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1.
Pharmaceutics ; 13(11)2021 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-34834310

RESUMO

Ceftriaxone has been a part of therapeutic regime for combating some of the most aggressive bacterial infections in the last few decades. However, increasing bacterial resistance towards ceftriaxone and other third generation cephalosporin antibiotics has raised serious clinical concerns especially due to their misuse in the COVID-19 era. Advancement in nanotechnology has converted nano-therapeutic vision into a plausible reality with better targeting and reduced drug consumption. Thus, in the present study, gold nanoparticles (GNPs) were synthesized by using ceftriaxone antibiotic that acts as a reducing as well as capping agent. Ceftriaxone-loaded GNPs (CGNPs) were initially characterized by UV-visible spectroscopy, DLS, Zeta potential, Electron microscopy and FT-IR. However, a TEM micrograph showed a uniform size of 21 ± 1 nm for the synthesized CGNPs. Further, both (CGNPs) and pure ceftriaxone were examined for their efficacy against Escherichia coli, Staphylococcus aureus, Salmonella abony and Klebsiella pneumoniae. CGNPs showed MIC50 as 1.39, 1.6, 1.1 and 0.9 µg/mL against E. coli, S. aureus, S. abony and K. pneumoniae, respectively. Interestingly, CGNPs showed two times better efficacy when compared with pure ceftriaxone against the tested bacterial strains. Restoring the potential of unresponsive or less efficient ceftriaxone via gold nanoformulations is the most alluring concept of the whole study. Moreover, applicability of the findings from bench to bedside needs further validation.

2.
Polymers (Basel) ; 13(19)2021 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-34641026

RESUMO

Gliomas are one of the prominent cancers of the central nervous system with limited therapeutic modalities. The present investigation evaluated the synergistic effect of paclitaxel (PAX) and resveratrol (RESV)-loaded Soluplus polymeric nanoparticles (PNPs) against glioma cell lines along with in vivo pharmacokinetics and brain distribution study. PAX-RESV-loaded PNPs were prepared by the thin film hydration technique and optimized for different dependent and independent variables by using DoE (Design-Expert) software. The in vitro physiochemical characterization of prepared PAX-RESV-loaded PNPs exhibited appropriate particle size, PDI and % encapsulation efficiency. Cytotoxicity assay revealed that PTX-RESV loaded PNPs had a synergistic antitumor efficacy against C6 glioma cells compared with single and combined pure drugs. Finally, the pharmacokinetic and brain distribution studies in mice demonstrated that the PNPs significantly enhanced the bioavailability of PTX-RESV PNPs than pure PAX and RESV. Thus, the study concluded that PAX-RESV PNPs combination could significantly enhance anti-glioma activity, and this could be developed into a potential glioma treatment strategy.

3.
Folia Microbiol (Praha) ; 66(6): 897-916, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34699042

RESUMO

Recent advancement in manipulation techniques of gut microbiota either ex vivo or in situ has broadened its plausible applicability for treating various diseases including cardiovascular disease. Several reports suggested that altering gut microbiota composition is an effective way to deal with issues associated with managing cardiovascular diseases. However, actual translation of gut microbiota manipulation-based techniques into cardiovascular-therapeutic approach is still questionable. This review summarized the evidence on challenges, opportunities, recent development, and future prospects of gut microbiota manipulation for targeting cardiovascular diseases. Initially, issues associated with current cardiovascular diseases treatment strategy, association of gut microbiota with cardiovascular disease, and its influence on cardiovascular drugs were discussed, followed by applicability of gut microbiota manipulation as a cardiovascular disease intervention strategy along with its challenges and future prospects. Despite the fact that the gut microbiota is rugged, interventions like probiotics, prebiotics, synbiotics, fecal microbiota transplantation, fecal virome transplantation, antibiotics, diet changes, and exercises could manipulate it. Advanced techniques like administration of engineered bacteriophages and bacteria could also be employed. Intensive exploration revealed that if sufficiently controlled approach and proper monitoring were applied, gut microbiota could provide a compelling answer for cardiovascular therapy.


