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1.
Int J Pharm ; 653: 123872, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38336178

RESUMO

Cardiotoxicity (CT) is a severe condition that negatively impacts heart function. ß-sitosterol (BS) is a group of phytosterols and known for various pharmacological benefits, such as managing diabetes, cardiac protection, and neuroprotection. This study aims to develop niosomes (NS) containing BS, utilizing cholesterol as the lipid and Tween 80 as the stabilizer. The research focuses on designing and evaluating both conventional BS-NS and hyaluronic acid (HA) modified NS (BS-HA-NS) to enhance the specificity and efficacy of BS within cardiac tissue. The resulting niosomal formulation was spherical, with a size of about 158.51 ± 0.57 nm, an entrapment efficiency of 93.56 ± 1.48 %, and a drug loading of 8.07 ± 1.62 %. To evaluate cytotoxicity on H9c2 heart cells, the MTT assay was used. The cellular uptake of BS-NS and BS-HA-NS was confirmed by confocal microscopy on H9c2 cardiac cells. Administering BS-NS and BS-HA-NS intravenously at a dose of 10 mg/kg showed the ability to significantly decrease the levels of cardiac troponin-I (cTn-I), creatine kinase-MB (CK-MB), lactate dehydrogenase (LDH), aspartate aminotransferase (AST), and lipid peroxidation (MDA). Tissue histopathology indicated a substantial potential for repairing cardiac tissue after treatment with BS-NS and BS-HA-NS and strong cardioprotection against ISO induced myocardial tissue damages. Thus, enhancing BS's therapeutic effectiveness through niosome surface modification holds promise for mitigating cardiac damage resulting from CT.


Assuntos
Cardiotoxicidade , Infarto do Miocárdio , Sitosteroides , Ratos , Animais , Isoproterenol/metabolismo , Isoproterenol/farmacologia , Cardiotoxicidade/tratamento farmacológico , Cardiotoxicidade/prevenção & controle , Lipossomos/farmacologia , Cardiotônicos/farmacologia , Infarto do Miocárdio/tratamento farmacológico , Miocárdio/patologia , Antioxidantes/farmacologia , Estresse Oxidativo
2.
Mol Pharm ; 20(2): 997-1014, 2023 02 06.
Artigo em Inglês | MEDLINE | ID: mdl-36630478

RESUMO

Psoriasis is an autoimmune skin disease that generally affects 1%-3% of the total population globally. Effective treatment of psoriasis is limited because of numerous factors, such as ineffective drug delivery and efficacy following conventional pharmaceutical treatments. Nanofibers are widely being used as nanocarriers for effective treatment because of their multifunctional and distinctive properties, including a greater surface area, higher volume ratio, increased elasticity and improved stiffness and resistance to traction, favorable biodegradability, high permeability, and sufficient oxygen supply, which help maintain the moisture content of the skin and improve the bioavailability of the drugs. Similar to the extracellular matrix, nanofibers have a regeneration capacity, promoting cell growth, adhesion, and proliferation, and also have a more controlled release pattern compared with that of other conventional therapies at the psoriatic site. To ensure improved drug targeting and better antipsoriatic efficacy, this study formulated and evaluated a tazarotene (TZT)-calcipotriol (CPT)-loaded nanofiber and carbopol-based hydrogel film. The nanofiber was prepared using electrospinning with a polyvinyl alcohol/polyvinylpyrrolidone (PVA/PVP) K-90 polymeric blend that was later incorporated into a carbopol base to form hydrogel films. The prepared nanofibers were biochemically evaluated and in vitro and in vivo characterized. The mean diameters of the optimized formulation, i.e., TZT-loaded polyvinyl alcohol/polyvinylpyrrolidone nanofiber (TZT-PVA/PVP-NF) and TZT-CPT-loaded polyvinyl alcohol/polyvinylpyrrolidone nanofiber (TZT-CPT-PVA/PVP-NF) were 244.67 ± 58.11 and 252.31 ± 35.50 nm, respectively, as determined by scanning electron microscopy, and their tensile strength ranged from 14.02 ± 0.54 to 22.50 ± 0.03 MPa. X-ray diffraction revealed an increase in the amorphous nature of the nanofibers. The biodegradability studies of prepared nanofiber formulations, irrespective of their composition, showed that these completely biodegraded within 2 weeks of their application. The TZT-CPT-PVA/PVP-NF nanofibers exhibited 95.68% ± 0.03% drug release at the end of 72 h, indicating a controlled release pattern and following Higuchi release kinetics as a best-fit model. MTT assay, antioxidant and lipid profile tests, splenomegaly assessment, and weight fluctuation were all performed in the in vitro as well as in vivo studies. We found that the TZT-CPT-PVA/PVP-NF-based hydrogel film has high potential for antipsoriatic activity in imiquimod-induced Wistar rats in comparison with that of TT-PVA/PVP-NF nanofibers.


