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OBJECTIVE: .In this study, we investigated the potential of meloxicam (MLX) developed as transferosomal gel as a novel lipidic drug delivery system to address osteoarthritis (OTA), a degenerative joint disease that causes pain and stiffness. By incorporating meloxicam into a transferosomal gel, our aim was to provide a targeted and efficient delivery system capable of alleviating symptoms and slowing down the progression of OTA. MATERIAL AND METHODS: Classical lipid film hydration technique was utilized to formulate different transferosomal formulations. Different transferosomal formulations were prepared by varying the molar ratio of phospholipon-90H (phosphodylcholine) to DSPE (50:50, 60:40, 70:30, 80:20, and 90:10) and per batch, 80mg of total lipid was used. The quality control parameters such as entrapment efficiency, particle size and morphology, polydispersity and surface electric charge, in vitro drug release, ex vivo permeation and stability were measured. RESULTS: The optimized transferosomal formulations revealed a small vesicle size (121±12nm) and greater MLX entrapment (68.98±2.3%). Transferosomes mediated gel formulation MLX34 displayed pH (6.3±0.2), viscosity (6236±12.3 cps), spreadability (13.77±1.77 gm.cm/sec) and also displayed sustained release pattern of drug release (81.76±7.87% MLX released from Carbopol-934 gel matrix in 24h). MLX34 revealed close to substantial anti-inflammatory response, with â¼81% inhibition of TNF-α in 48h. Physical stability analysis concluded that refrigerator temperature was the preferred temperature to store transferosomal gel. CONCLUSION: MLX loaded transferosomes containing gel improved the skin penetration and therefore resulted into increased inhibition of TNF-α level.
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Anti-Inflamatórios não Esteroides , Liberação Controlada de Fármacos , Géis , Lipossomos , Meloxicam , Osteoartrite , Tiazinas , Tiazóis , Meloxicam/administração & dosagem , Osteoartrite/tratamento farmacológico , Tiazóis/administração & dosagem , Animais , Tiazinas/administração & dosagem , Tiazinas/uso terapêutico , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/uso terapêutico , Tamanho da Partícula , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Absorção Cutânea , Química FarmacêuticaRESUMO
BACKGROUND: India suffers a quarter of the global burden of cervical cancer (CC) but is controllable by taking some precautions. The major issue is the low amount of participation among women in screening and vaccination for disease. The objective of the research is to evaluate knowledge, attitude, and practice (KAP) regarding CC among college going students residing in the Rayalaseema region of Andhra Pradesh-India. MATERIAL AND METHODS: A cross-sectional study was conducted on a total of 380 subjects whose ages ranged from 15 to 25 and older. The questionnaires were circulated through google forms. The socio-demographic variables and KAP levels are represented by descriptive statistics. The Chi-square test is used to determine the relationship between sociodemographic factors and KAP levels. RESULTS: Among 380 subjects, 172 (54.7%) are aware of CC, 71% have poor knowledge, and 20% have good knowledge about CC. More than three-fourths of women 374 (98.4%) are not having regular practice towards CC. CONCLUSION: The awareness about CC is very low in the population, so prevention of CC relies on routine screening, proper vaccination, and treatment. Awareness programs and promoting knowledge about cervical health in social media are required.
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Physical and psychological stress has an inverse relation with male libido and sperm quality. The present study investigates the potential fertility-enhancing properties of Desmodium gangeticum (DG) root extracts in male Wister rats subjected to immobilization-induced stress (SIMB). DG roots were extracted using n-hexane (HEDG), chloroform (CEDG), and water (AEDG). In the pilot study, aphrodisiac protentional was investigated at two doses (125 and 250â¯mgâ¯kg-1) of each extract. In the main study, the HEDG and AEDG at 125 and 250â¯mgâ¯kg-1 were challenged for the stress by immobilization (SIMB), for 6â¯h daily over 28 days. Parameters assessed included aphrodisiac effects, gonadosomatic index (GSI), semen quality, sperm quantity, fructose content, serum hormonal levels, testicular oxidative stress, and testicular histopathology. Additional in silico studies, including the lipid solubility index, molecular docking, molecular dynamics, and SymMap studies were conducted for validation. HEDG demonstrated significant aphrodisiac activity, improved - GSI, sperm quality and quantity, and fructose content, serum testosterone levels, histological changes induced by SIMB in the testes. Swiss ADME studies indicated Gangetin (a pterocarpan) had a high brain permeation index (4.81), a superior docking score (-8.22), and higher glide energy (-42.60), compared with tadalafil (-7.17). The 'Lig fit Prot' plot in molecular dynamics simulations revealed a strong alignment between Gangetin and phosphodiesterase type 5 (PDE5). HEDG exerts aphrodisiac effects by increasing blood testosterone levels and affecting PDE5 activity. The protective effects on spermatozoa-related parameters and testicular histological changes are attributed to the antioxidant and anti-inflammatory properties, of pterocarpan (gangetin).