Assuntos
Doenças Cardiovasculares , Microbioma Gastrointestinal , Probióticos , Simbióticos , Doenças Cardiovasculares/terapia , Transplante de Microbiota Fecal , Humanos , Prebióticos
4.
Curr Issues Mol Biol ; 43(2): 932-940, 2021 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-34449548

RESUMO

Prostate cancer (PCa) is addressed as the second most common form of onco-threat worldwide and is usually considered as the major cause of mortality in men. Recent times have seen a surge in exploration of plant-derived components for alternative therapeutical interventions against different oncological malignancies. Dammarolic acid or Asiatic acid (AsA) is an aglycone asiaticoside that has been reported for its efficacy in several ailments including cancer. The current study aimed to investigate the anti-proliferative potency of AsA against human prostate cancer PC-3 cells. Purified AsA was diluted and PC-3 cells were exposed to 20, 40, and 80 µM concentration and incubated for 24 h. Post-exposure, PC-3 cells showcased a substantial loss of their viability at 20 µM (p < 0.05), moreover, this reduction in cell viability escalated proportionally with an increase in AsA at concentrations of 40 and 80 µM (p < 0.01; p < 0.001) respectively. AsA-impelled loss of cellular viability was also evident from the acridine orange-stained photomicrographs, which was also used to quantify the viable and apoptotic cells using Image J software. Additionally, quantification of ROS within PC-3 cells also exhibited an increase in DCF-DA-mediated fluorescence intensity post-exposure to AsA in a dose-dependent manner. AsA-induced apoptosis in PC-3 cells was shown to be associated with augmented activity of caspase-3 proportionally to the AsA concentrations. Thus, initially, this exploratory study explicated that AsA treatment leads to anti-proliferative effects in PC-3 cells by enhancing oxidative stress and inciting apoptosis en route to onset of nuclear fragmentation.


Assuntos
NF-kappa B/antagonistas & inibidores , Triterpenos Pentacíclicos/farmacologia , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Anti-Infecciosos/farmacologia , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Masculino , NF-kappa B/metabolismo , Células PC-3 , Neoplasias da Próstata/metabolismo , Triterpenos/farmacologia
5.
Drug Deliv ; 28(1): 1626-1636, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34328806

RESUMO

Silk fibroin (SF) is a natural polymeric biomaterial that is widely adopted for the preparation of drug delivery systems. Herein, we aimed to fabricate and characterize SF nanoparticles loaded with the selective estrogen receptor modulator; tamoxifen citrate (TC-SF-NPs) and to assess their in vitro efficacy against breast cancer cell lines (MCF-7 and MDA-MB-231). TC-loaded SF-NPs were characterized for particle size, morphology, entrapment efficiency, and release profile. In addition, we examined the in vitro cytotoxicity of TC-SF-NPs against human breast cancer cell lines and evaluated the anticancer potential of TC-SF-NPs through apoptosis assay and cell cycle analysis. Drug-loaded SF-NPs showed an average particle size of 186.1 ± 5.9 nm and entrapment efficiency of 79.08%. Scanning electron microscopy (SEM) showed the nanoparticles had a spherical morphology with smooth surface. Tamoxifen release from SF-NPs exhibited a biphasic release profile with an initial burst release within the first 6 h and sustained release for 48 h. TC-SF-NPs exerted a dose-dependent cytotoxic effect against breast cancer cell lines. In addition, flow cytometry analysis revealed that cells accumulate in G0/G1 phase, with a concomitant reduction of S- and G2-M-phase cells upon treatment with TC-SF-NPs. Consequently, the potent anticancer activities of TC-SF-NPs against breast cancer cells were mainly attributed to the induction of apoptosis and cell cycle arrest. Our results indicate that SF nanoparticles may represent an attractive nontoxic nanocarrier for the delivery of anticancer drugs.