Assuntos
Nanofibras , Psoríase , Ratos , Animais , Álcool de Polivinil/química , Nanofibras/química , Povidona/química , Preparações de Ação Retardada , Ratos Wistar , Psoríase/tratamento farmacológico
3.
Pharmaceuticals (Basel) ; 15(3)2022 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-35337100

RESUMO

Diabetic foot ulceration is the most distressing complication of diabetes having no standard therapy. Nanofibers are an emerging and versatile nanotechnology-based drug-delivery system with unique wound-healing properties. This study aimed to prepare and evaluate silk-sericin based hybrid nanofibrous mats for diabetic foot ulcer. The nanofibrous mats were prepared by electrospinning using silk sericin mixed with different proportions of polycaprolactone (PCL) and cellulose acetate (CA) loaded with ferulic acid (FA). The in vitro characterizations, such as surface morphology, mechanical properties, swelling behavior, biodegradability, scanning electron microscopy, and drug release were carried out. The SEM images indicated that nanofibers formed with varied diameters, ranging from 100 to 250 nm, and their tensile strength was found to range from 7 to 15 MPa. In vitro release demonstrated that the nanofibers sustained FA release over an extended time of period. In vitro cytotoxicity showed that the nanofibers possessed a lower cytotoxicity in HaCaT cells. The in vivo wound-healing studies demonstrated an excellent wound-healing efficiency of the nanofibers in diabetic rats. Furthermore, the histopathological studies showed the nanofibers' ability to restore the skin's normal structure. Therefore, it was concluded that the prepared silk-sericin-based hybrid nanofibers loaded with FA could be a promising drug-delivery platform for the effective treatment of diabetic foot ulcers.

4.
Trop Anim Health Prod ; 53(4): 413, 2021 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-34308489

RESUMO

Leptin an adipokine plays a significant role in several physiological processes and has been indicated as a candidate gene for marker-assisted selection for high-yielding cows. Insulin-like growth factor-1 (IGF-1) hormone plays an important physiological role in growth, development, metabolism, and lactation in bovines. It is believed to be one of the main mediators of energy balance effects on the reproductive performance of dairy cows after calving. The present investigation was carried out to identify the novel polymorphisms in exon 3 region of leptin and exon 3 partial intron 3 of IGF-1 genes and their association with the milk production performance in indicine and taurine crossbred (Karan Fries) cows. Blood samples were collected from 160 apparently healthy Karan Fries (KF) cows. Four SNPs (single-nucleotide polymorphisms) at positions rs29004508 (C > T), rs29004509 (C > T), rs29004510 (T > C), and rs29004511 (T > C) in leptin gene and two SNPs at positions rs133251968 (C > A) and rs137289661 (C > T) in IGF-1 gene were found in KF cows; however, rs29004509 (C > T) had a positive correlation (r = 0.376; P < 0.05) with milk yield. The genetic variants observed in exon 3 region of leptin gene and their association with milk yield traits revealed the importance of CT genotype, which had been useful for genetic improvement of KF cow for milk production traits and can also be utilized as a potential genetic marker to select appropriate animals.


