distribution on the particles surface was relatively homogeneous and similar for all microparticles. Drug release from the microparticles was observed at a higher rate depending on the solubility of HPMCAS in the solvent used for electrospraying, and in all cases an at least 4-fold higher rate was observed compared with the crystalline drug. Drug precipitation from the supersaturated solution was inhibited by HPMCAS for all microparticles based on its parachute effect while crystalline CEL did not reach supersaturation. This study demonstrated that electrospraying can be used to produce microparticles with tailored properties for pharmaceutical application by adjusting solvent selection.

关键词： Celecoxib Electrospraying Hypromellose acetate succinate Oral drug delivery Polymeric microparticles Solvent mixture

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Pulmonary immunization:deposition site is of minor relevance for influenza vaccination but deep lung deposition is crucial for hepatitis B vaccination

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Acta Pharmaceutica Sinica B 2019年第6期9卷 1231-1240页

作者： Jasmine Tomar Wouter FTonnis Harshad P.Patil Anne H.de boer Paul Hagedoorn Rita Vanbever Henderik W.Frijlink Wouter L.J.Hinrichs department of Pharmaceutical Technology and biopharmacy University of GroningenGroningen 9713 AVthe Netherlands Advanced Drug Delivery and Biomaterials Louvain Drug Research Institute(LDRI)Universite catholique de LouvainBrussels 1200Belgium

Vaccination via the pulmonary route could be an attractive alternative to parenteral *** towards the best site of antigen deposition within the lungs to induce optimal immune responses has conflicting results which might be dependent on the type of vaccine and/or its physical ***,in this study,we explored whether deep lung deposition is crucial for two different vaccines,i.e.,influenza and hepatitis B *** view of this,influenza subunit vaccine and hepatitis B surface antigen were labeled with a fluorescent dye and then *** data showed that after pulmonary administration to mice the powders were deposited in the trachea/central airways when a commercially available insufflator was used while deep lung deposition was achieved when an in-house built aerosol generator was *** studies revealed that comparable immune responses were induced upon trachea/central airways or deep lung targeting of dry influenza vaccine ***,for hepatitis B vaccine,no immune responses were induced by trachea/central airways deposition whereas they were considerable after deep lung ***,we conclude that deep lung targeting is not a critical parameter for the efficacy of pulmonary administered influenza vaccine whereas for hepatitis B vaccine it is.

关键词： Inhalation Powders Deep lung deposition Influenza Hepatitis B

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Oxidative Metabolism of Estrone Modified by Genistein and Bisphenol A in Rat Liver Microsomes

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Biomedical and Environmental Sciences 2015年第11期28卷 834-838页

作者： GHELDIU Ana-Maria POPA Daniela-Saveta LOGHIN Felicia VLASE Laurian department of Pharmaceutical Technology and biopharmacy Faculty of Pharmacy‘Iuliu Hatieganu’University of Medicine and Pharmacy Cluj-Napoca department of Toxicology Faculty of Pharmacy‘Iuliu Hatieganu’University of Medicine and Pharmacy Cluj-Napoca

Genistein, the main isoflavone from soy, and bisphenol A （BPA）, a food contaminant, are considered ubiquitous xenoestrogens. Here we investigated the influence of genistein and BPA on estrone （El） metabolism in rat liver microsomes. Both substances inhibited the 2-hydroxylation and 16a-hydroxylation of E1, but in different degrees, thereby reducing the 2-OH-E1/16a-OH-E1 ratio,

关键词： BPA Oxidative Metabolism of Estrone Modified by Genistein and Bisphenol A in Rat Liver Microsomes

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Clopidogrel delays and can reverse diabetic nephropathy pathogenesis in type 2 diabetic db/db mice

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World Journal of Diabetes 2022年第8期13卷 600-612页

作者： Hong-Qin Li Nian Liu Zong-Yu Zheng Hao-Lin Teng Jin Pei department of biopharmacy Jilin University School of Pharmaceutical SciencesChangchun 130021Jilin ProvinceChina department of Urology The First Hospital of Jilin UniversityChangchun 130021Jilin ProvinceChina