6.
Life (Basel) ; 11(5)2021 May 05.
Artigo em Inglês | MEDLINE | ID: mdl-34063122

RESUMO

OBJECTIVE: Brain tumors are the most challenging of all tumors and accounts for about 3% of all cancer allied deaths. The aim of the present review is to examine the brain tumor prevalence and treatment modalities available in the Kingdom of Saudi Arabia. It also provides a comprehensive analysis of the application of various nanotechnology-based products for brain cancer treatments along with their prospective future advancements. METHODS: A literature review was performed to identify and summarize the current status of brain cancer in Saudi Arabia and the scope of nanobiotechnology in its treatment. RESULTS: Depending upon the study population data analysis, gliomas, astrocytoma, meningioma, and metastatic cancer have a higher incidence rate in Saudi Arabia than in other countries, and are mostly treated in accordance with conventional treatment modalities for brain cancer. Due to the poor prognosis of cancer, it has an average survival rate of 2 years. Conventional therapy includes surgery, radiotherapy, chemotherapy, and a combination thereof, but these do not control the disease's recurrence. Among the various nanomaterials discussed, liposomes and polymeric nanoformulations have demonstrated encouraging outcomes for facilitated brain cancer treatment. CONCLUSIONS: Nanomaterials possess the capacity to overcome the shortcomings of conventional therapies. Polymer-based nanomaterials have shown encouraging outcomes against brain cancer when amalgamated with other nano-based therapies. Nonetheless, nanomaterials could be devised that possess minimal toxicity towards normal cells or that specifically target tumor cells. In addition, rigorous clinical investigations are warranted to prepare them as an efficient and safe modality for brain cancer therapy.

7.
Metab Brain Dis ; 36(5): 829-847, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33704660

RESUMO

Neurodegeneration-associated dementia disorders (NADDs), namely Alzheimer and Parkinson diseases, are developed by a significant portion of the elderly population globally. Extensive research has provided critical insights into the molecular basis of the pathological advancements of these diseases, but an efficient curative therapy seems elusive. A common attribute of NADDs is neuroinflammation due to a chronic inflammatory response within the central nervous system (CNS), which is primarily modulated by microglia. This response within the CNS is positively regulated by cytokines, chemokines, secondary messengers or cyclic nucleotides, and free radicals. Microglia mediated immune activation is regulated by a positive feedback loop in NADDs. The present review focuses on evaluating the crosstalk between inflammatory mediators and microglia, which aggravates both the clinical progression and extent of NADDs by forming a persistent chronic inflammatory milieu within the CNS. We also discuss the role of the human gut microbiota and its effect on NADDs as well as the suitability of targeting toll-like receptors for an immunotherapeutic intervention targeting the deflation of an inflamed milieu within the CNS.

8.
Sci Total Environ ; 768: 144990, 2021 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-33736303

RESUMO

A rapid increase in world population is leading to the rise in global demand of food and agriculture (agri) products. Nanotechnology and its applications have emerged as one of the most pioneering and promising technology for transforming conventional food and agri industries, with the aim of sustainable farming, improving the food security, quality and safety which could revolutionize the food and agri industries. Current developments in nanotechnology have led to the new paths progressively and bringing the radical changes the way food is perceived throughout the farming, transportation, processing, packaging, storage, monitoring and consumption. This review brings the current updates on novel nanomaterials in food and agri industries. Emphasis is given on the importance of nanotechnological applications, offering complete food solutions from farm to fork; including nutraceutical and functional foods, improving bioavailability, efficiency, nutritional status, nano-additives, food texture, color, taste and packaging. Agricultural sector also witnessed several nano-based products, such as nano-fertilizer, nano-pesticide, nano growth promoters and many more for the development of sustainable farming and crop improvement. Despite of numerous advantages of nanotechnology, there are still toxicity challenges, safety concerns, which needs to be addressed and demands transformations in regulatory policies. Rapid development is projected to transform several foods and agri sectors, with rapid increase in market stake and investment. Government agencies, private research centers as well as academicians are also coming together to explore the benefits of nanotechnology to improve food scarcity in the coming years.