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Afrodisíacos , Infertilidade Masculina , Pterocarpanos , Ratos , Masculino , Animais , Humanos , Afrodisíacos/farmacologia , Ratos Wistar , Análise do Sêmen , Projetos Piloto , Simulação de Acoplamento Molecular , Pterocarpanos/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo , Sêmen , Testículo , Estresse Oxidativo , Infertilidade Masculina/tratamento farmacológico , Infertilidade Masculina/etiologia , Infertilidade Masculina/metabolismo , Testosterona , Frutose/metabolismoRESUMO
Hypothalamus is central to food intake and satiety. Recent data unveiled the expression of N-methyl-D-aspartate receptors (NMDAR) on hypothalamic neurons and their interaction with GABAA and serotoninergic neuronal circuits. However, the precise mechanisms governing energy homeostasis remain elusive. Notably, in females, the consumption of progesterone-containing preparations, such as hormonal replacement therapy and birth control pills, has been associated with hyperphagia and obesity-effects mediated through the hypothalamus. To elucidate this phenomenon, we employed the progesterone-induced obesity model in female Swiss albino mice. Four NMDAR modulators were selected viz. dextromethorphan (Dxt), minocycline, d-aspartate, and cycloserine. Obesity was induced in female mice by progesterone administration for 4 weeks. Mice were allocated into 7 groups, group-1 as vehicle control (arachis oil), group-2 (progesterone + arachis oil), and group-3 as positive-control (progesterone + sibutramine); other groups were treated with test drugs + progesterone. Various parameters were recorded like food intake, thermogenesis, serum lipids, insulin, AST and ALT levels, organ-to-body weight ratio, total body fat, adiposity index, brain serotonin levels, histology of liver, kidney, and sizing of fat cells. Dxt-treated group has shown a significant downturn in body weight (p < 0.05) by a decline in food intake (p < 0.01), organ-to-liver ratio (p < 0.001), adiposity index (p < 0.01), and a rise in body temperature and brain serotonin level (p < 0.001). Dxt demonstrated anti-obesity effects by multiple mechanisms including interaction with hypothalamic GABAA channels and anti-inflammatory and free radical scavenging effects, improving the brain serotonin levels, and increasing insulin release from the pancreatic ß-cells.
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Insulinas , N-Metilaspartato , Feminino , Camundongos , Animais , N-Metilaspartato/farmacologia , Receptores de N-Metil-D-Aspartato/metabolismo , Serotonina/metabolismo , Progesterona/farmacologia , Óleo de Amendoim/metabolismo , Óleo de Amendoim/farmacologia , Óleo de Amendoim/uso terapêutico , Obesidade/tratamento farmacológico , Obesidade/metabolismo , Hipotálamo , Insulinas/metabolismo , Insulinas/farmacologia , Insulinas/uso terapêutico , Ácido gama-AminobutíricoRESUMO
OBJECTIVE: This investigation aimed to explore the potential of non-ionic surfactant based niosomal vesicles encapsulating tenoxicam (TN; anti-rheumatic drug) for the treatment of rheumatic diseases. MATERIAL AND METHODS: Mechanical dispersion technique with controlled pressure was employed to prepare different niosomal formulations. The effects of different ratios of surfactant (span-60), lipid, and sodium deoxycholate on noisome's physicochemical properties have been examined. Moreover, inhibition of TNF-α in lipopolysaccharide-activated cultured Human leukemia monocytic (THP-1) cells were demonstrated to assess the in vitro inflammation profile. Finally, the optimized niosomal formulation (TN3) was prepared in gel matrix consist of carbopol 934 (termed as TN34) and stability was also tested at 4±2 ÌC, 25±2 ÌC, 37±2 ÌC and 45±2 ÌC for 6 months. RESULTS: The optimized niosomal formulation exhibited a small vesicle size (165±14nm) and high drug encapsulation (79.64±1.5%). Niosomal gel formulation TN34 showed pH (6.7), viscosity (6810±3.34 cps), spreadability (19.11±1.87gm.cm/sec) and also displayed sustained release pattern of drug release (98.16±0.07% TN released from gel matrix in 24h) in vitro release study. TN34 exhibited substantial anti-inflammatory response, with â¼75% inhibition of TNF-α in 48h. Stability investigation revealed that refrigerator temperature is most suitable for the storage of niosomal gel. CONCLUSION: Transdermal niosomal formulation displayed promising potential in the treatment of rheumatic diseases.
