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1.
J Vector Borne Dis ; 61(1): 107-116, 2024 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-38648412

RESUMO

BACKGROUND OBJECTIVES: Mosquitoes alone transmit diseases to around 700 million individuals annually, killing approximately 0.7 million people every year worldwide. Considering the potential health risks linked with synthetic repellents, it has become vital to identify eco-friendly, natural repellents for mosquito control as well as to understand the underlying mechanism for mosquito repellent activity. To address this, objectives were set to extract essential oils from Citrus macroptera peel and Homalomena aromatica (Spreng.) Schott. rhizomes, evaluate their mosquito repellent activity against Aedes aegypti, and further explore their mosquito odorant receptor inhibition potential. METHODS: The oils were extracted using Clevenger's apparatus, and properties like specific gravity, refractive index, and boiling point were evaluated and characterised using Fourier transform infrared spectroscopy (FTIR) and gas chromatography-mass spectroscopy (GC-MS). Aedes aegypti mosquito eggs collected from the Indian Council of Medical Research (ICMR), Dibrugarh, were reared in the Department of Pharmaceutical Sciences, Research Laboratory, to obtain adult Aedes aegypti mosquitoes for the mosquito repellent activity evaluation of the essential oils using the Human Bait technique'. Molecular docking studies were performed for the oil components against mosquito odorant binding proteins. Further, toxicity studies of these two oils were evaluated against human dermal fibroblast adult (HDFa) cells. RESULTS: The results revealed the presence of limonene (86.76%) and linalool (52.35%), respectively, in Citrus macroptera and Homalomena aromatica oils. It was found that the combination of the oils in a ratio of 1:1 showed mosquito repellent activity for up to 6.33 ± 0.23 h. Molecular docking studies showed the presence of major oil components having mosquito odorant receptor blocking potential comparable to N, N-diethyl-meta-toluamide (DEET), indicating a rationale for extended mosquito repellent action. Further, both of these oils were found to be non-cytotoxic against HDFa cells after 24 h. INTERPRETATION CONCLUSION: The encouraging mosquito repellent activity of these two oils as compared to synthetic mosquito repellent DEET might pave the way for the development of novel herbal mosquito repellent formulations containing these essential oils.


Assuntos
Aedes , Citrus , Repelentes de Insetos , Simulação de Acoplamento Molecular , Óleos Voláteis , Repelentes de Insetos/farmacologia , Repelentes de Insetos/química , Repelentes de Insetos/isolamento & purificação , Animais , Aedes/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Citrus/química , Humanos , Cromatografia Gasosa-Espectrometria de Massas , Espectroscopia de Infravermelho com Transformada de Fourier , Receptores Odorantes/metabolismo , Receptores Odorantes/química , Feminino , Rizoma/química
2.
Heliyon ; 10(7): e28457, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38586388

RESUMO

ß-carotene is obtained from both plants and animals and has been the subject of intense research because of its provitamin-A, antioxidant, and anticancer effects. Its limited absorption and oxidative degradation significantly reduce its antitumor efficacy when taken orally. In our study, we utilize a central composite design to develop "bio-safe and highly bio-compatible" solid lipid nanoparticles (SLNs) by using only the combination of palmitic acid and poloxamer-407, a block co-polymer as a surfactant. The current research aim to develop and characterize SLNs loaded with ß-carotene to improve their bioavailability and therapeutic efficacy. In addition, the improved cytotoxicity of solid lipid nanoparticles loaded with ß-carotene was screened in-vitro in human breast cancer cell lines (MCF-7). The nanoparticles exhibits good stability, as indicated by their mean zeta potential of -26.3 ± 1.3 mV. The particles demonstrated high drug loading and entrapment capabilities. The fabricated nanoparticle's prolonged release potential was shown by the in-vitro release kinetics, which showed a first-order release pattern that adhered to the Higuchi model and showed a slow, linear, and steady release over 48 h. Moreover, a diffusion-type release mechanism was used to liberate ß-carotene from the nanoparticles. For six months, the nanoparticles also showed a notable degree of physical stability. Lastly, using the MTT assay, the anti-cancer properties of ß-carotene-loaded solid lipid nanoparticles were compared with intact ß-carotene on MCF-7 cell lines. The cytotoxicity tests have shown that the encapsulation of ß-carotene in the lipid bilayers of the optimized formulation does not interfere with the anti-cancer activity of the drug. When compared to standard ß-carotene, ß-carotene loaded SLNs showed enhanced anticancer efficacy and it is a plausible therapeutic candidate for enhancing the solubility of water-insoluble and degradation-sensitive biotherapeutics like ß-carotene.