9.
Pharmaceutics ; 13(1)2021 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-33430162

RESUMO

In the present study, the objective was to attain a localized lung delivery of an anti-tubercular fluoroquinolone, moxifloxacin (MXF), targeting the alveolar macrophages through a non-invasive pulmonary route using inhalable microspheres as a dry powder inhaler approach. MXF-loaded poly (lactic-co-glycolic acid) (PLGA) microspheres (MXF-PLGA-MSs) were fabricated by solvent evaporation technique and optimized by using a central composite statistical design. The morphology and particle size, as well as the flowability of the optimized microspheres, were characterized. In addition, the aerosolization performance of the optimized formula was inspected using an Andersen cascade impactor. Furthermore, in vivo fate following intrapulmonary administration of the optimized formula was evaluated. The optimized MXF-PLGA-MSs were spherical in shape with a particle size of 3.16 µm, drug loading of 21.98% and entrapment efficiency of 78.0%. The optimized formula showed a mass median aerodynamic diameter (MMAD) of 2.85 ± 1.04 µm with a favorable fine particle fraction of 72.77 ± 1.73%, suggesting that the powders were suitable for inhalation. Most importantly, in vivo studies revealed that optimized MXF-PLGA-MSs preferentially accumulated in lung tissue as manifested by a two-fold increase in the area under the curve AUC0-24h, compared to plain drug. In addition, optimized MXF-PLGA-MS sustained drug residence in the lung for up to 24 h following inhalation, compared to plain drug. In conclusion, inhalable microspheres of MXF could be a promising therapeutic approach that might aid in the effective eradiation of tuberculosis along with improving patient adherence to the treatment.

10.
Drug Des Devel Ther ; 14: 5325-5336, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33293794

RESUMO

Purpose: The present work aimed at challenging the efficacy of natural gums, karaya and locust bean gum, as matrix-forming polymers for the formulation of sustained-release tablets of diltiazem, a model drug. Methods: Central design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out. Results and Discussion: It was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug-polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile. Conclusion: The results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.


Assuntos
Anti-Hipertensivos/farmacocinética , Produtos Biológicos/química , Diltiazem/farmacocinética , Galactanos/química , Mananas/química , Gomas Vegetais/química , Polímeros/química , Sterculia/química , Animais , Anti-Hipertensivos/química , Diltiazem/química , Liberação Controlada de Fármacos , Coelhos , Propriedades de Superfície , Comprimidos
11.
Pharmaceutics ; 12(12)2020 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-33321953

RESUMO

A paradigm shift in treating the most aggressive and malignant form of glioma is continuously evolving; however, these strategies do not provide a better life and survival index. Currently, neurosurgical debulking, radiotherapy, and chemotherapy are the treatment options available for glioma, but these are non-specific in action. Patients invariably develop resistance to these therapies, leading to recurrence and death. Receptor Tyrosine Kinases (RTKs) are among the most common cell surface proteins in glioma and play a significant role in malignant progression; thus, these are currently being explored as therapeutic targets. RTKs belong to the family of cell surface receptors that are activated by ligands which in turn activates two major downstream signaling pathways via Rapidly Accelerating Sarcoma/mitogen activated protein kinase/extracellular-signal-regulated kinase (Ras/MAPK/ERK) and phosphatidylinositol 3-kinase/a serine/threonine protein kinase/mammalian target of rapamycin (PI3K/AKT/mTOR). These pathways are critically involved in regulating cell proliferation, invasion, metabolism, autophagy, and apoptosis. Dysregulation in these pathways results in uncontrolled glioma cell proliferation, invasion, angiogenesis, and cancer progression. Thus, RTK pathways are considered a potential target in glioma management. This review summarizes the possible risk factors involved in the growth of glioblastoma (GBM). The role of RTKs inhibitors (TKIs) and the intracellular signaling pathways involved, small molecules under clinical trials, and the updates were discussed. We have also compiled information on the outcomes from the various endothelial growth factor receptor (EGFR)-TKIs-based nanoformulations from the preclinical and clinical points of view. Aided by an extensive literature search, we propose the challenges and potential opportunities for future research on EGFR-TKIs-based nanodelivery systems.