BACKGROUND Diabetic nephropathy(DN)is the principal cause of end-stage renal *** studies have shown that clopidogrel can prevent the early progression of renal *** To elucidate whether clopidogrel is beneficial against DN by using a db/db mouse *** db/db mice with a higher urinary albumin/creatinine ratio(ACR)relative to ageand sex-matched wild-type control mice were randomly allocated to clopidogrel and vehicle treatment *** was administered at doses of 5,10,and 20 mg/kg by gavage for 12 *** mass,blood glucose level,and urinary creatinine and albumin concentrations in each group were measured before and after the *** fibrosis was evaluated using periodic acid-Schiff and Masson’s trichrome *** renal protein expression of tumor necrosis factor-α(TNF-α),interleukin-1β(IL-1β),and F4/80 was assessed using *** TNF-α,monocyte chemoattractant protein-1(MCP-1),and IL-6 levels were analyzed using enzyme-linked immunosorbent assay;TNF-αand IL-1βmRNA expression was measured using real-time quantitative polymerase chain *** protein expression of fibronectin(FN)and collagen I was assessed using *** Clopidogrel treatment did not affect the body mass or blood glucose level of the db/db mice;however,it increased bleeding time and reduced urinary ACR in a dose-dependent *** staining revealed an amelioration of renal fibrosis,significantly lower deposition of FN and collagen I,and significantly lower expression of the proinflammatory cytokines TNF-αand IL-1βand lower levels of urinary TNF-αand MCP-1 in the clopidogrel-treated db/db mice(P<0.05).Furthermore,clopidogrel significantly reduced macrophage infiltration into the glomeruli of the db/db *** Clopidogrel significantly reduced renal collagen deposition and fibrosis and prevented renal dysfunction in db/db mice,most likely through inhibition of renal macrophage infi

关键词： Diabetes Clopidogrel Inflammation Fibronectin Diabetic nephropathy

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Fabrication and characterization of spearmint oil loaded nanoemulsions as cytotoxic agents against oral cancer cell

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Asian Journal of Pharmaceutical Sciences 2018年第5期13卷 425-437页

作者： Sukannika Tubtimsri Chutima Limmatvapirat Siripan Limsirichaikul Prasert Akkaramongkolporn Yutaka Inoue Sontaya Limmatvapirat Faculty of Pharmaceutical Science Burapha University department of Pharmaceutical Technology Faculty of Pharmacy Silpakorn University department of Pharmaceutical Chemistry Faculty of Pharmacy Silpakorn University department of biopharmacy Faculty of Pharmacy Silpakorn University Laboratory of Drug Safety Management Faculty of Pharmacy and Pharmaceutical Science Josai University

Spearmint oil(SMO), a commonly used essential oil for oral care products, possesses various interesting functions, especially for anticancer property. However, the application of SMO for cancer treatment is limited due to water insoluble. In the present study, nanoemulsions, which have been widely accepted as dosage forms for poorly water-soluble drugs, were selected as candidate carriers for SMO to inhibit oral cancer cell. The nanoemulsions were fabricated using phase inversion temperature method. The factors affecting formation and properties of nanoemulsions including type and amount of surfactants, oil loading and ratio of SMO to virgin coconut oil(VCO) were investigated. Among the surfactants used, the nanoemulsions containing polyoxyethylene castor oil derivatives(Kolliphor ?EL; PCO35, Cremophor ?RH40; PCO40, Eumulgin ?CO60; PCO60) and polyoxyethylene sorbitan fatty acid esters(PSF80) showed 100% creaming after temperature cycling test indicating excellent physical stability while those containing PCO40 demonstrated more transparency and better physical stability. With an increasing amount of PCO40, the droplet size tended to decrease and was in the nano-size range( < 1000 nm) after increasing to more than 5%(w/w). SMOVCO loading also influenced on the droplet size. At 5%(w/w) PCO40, the maximum SMO-VCO loading of 25%(w/w) to attain nanoemulsions was observed. Moreover, the composition of oils had an impact on size of emulsions. The transparent nanoemulsions were only prepared in the range of SMO-VCO from 40:60 to 80:20, suggesting the optimum ratio of SMO tosurfactant and the composition of oils were the critical factors for formation of nanoemulsions. NMR study disclosed that the interaction between PCO40 with both VCO and SMO should be a possible stabilization mechanism. Furthermore, the SMO-VCO nanoemulsions exhibited significant cytotoxic effect against oral carcinoma(KON) cell line using MTT assay. The finding, therefore, revealed the good feasibility o