Assuntos
Leptina , Leite , Animais , Bovinos/genética , Feminino , Fator de Crescimento Insulin-Like I/genética , Lactação , Leptina/genética , Polimorfismo de Nucleotídeo Único
5.
Curr Drug Deliv ; 18(8): 1094-1104, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33645481

RESUMO

Cardiovascular diseases cover various disorders like ischemic heart disease, hyperlipidemia, atherosclerosis, myocardial infarction, hypertension, etc. There are many synthetic drugs available for the treatment of cardiovascular therapy. However, they have several drawbacks like high dosing, toxicity, elevated blood potassium levels, low blood pressure, gastrointestinal issues, etc. To overcome these side effects of synthetic drugs, targeting the drug to the specific cardiac tissue is the best novel method in cardiovascular therapy. The highest targeting efficacy of ligand- based therapy with proper mechanisms and improved expandability provides a novel therapeutic strategy in cardiovascular diseases. Ligand therapy is more cost-effective compared to cell- based therapy. The surface area of protein is much larger than the orally bioavailable drug. Therefore, the targeting of various less active drug molecules to the particular ligand can be possible. The efficacy of ligands to induce cardiomyocytes proliferation has been ratified. The fact that ligand- based approaches are effective for cardiac transformation has been pointed out. Ligands interact with proteins in target cells, which are influenced by chemical signals. These various receptors selectively bind to biased ligands and energize the intracellular signaling pathway. The ligands can directly stabilize the active receptor conformations by a non-standard connective site. The key function of ligands is functional selectivity, which enhances the therapeutic efficacy and minimizes the side effects of drugs through the interpretation of signal transduction pathways. This review covers the role and effectiveness of novel ligands in cardiovascular disorders.


Assuntos
Doenças Cardiovasculares , Hipertensão , Hormônios Peptídicos , Receptores de Apelina , Doenças Cardiovasculares/tratamento farmacológico , Humanos , Ligantes
6.
Curr Drug Deliv ; 2021 02 23.
Artigo em Inglês | MEDLINE | ID: mdl-33655835

RESUMO

The article has been withdrawn at the request of the editor of the journal Current Drug Delivery due to incoherent content.Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused.The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php Bentham Science Disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submit- ting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript, the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.

7.
Vet World ; 9(3): 256-9, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27057108

RESUMO

AIM: To investigate the effect of pre-partum prilled fat feeding on dry matter intake (DMI), energy balance and milk production in Murrah buffaloes. MATERIALS AND METHODS: Advance pregnant Murrah buffaloes were either received a dietary supplement of prilled fat at 100 g/day for 35 days pre-partum and at 150 g/day for 95 days post-partum (supplemented group [SG]) or did not receive fat supplement (control group [CG]). DMI and the yields of milk and milk component were measured. A body condition score (BCS) was recorded. Energy balance and gross feed efficiency (GFE) were calculated. DMI and BCS were recorded and milk yield (MY), fat, protein, lactose, solid not fat, energy balance were measured. The fat corrected milk yield was calculated. RESULTS: The DMI was non-significant between groups and periods of study. BCS of buffaloes improved in the SG than CG (p<0.01). The energy intake in terms of total digestible nutrients (TDN%), TDN intake, digestible energy (DE), metabolizable energy/kg of milk, DE of milk, net energy, and GFE were higher (p<0.01) in SG during post-partum period. Crude protein intake was statistically similar in both the groups. MY was higher (p<0.01) in SG than in CG during 95 days of early lactation. Milk fat, fat corrected MY was higher (p<0.01) in SG however protein, lactose and solid not fat content did not varied between the groups. The feed efficiency of the SG was higher (p<0.01) than the CG during the post-partum period. CONCLUSION: It was inferred that prilled fat supplementation augments energy balance and milk production in transition Murrah buffaloes.

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