12.
Pharmaceutics ; 12(11)2020 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-33212921

RESUMO

Microneedles (MNs) are tiny needle like structures used in drug delivery through layers of the skin. They are non-invasive and are associated with significantly less or no pain at the site of administration to the skin. MNs are excellent in delivering both small and large molecules to the subjects in need thereof. There exist several strategies for drug delivery using MNs, wherein each strategy has its pros and cons. Research in this domain lead to product development and commercialization for clinical use. Additionally, several MN-based products are undergoing clinical trials to evaluate its safety, efficacy, and tolerability. The present review begins by providing bird's-eye view about the general characteristics of MNs followed by providing recent updates in the treatment of cancer using MNs. Particularly, we provide an overview of various aspects namely: anti-cancerous MNs that work based on sensor technology, MNs for treatment of breast cancer, skin carcinoma, prostate cancer, and MNs fabricated by additive manufacturing or 3 dimensional printing for treatment of cancer. Further, the review also provides limitations, safety concerns, and latest updates about the clinical trials on MNs for the treatment of cancer. Furthermore, we also provide a regulatory overview from the "United States Food and Drug Administration" about MNs.

13.
Nanomaterials (Basel) ; 10(10)2020 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-33008104

RESUMO

The purpose of this study was to fabricate biostable inorganic silver nanoparticles (AgNPs) using fresh peel (aqueous) extract of Benincasa hispida. A fast, robust, and eco-friendly approach was used for the synthesis of AgNPs, where bioactive components of peel extract of B. hispida acted as reducing and stabilizing agents. Synthesized AgNPs were characterized using a UV-Vis spectrophotometer, Fourier-transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), and electron microscopy. The synthesized nanoparticles exhibited maximum absorption at 418 nm under the typical AgNPs surface plasmon resonance band range. They depicted a mean size of 26 ± 2 nm with a spherical shape. Their therapeutic prospective was determined by evaluating their antimicrobial and anticancer potential. The bio-synthesized silver nanoparticles exhibited strong antimicrobial activity with minimum inhibitory concentration (MIC 50) values of 14.5, 8.6, 6.063, and 13.4 µg/mL against Staphylococcus aureus (ATCC 25923), Micrococcus luteus (ATCC 14593), Escherichia coli (ATCC 25922), and Klebsiella pneumonia (ATCC 13883), respectively. The biosynthesized AgNPs showed potent in vitro cytotoxicity against human cervical cancer cell line with a half maximal inhibitory concentration (IC50) value of 0.066 µg/mL; however, no cytotoxic effect was observed on normal human primary osteoblasts cell line. This study explored B. hispida extract and confirmed its effectiveness as a promising source in producing AgNPs that could be employed for several therapeutic applications.

14.
Plants (Basel) ; 9(9)2020 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-32967179

RESUMO

SARS-CoV-2 infection (COVID-19) is in focus over all known human diseases, because it is destroying the world economy and social life, with increased mortality rate each day. To date, there is no specific medicine or vaccine available against this pandemic disease. However, the presence of medicinal plants and their bioactive molecules with antiviral properties might also be a successful strategy in order to develop therapeutic agents against SARS-CoV-2 infection. Thus, this review will summarize the available literature and other information/data sources related to antiviral medicinal plants, with possible ethnobotanical evidence in correlation with coronaviruses. The identification of novel antiviral compounds is of critical significance, and medicinal plant based natural compounds are a good source for such discoveries. In depth search and analysis revealed several medicinal plants with excellent efficacy against SARS-CoV-1 and MERS-CoV, which are well-known to act on ACE-2 receptor, 3CLpro and other viral protein targets. In this review, we have consolidated the data of several medicinal plants and their natural bioactive metabolites, which have promising antiviral activities against coronaviruses with detailed modes of action/mechanism. It is concluded that this review will be useful for researchers worldwide and highly recommended for the development of naturally safe and effective therapeutic drugs/agents against SARS-CoV-2 infection, which might be used in therapeutic protocols alone or in combination with chemically synthetized drugs.