关键词： Nanoemulsions Spearmint oil Coconut oil Surfactants Anticancer NMR

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Hormone replacement therapy decreases noradrenaline release in human myometrium

Hormone replacement therapy decreases noradrenaline release ...

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第十五届国际药理学大会

作者： Csonka Denes Kormanyos Zsolt Zupko Istvan Falkay George department of Pharmacodynamics and biopharmacy University of Szeged Hungary. department of Obstetrics and Gynecology University of Szeged Hungary. department of Pharmacodynamics and biopharmacy University of Szeged Hungary. department of Pharmacodynamics and biopharmacy University of Szeged Hungary.

＜正＞ Aim: The aim of the present study was to investigate the effect of hormone replacement therapy （HRT） on noradrenaline release profile of human myometrial tissue. Samples were collected from women with different hormonal status （regular cycle, postmenopause. receiving HRT）.Method: Samples were loaded with [3H] - noradrenaline and transferred into a chamber for superfusion after excision. After a wash- out period. 3 - min fractions were collected. In the 5th and 15th fraction tissues were stimulated with electric field. [3H] - noradrenaline content of the fractions was determined together with remaining amount in the tissue for fractional release calculation. Results: Myometrial [3H] - noradrenaline release and uptake was substantially decreased among patients in postmenopause and in patients who have received HRT compared to control group. These differences were more pronounced in HRT - treated patients than in postmenopausal ***: HRT decreases the noradrenaline content of myometrial neurons and their stimulus - evoked noradrenaline release. These results support previous findings that found HRT to inhibit sympathetic activity.

关键词： hormone replacement myometrium noradrenaline

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Influence of Genista Tinctoria L or Methylparaben on Subchronic Toxicity of Bisphenol A in Rats

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Biomedical and Environmental Sciences 2014年第2期27卷 85-96页

作者： Daniela-Saveta POPA Pompei BOLFA Bela KISS Laurian VLASE Ramona PLTINEAN Anca POP Cornel CTOI Gianina CRISAN Felicia LOGHIN department of Toxicology Faculty of Pharmacy Iuliu Hatieganu University of Medicine and Pharmacy Cluj-Napoca department of Pathology Faculty of Veterinary MedicineUniversity of Agricultural Sciences and Veterinary Medicine department of Biomedical Sciences Ross University School of Veterinary Medicine department of Pharmaceutical Technology and biopharmacy Faculty of Pharmacy ‘Iuliu Hatieganu'University of Medicine and Pharmacy Cluj-Napoca department of Pharmaceutical Botany Faculty of Pharmacy ‘Iuliu Hatieganu' University of Medicine and Pharmacy Cluj-Napoca