3.
Curr Cancer Drug Targets ; 23(8): 620-633, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36843367

RESUMO

Pancreatic ductal adenocarcinoma (PDAC) is one of the foremost causes of cancer-related morbidities worldwide. Novel nanotechnology-backed drug delivery stratagems, including molecular targeting of the chemotherapeutic payload, have been considered. However, no quantum leap in the gross survival rate of patients with PDAC has been realized. One of the predominant causes behind this is tumor desmoplasia, a dense and heterogenous stromal extracellular matrix of the tumor, aptly termed tumor microenvironment (TME). It plays a pivotal role in the tumor pathogenesis of PDAC as it occupies most of the tumor mass, making PDAC one of the most stromal-rich cancers. The complex crosstalk between the tumor and dynamic components of the TME impacts tumor progression and poses a potential barrier to drug delivery. Understanding and deciphering the complex cascade of tumorstromal interactions are the need of the hour so that we can develop neoteric nano-carriers to disrupt the stroma and target the tumor. Nanodiamonds (NDs), due to their unique surface characteristics, have emerged as a promising nano delivery system in various pre-clinical cancer models and have the potential to deliver the chemotherapeutic payload by moving beyond the dynamic tumor-stromal barrier. It can be the next revolution in nanoparticle-mediated pancreatic cancer targeting.


Assuntos
Carcinoma Ductal Pancreático , Nanodiamantes , Neoplasias Pancreáticas , Humanos , Nanodiamantes/uso terapêutico , Terapia de Alvo Molecular , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/patologia , Carcinoma Ductal Pancreático/tratamento farmacológico , Carcinoma Ductal Pancreático/patologia , Microambiente Tumoral , Neoplasias Pancreáticas
4.
Carbohydr Polym ; 206: 336-343, 2019 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-30553330

RESUMO

Microcrystalline cellulose (MCC) is one of the most important functional excipient in Pharmaceutical industries. A renewable biomass from Ensete glaucum (Roxb.) was investigated as a potential source of a novel functional MCC. MCC was prepared by a simple, dilute acid hydrolysis and characterized through FTIR, DSC, XRD, along with micromeritic studies. Functional properties such as packing, rearrangement, consolidation and compactibility of the prepared MCC were also evaluated in view of its application as drug delivery biomaterial. Results suggest that the prepared MCC exhibit properties comparable to commercially available standard MCC. From Kawakita and Heckel plots, it was observed that the new MCC consolidates better than the standard MCC. Disintegration efficiency test also indicates that the novel MCC functions as a better tablet disintegrant to the standard MCC indicating the potential of Ensete glaucum (Roxb.) as a green resource for preparation of the low cost, functional and sustainable carbohydrate polymer.


Assuntos
Materiais Biocompatíveis/química , Celulose/química , Portadores de Fármacos/química , Excipientes/química , Musa/química , Materiais Biocompatíveis/isolamento & purificação , Biomassa , Celulose/isolamento & purificação , Portadores de Fármacos/isolamento & purificação , Excipientes/isolamento & purificação , Química Verde/métodos , Porosidade , Comprimidos/química , Resistência à Tração , Viscosidade
5.
Int J Biol Macromol ; 118(Pt A): 397-405, 2018 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-29935240

RESUMO

The objective of the present work is to study the physicochemical and functional properties of taro starch (Colocasia esculenta) and to further modify the starch by treating with citric acid to obtain a novel functional material. DSC, FTIR and SEM studies were performed along with physicochemical analysis. The disintegrant efficiency ratio and dissolution efficiency were determined on paracetamol tablets prepared by wet granulation taking the starch as a binder-disintegrant. The moisture content and ash values of taro and citrate taro starches were about 13% and 0.5% respectively. The average particle size of taro starch was found to be 1.53 µm and citration was not found to cause significant changes in the particle size. Results from disintegration efficiency study showed that both the taro and citrate modified taro starch showed tablet disintegrant property and even performed better than the standard corn starch. The reduced disintegration time was also found to enhance dissolution of the model drug from the tablet.