15.
AAPS PharmSciTech ; 21(4): 129, 2020 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-32405982

RESUMO

Simvastatin a cholesterol-lowering agent used to treat hypercholesterolemia, coronary heart disease, and dyslipidemia. However, simvastatin (SV) has shown low oral bioavailability in GIT. The main purpose of the work was to develop proliposomal formulations to increase the oral bioavailability of SV. Film deposition on the carrier method has been used to prepare the proliposomes. The proliposomes were assessed for morphology, particulate size, entrapment efficacy, drug-polymer compatibility, in vitro and in vivo studies. FTIR and DSC results revealed no drug-polymer interaction. SEM and XRD analysis conform; proliposomes are spherical, amorphous in nature, so that it enhances the solubility of SV between 15.01 ± 0.026 and 57.80 ± 0.015 µg/mL in pH 7.4 phosphate buffer. The optimised formulation (PL6) shows drug release up to 12 h (99.78 ± 0.067%). The pharmacokinetics of pure SV and SV proliposomes (SVP) in rats were Tmax 2 ± 0.5 and 4 ± 0.7 h, Cmax 10.4 ± 2.921 and 21.18 ± 12.321 µg/mL, AUC0-∞ 67.124 ± 0.23 and 179.75 ± 1.541 µg/mL h, respectively. Optimised SVP shows a significant improvement in the rate and absorption of SV. The optimised formulation showed enhanced oral bioavailability of SV in Albino Wister rats and offers a new technique to improve the poor water-soluble drug absorption in the gastrointestinal system.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos/fisiologia , Inibidores de Hidroximetilglutaril-CoA Redutases/administração & dosagem , Inibidores de Hidroximetilglutaril-CoA Redutases/sangue , Sinvastatina/administração & dosagem , Sinvastatina/sangue , Administração Oral , Animais , Disponibilidade Biológica , Avaliação Pré-Clínica de Medicamentos/métodos , Lipossomos , Masculino , Tamanho da Partícula , Ratos , Solubilidade , Difração de Raios X/métodos
16.
PLoS One ; 15(4): e0232322, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32343748

RESUMO

OBJECTIVES: To determine the factors motivating the consumers towards self-medication, the intended indications and the consumers' perceptions about complications that may arise due to its use. DESIGN: Cross-sectional community based prospective study. PLACE AND DURATION OF STUDY: Community pharmacies located at various locations of Hail, Saudi Arabia from January 2019 to March 2019. METHODS: The subjects of this cross-sectional study were people visiting community pharmacies for self-medication. Data on 663 participants was collected through a validated questionnaire prepared on the basis of WHO guidelines for the regulatory assessment of medicinal products for use in self-medication. Two trained data collectors visited the randomly selected community pharmacies, approached and interviewed the consumers purchasing medicines without prescriptions. Data was entered in SPSS and analyzed using descriptive and inferential analyses (alpha level = 0.05). RESULTS: Out of 663 respondents, 68.6% were university graduates; and 33.9% were healthcare professionals. Consumers preferred self-medication mainly for headache (85.8%), cold and sore throat (80.8%), cough (75.7%) and fever (71.8%) with the justification that these illnesses were minor (90.2%), time saving (82.2%), convenient (74.7%), quicker relief (66.1%), and economical (61.2%). Occupation was significantly associated with the reasons for preferring self-medication (p<0.001). Similarly, age, gender and education were also significantly associated with most of the reasons for opting self-medication. People were quite aware about harmful consequences of self-medication. Multivariate logistic regression analysis showed that the respondents with lower education (AOR = 2.404 [95% CI: 1.579-3.661]), non-healthcare professionals (AOR = 1.712 [95% CI: 1.143-2.565]) and higher monthly income (AOR = 0.376 [95% CI: 0.236-0.599]) preferred self-medication (p <0.001, p = 0.009, p <0.001) respectively. CONCLUSION: Self-medication was prevalent among young university graduate males for minor ailments mainly due to convenience and time saving. Despite people beliefs about the harmful consequences of self-medication, its use was omnipresent particularly among the respondents with lower education, non-healthcare professionals and people with higher monthly income.