Objective To evaluate the influence of an extract of Genista tinctoria L. herba （GT） or methylparaben （MP） on histopathological changes and 2 biomarkers of oxidative stress in rats subchronicly exposed to bisphenol A （BPA）. Methods Adult female Wistar rats were orally exposed for 90 d to BPA （50 mg/kg）, BPA＋GT （35 mg isoflavones/kg） or BPA＋MP （250 mg/kg）. Plasma and tissue samples were taken from liver, kidney, thyroid, uterus, ovary, and mammary gland after 30, 60, and 90 d of exposure respectively. Lipid peroxidation and in vivo hydroxyl radical production were evaluated by histological analysis along with malondialdehyde and 2,3-dihydroxybenzoic acid detection. Results The severity of histopathological changes in liver and kidneys was lower after GT treatment than after BPA or BPA＋MP treatment. A minimal thyroid receptor antagonist effect was only observed after BPA＋MP treatment. The abnormal folliculogenesis increased in a time-dependent manner, and the number of corpus luteum decreased. No significant histological alterations were found in the uterus. The mammary gland displayed specific estrogen stimulation changes at all periods. Both MP and GT revealed antioxidant properties reducing lipid peroxidation and BPA-induced hydroxyl radical generation. Conclusion GT L. extract ameliorates the toxic effects of BPA and is proved to have antioxidant potential and antitoxic effect. MP has antioxidant properties, but has either no effect or exacerbates the BPA-induced histopathological changes.

关键词： Food contaminant Phytoestrogen Morphological effect Lipid peroxidation Hydroxylradical

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Layer-by-layer nanostructured protein loaded nanoparticles: A feasibility study using lysozyme as model protein and chitosan as coating material

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 64-65页

作者： Cuifang Cai Shirui Mao Thomas Kissel School of Pharmacy Shenyang Pharmaceutical UniversityWenhua Road 103110016 ShenyangChina department of Pharmaceutics and biopharmacy Phillips-Universitat of MarburgKetzerbach 63D-35032 MarburgGermany

Stabilization of proteins in delivery devices and design of appropriate protein carriers are major research issues due to the extreme sensitivity of ***,negatively charged nanoparticles,consisting of poly(lactic-co-glycolic acid)(PLGA)and poly(styrene-co-4–styrene-sulfonate)(PSS),showed considerably high loading capacity for positively charged model protein lysozyme depending on the surface charge density of nanoparticles.

关键词： Chitosan Nanoparticles Lysozyme Electrostatic interaction Protein carrier Layer-by-layer

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Tannic acid assisted anti-TNF-αnanobody assembly modulating the epithelial barrier dysregulation of allergic rhinitis

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Nano Research 2023年第7期16卷 9781-9791页

作者： Shuilian Fu Zhiting Cao Baolian Huang Te Yin Chujun Huang Zhiqian Bi Yingying Yao Xiaoyao Chang Hongqin Zhuang Zi-Chun Hua The State Key Laboratory of Pharmaceutical Biotechnology College of Life SciencesNanjing UniversityNanjing 210023China Changzhou High-Tech Research Institute of Nanjing University and Jiangsu TargetPharma Laboratories Inc. Changzhou 213164China School of biopharmacy China Pharmaceutical UniversityNanjing 211198China

The derailed nasal epithelial barrier is associated with the disorder of tight junctions(TJ)function or expression,leading to more penetration of allergens to the barrier,accompanied by the release of cytokines,which develop allergic rhinitis(AR).Considering the increasing AR disease incidence worldwide,there is still an urgent unmet medical need to develop new *** necrosis factor-alpha(TNF-α)inhibitors have been applied in treating autoimmune ***,their roles in AR remain *** this study,anti-TNF-αnanobody(V)was assembled with tannic acid(V/TA)as a functional antibody drug candidate which could inhibit the release of the cytokines in ovalbumin(OVA)-induced AR murine *** receiving V/TA treatment,the infiltration level of inflammatory cells,and the number of mucus-secreting cells and mast cells in the nasal mucosa recovered to a relatively normal *** mechanism of action research revealed that the efficacy of V/TA was accompanied by the restricted level of TJ molecules:zonula occluden-1(ZO-1),occludin,claudin-1,and *** therapeutic effect of the anti-TNF-αnanobody against AR was enhanced with the tannic acid assisted without any toxicity *** study supplied a promising delivery strategy of TNF-αinhibitor for the effective treatment of complicated allergic rhinitis disease,with an advantage in restoring effect on the AR-caused epithelial barrier defects than the commercial drug Infliximab.

关键词： allergic rhinitis tumor necrosis factor-alpha(TNF-α)nanobody nanoparticles epithelial permeability tight junctions

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