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OBJECTIVE: Lamotrigine (LTG) an anticonvulsant drug with a dissociation constant (pKa: 5.7), suffers from enhanced blood plasma spike after each dose, when administered as fast release tablet. Being BCS class-II candidate and pH dependent solubility, development of release-controlled tablets of LTG is a major challenge. This investigation aims at designing the release-controlled tablet (RCT) formulation of LTG using a solid dispersion (SD) technique via addressing its solubility and release problems. MATERIAL AND METHODS: RCT of LTG was fabricated using SD blend of Eudragit RL and Eudragit RS and PVP K-30 with different polymer blend ratio (1:5 and 1:7). The optimization of RCT of LTG was performed using D-optimal mixture design with three independent variables, three response variables, and one constraint. The dissolution rate was determined and data were then fitted to different mathematical models. Scanning electron microscopy (SEM) and X-ray diffraction (XRD) studies and tableting parameters were analyzed. RESULT: In vitro studies of predicted optimized batches (POBs) have shown that drug release over a period of 12hours was 88.05±3.4% in media I, 86.10±3.7% in media II and 85.84±4.2% in media III. An in vitro kinetic model equating R2-value for all the tested models indicated that the first order and Higuchi release kinetics model were the most appropriate. CONCLUSION: Based on the optimized formulation consisting of SD of LTG with Eudragit RL, Eudragit RS and PVP K-30, the release rate was consistently similar throughout the GI tract, regardless of the pH of the environment.
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Biogenic nanoparticle production is in demand as it is secure, has great promise, and is environmental friendly. This study aimed at green synthesis, characterization, and evaluation of Terminalia arjuna selenium nanoparticles (TA-SeNPs) for their antioxidant, antibacterial, anticancer activities, and their incorporation in gel for biomedical applications. The bio-reduction attributes of the T. arjuna (TA) bark extract were utilized to fabricate selenium nanoparticles. The TA bark extract is abundant in phenolics (193.63 ± 1.61 mg gallic acid equivalents/g), flavonoids (88.23 ± 0.39 mg quercetin equivalents/g), and tannins (109.46 ± 1.16 mg catechin equivalents/g), which perform as effective capping and stabilizing agents, thus enabling the fabrication of stable SeNPs. The fabrication of TA-SeNPs was corroborated by UV-visible spectra, which exhibited surface plasmon resonance at 291 nm. Transmission electron microscopy (TEM) and scanning electron microscopy (SEM) demonstrated nano-sized spherical TA-SeNPs with an average diameter ranging from 100 to 150 nm. Zeta potential analysis revealed that TA-SeNPs were negatively charged (-26.1 mV). X-ray diffraction presented amorphous TA-SeNPs with a quantification of 82.36 ± 10.2 µg/mL resulting from ICP-AES. The IC50 45.18 ± 0.11 µg/mL for the DPPH assay and 66.51% reducing power capacity values indicated that the TA-SeNPs possessed excellent radical scavenging efficacy. Moreover, the TA-SeNPs exhibited a broad spectrum of antimicrobial activity against potential pathogens. Additionally, the TA-SeNPs exhibited a dose-dependent cytotoxic effect on the MCF-7 breast cancer cell line, with an IC50 of 23.41 µg/mL. Furthermore, the TA-SeNP-incorporated gel showed excellent spreadability, extrudability, and consistency with retention of antimicrobial properties and hydrophilic contact angle. As an outcome, TA-SeNPs offer the possibility of the formulation and growth of sustainably designed green SeNPs that can be produced, conserved, and marketed securely across the globe.
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The main objective of this review is to provide a comprehensive overview of the current evidence regarding the use of chitosan-based hydrogels to manage skin infections. Chitosan, a naturally occurring polysaccharide derived from chitin, possesses inherent antimicrobial properties, making it a promising candidate for treating various dermal infections. This review follows a systematic approach to analyze relevant studies that have investigated the effectiveness of chitosan-based hydrogels in the context of dermal infections. By examining the available evidence, this review aims to evaluate these hydrogels' overall efficacy, safety, and potential applications for managing dermal infections. This review's primary focus is to gather and analyze data from different recent studies about chitosan-based hydrogels combating dermal infections; this includes assessing their ability to inhibit the growth of microorganisms and reduce infection-related symptoms. Furthermore, this review also considers the safety profile of chitosan-based hydrogels, examining any potential adverse effects associated with their use. This evaluation is crucial to ensure that these hydrogels can be safely utilized in the management of dermal infections without causing harm to patients. The review aims to provide healthcare professionals and researchers with a comprehensive understanding of the current evidence regarding the use of chitosan-based hydrogels for dermal infection management. The findings from this review can contribute to informed decision-making and the development of potential treatment strategies in this field.