Assuntos
Conhecimentos, Atitudes e Prática em Saúde , Automedicação/psicologia , Adolescente , Adulto , Estudos Transversais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Farmácias , Estudos Prospectivos , Arábia Saudita , Inquéritos e Questionários , Adulto Jovem
17.
Pak J Pharm Sci ; 33(6(Supplementary)): 2847-2857, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33879446

RESUMO

Uropathogenic strains belonging to the Enterobacteriaceae family are considered one of factors for urinary tract infections, and type 1 pilus fimbrial adhesin (FimH) and beta lactamase CTX-M-15 play crucial roles in their pathogenesis and resistance. Thus, a promising approach is to explore dual-targeting therapeutic agents that act against both FimH and CTX-M-15. In the present study, active constituents of Nigella sativa were selected on the basis of significant activity against UTIs. Molecular docking was used to target active constituents of Nigella sativa to the active sites of FimH and CTX-M-15; these included thymoquinone, dithymoquinone, carvacrol, p-cymene, thymol, thymohydroquinone and longifolene. Dithymoquinone was found to be the most potent dual inhibitor, with binding energy of -7.01 and -5.38kcal/mol against CTX-M-15 and FimH, respectively; In addition, Dithymoquinone exhibited superior activity compared to positive controls avibactam and heptyl α-D-mannopyranoside. Further molecular dynamic simulation studies were carried out to assess the stability of dithymoquinone-target protein complexes via RMSD, Rg, SASA, hydrogen bond number, and RMSF analysis. Both protein-ligand complexes were conserved and attained equilibrium at around 2.0 to 2.5 ns during 10 ns runs. These results suggest that active constituents of Nigella sativa, particularly dithymoquinone, might represent a plausible therapeutic strategy against resistant uropathogenic bacteria.


Assuntos
Adesinas Bacterianas/efeitos dos fármacos , Enterobacteriaceae/efeitos dos fármacos , Nigella sativa/química , Infecções Urinárias/tratamento farmacológico , Inibidores de beta-Lactamases/farmacologia , beta-Lactamases/efeitos dos fármacos , Aderência Bacteriana/efeitos dos fármacos , Farmacorresistência Bacteriana , Simulação de Acoplamento Molecular , Infecções Urinárias/microbiologia
18.
Biomed Pharmacother ; 107: 7-18, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30075371

RESUMO

Management of bacterial infections of central nervous system is a major challenge for the scientists all over the world. Despite the development of various potential drugs, the issue of central nervous system infections persists in the society. The main constraint is the delivery of drugs across the blood brain barrier and only a few drugs after meeting the stringent criteria could cross the blood brain barrier. On the other hand, certain bacterial pathogens could easily enter the brain by using several factors and mechanisms by crossing the blood brain barriers. Interestingly, in the recent past, gold nanoparticles have shown immense potential to overcome the issues associated with the treatment of central nervous system infections, especially due to their inherent ability to cross the blood brain barrier. Initially, the present review summarized the recent updates on the pathogenesis and factors involved in neurological bacterial infections, including the mechanism used by bacterial pathogens to cross the blood brain barriers. Thereafter, the emphasis of the review was on providing current information on gold nanoparticles pertinent to their applicability for the treatment of neurological infections. After discussing the background of neurological bacterial infections, the characteristic features, antibacterial properties, mechanisms of antibacterial action and ability to cross the blood brain barrier of gold nanoparticles have been summarized. Some of the features of gold nanoparticles that make them an ideal candidate for brain delivery are biocompatibity, stability, ability to get synthesized in different sizes with facile methods, surface affinity towards various functional groups, spontaneous crossing of blood brain barrier without applying any external field and most importantly, easy non-invasive tracing by CT imaging. The current updates on the development of gold nanoparticles based therapeutic strategies for the prevention and treatment of central nervous system infections have been discussed in the present study. However, further investigation would be required to translate these preclinical outcomes into clinical applications. Nevertheless, we could safely state that the information gathered and discussed in the present review would benefit the scientists working in the field of neuro-nanotechnology.