Assuntos
Química Farmacêutica , Ácido Cítrico/química , Colocasia/química , Amido/química , Ácido Cítrico/uso terapêutico , Composição de Medicamentos , Humanos , Tamanho da Partícula , Solubilidade , Amido/uso terapêutico , Comprimidos/química
6.
Indian J Surg Oncol ; 9(1): 11-14, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29563728

RESUMO

Angioimmunoblastic T cell lymphoma (AITL) is a peripheral T cell non-Hodgkin lymphoma with an aggressive fatal course and it has varied clinical presentation with an uncommon presentation when they present as soft tissue masses or when there is spill in the peripheral blood or there are composite lymphomas that are rare presentations. Common presentations include lymphadenopathy, fever and systemic symptoms, hemolytic anemias, skin rashes, and rheumatoid arthritis. The classical histopathology is absence of follicles in lymph nodes with presence of high endothelial venules and the tumor cells of small to medium-sized lymphocytes with pale cytoplasm mixed with reactive T cells. On immunohistochemistry, the cells are positive for CD3, CD4, CD10, BCL2, and CXCL13. In this observational study, the clinicopathologic presentation and the immunohistochemical profile of five cases who initially presented with a soft tissue mass which is an extremely rare presentation of this rare type of non-Hodgkin lymphoma that was diagnosed at our center with peripheral blood and bone marrow involvement and the clinicopathologic presentation, immunohistochemical profile, and response to treatment on follow-up are correlated with the literature review. One case had a fulminant and aggressive course and was fatal within 2 months of diagnosis. The rest of the four cases are on regular chemotherapy and follow-up. Our five cases had presented with soft tissue masses, two in the axillary regio,n two in the hand, and one in the scapular region with an extranodal presentation, and there was associated lymphadenopathy which developed subsequently with classic histomorphology and immunohistochemical findings. The age range was 46-54 years and all five cases were males. Three cases were with anemia (hemoglobin range 6.5-8.0 mg/dl) and all five cases were having peripheral blood plasmacytosis. Histopathology was classic with paracortical involvement with polymorphous population of cells with neoplastic lymphocytes of small and large sizes with numerous arborizing blood vessels which correspond to high endothelial venules. Microscopically, three architectural patterns; pattern I was seen in three cases (60%) and then pattern II and III in one case each (20% each). Immunohistochemistry revealed CD4+, CD8-, CXCL13+, CD10+, BCL6+, CD19, CD20, CD1a, Tdt, CD21, and CD23+ in follicular dendritic cells. AITL is a rare and aggressive non-Hodgkin lymphoma with varied clinical presentation with classic histomorphology with various patterns which may cause diagnostic dilemma and immunophenotypic findings, and prompt and early diagnosis is mandatory for institution of therapy.

7.
Int J Biol Macromol ; 95: 1298-1304, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27840214

RESUMO

The objective of the current work is to characterize the physicochemical and disintegrant properties of a starch obtained from a novel glutinous rice variety from Mizoram, India. Different properties such as total starch, apparent amylose content, protein and moisture content, along with micromeritic properties were evaluated. Viscosity was determined by Brookfield viscometer, DSC and FTIR spectroscopic analyses were also performed. The disintegrant efficiency was evaluated after dicalcium phosphate tablets were prepared using the starch as binder-disintegrant at different concentrations. The total starch content was found to be 83.48% with 2.83% crude protein and 10.22% moisture content. The average particle size of the starch was also found to be 11.39µm. DSC and FTIR analysis shows the starch possesses typical characteristics of starches. Results from disintegration efficiency study also showed that the starch possesses significant disintegration property and the disintegration efficiency increases with increase in concentration of the starch.


Assuntos
Amilose/análise , Oryza/química , Proteínas de Plantas/análise , Amido/química , Fosfatos de Cálcio/química , Hidrólise , Tamanho da Partícula , Solubilidade , Amido/isolamento & purificação , Viscosidade , Água/análise
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