Assuntos
Infecções Bacterianas/terapia , Sistema Nervoso Central/microbiologia , Sistema Nervoso Central/patologia , Ouro/química , Nanopartículas Metálicas/química , Animais , Antibacterianos/uso terapêutico , Barreira Hematoencefálica/patologia , Ouro/toxicidade , Humanos , Nanopartículas Metálicas/toxicidade
19.
Curr Drug Metab ; 19(7): 584-595, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29512451

RESUMO

BACKGROUND: There is a long history of traditional medicine for serving the world population. For the prevention and treatment of cancer, herbal remedies have played a significant role. In this review, we have summarized medicinal herbs from the entire world, including India, that are used traditionally for various cancer treatment. Whenever we talk about cancer treatment, medicinal plants always have been on the priority. OBJECTIVE: In this article, we have summarized the flora used in earlier times and recently identified for pre-clinical anticancer treatment. The present paper is a comprehensive review of different literature sources with discussion being made on the therapeutic value of diverse medicinal herbs in the treatment of various kinds of cancer by using different in vitro cancer cell lines. Countless anticancer plants have been recognized with the help of innovative techniques including isolation and structure elucidation that implement their beneficial effect by increasing the immunity of the body, inducing antioxidant action, endorsing making of shielding enzymes, hindering cancer triggering enzymes and hormones, and exciting DNA restoration mechanism. CONCLUSION: Finally, we have concluded that Argemone mexicana shows maximum anti-cancer activity on various cancer cell lines in comparison to other medicinal plants.


Assuntos
Antineoplásicos/farmacologia , Plantas Medicinais , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Medicina Tradicional , Neoplasias/tratamento farmacológico , Preparações de Plantas/farmacologia
20.
Curr Drug Metab ; 19(12): 1002-1011, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29600757

RESUMO

BACKGROUND: Liver ailments including alcoholic liver disease (ALD), still remain the main reason for morbidity & mortality worldwide. In fact, ALD is a multifactorial disease with complex pathophysiology which is linked to several types of liver damages including steatohepatitis, fibrosis and cirrhosis. METHODS: This review emphasizes on 30 herbal medicinal plants with their extracts studied for protective effect against ALD and current scientific evidence of ALD cure by thirty Indian Materia Medica including Tilia Platyphyllos, Amomum subulatum, Carica papaya, Pogostemon patchouli, Commelina benghalensis, Bacopamonnieri, Pecan nut, Allium cepa, Beta Vulgaris, Adina cordifolia, Ocimum gratissimum, Vernonia amygdalina, Sida veronicaefolia, Chenopodium album, Korean red ginseng, Elephantopus scaber, Tecomella undulata, Prunus armeniaca, Sea tangle (Laminaria japonica), Emblica officinalis, Saccharum officinarum, Cocculus hirsutus, Cassia roxburghii, Zhi-Zi-Da- Huang, Phyllanthus amarus, Aegle marmelos, Agrimonia eupatoria, Flaveria trinervia, Curcuma longa and Garcinia indica. RESULTS: Reduction in oxidative stress, improvement in inflammation, reduction in degeneration of fat and necrosis are some of the mechanisms of action of these medicinal plants observed in alcohol induced in-vivo and in-vitro liver injury models. CONCLUSION: Accordingly, this review provides several evidences which show that these medicinal plants could be used for the treatment and prevention of ALD.


Assuntos
Hepatopatias Alcoólicas/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Plantas Medicinais , Substâncias Protetoras/uso terapêutico , Animais
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