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In the 21st century, melanoma and non-melanoma skin cancers have become an epidemic outbreak worldwide. Therefore, the exploration of all potential preventative and therapeutic measures based on either physical or bio-chemical mechanisms is essential via understanding precise pathophysiological pathways (Mitogen-activated protein kinase, Phosphatidylinositol 3-kinase Pathway, and Notch signaling pathway) and other aspects of such skin malignancies. Nano-gel, a three-dimensional polymeric cross-linked porous hydrogel having a diameter of 20-200 nm, possesses dual properties of both hydrogel and nanoparticle. The capacity of high drug entrapment efficiency with greater thermodynamic stability, remarkable solubilization potential, and swelling behavior of nano-gel becomes a promising candidate as a targeted drug delivery system in the treatment of skin cancer. Nano-gel can be either synthetically or architectonically modified for responding to either internal or external stimuli, including radiation, ultrasound, enzyme, magnetic, pH, temperature, and oxidation-reduction to achieve controlled release of pharmaceuticals and several bio-active molecules such as proteins, peptides, genes via amplifying drug aggregation in the active targeted tissue and reducing adverse pharmacological effects. Several drugs, such as anti-neoplastic biomolecules having short biological half-lives and prompt enzyme degradability capacity, must be appropriate for administration employing either chemically bridged or physically constructed nano-gel frameworks. The comprehensive review summarizes the advancement in the preparation and characterization methods of targeted nano-gel with enhanced pharmacological potential and preserved intracellular safety limits for the mitigation of skin malignancies with a special emphasize on skin cancer inducing pathophysiological pathways and prospective research opportunities for skin malignancy targeted nano-gels.
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BACKGROUND: Doxorubicin (DOX) is the most active cytotoxic agents having efficacy in malignancies either alone or combined with other cytocidal agents. The clinical usefulness of the anthracycline drug has been precluded by cardiac toxicity. Many therapeutic interventions have been attempted to improve the therapeutic benefits of the drug. This study is based on the possible protective effects of combination of p-coumaric acid (PC) and naringenin (NR) on DOX induced cardiac toxicity in male Swiss albino rats. METHODS: Total nine groups of Swiss albino rats were used, Group I (vehicle control) receive saline solution daily and Group II (disease control) receive saline solution daily up to 29(th) day and at 30(th) day a single dose of DOX (15 mg/kg i.p.) is given. PC alone (100 mg/kg/day p.o.) and (200 mg/kg/day p.o.) also NR alone (15 mg/kg/day) orally administer for 30 days. Similarly a standard drug Vit. E (100 mg/kg/day) administers alone for 30 days. Group PC/DOX and PC and NR/DOX receive PC (200 mg/kg/day) and combine PC (200 mg/kg/day). RESULTS: Doxorubicin induced marked biochemical alterations characteristic of cardiac toxicity including increase in MDA level and decrease SOD, CAT & GSH level but prior administration of combination of PC & NR ahead of doxorubicin challenge ameliorated all these biochemical markers. CONCLUSION: The study proves the beneficial effects of combination of PC and NR in protecting animal against DOX induced cardiotoxicity.
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The whole plant of Stellaria media (family: Caryophyllaceae) has been tested for its antiobesity activity by using progesterone-induced obesity model in female albino mice. The effect of S. media on food consumption pattern, change in body weight, thermogenesis, lipid metabolism, and histology of fat pad. were examined. Methanolic and alcoholic extracts of the S. media were used in the study. Methanolic extract of S. media (MESM) have prevented the increase in body weight, adipose tissue weight and size, and upturned obesity and associated complications. MESM has also shown promising effects compared with alcoholic extract of S. media may be because of its multiple mechanisms. These findings suggest that antiobesity activity produced by MESM is because of its anorexic property mediated by saponin and flavonoid and partly of by its ß-sitosterol content. ß-Sitosterol in the plant extract was confirmed by thin-layer chromatography study. ß-sitosterol is plant sterol having structural similarity with dietary fat which do the physical competition in the gastrointestinal tract and reduces fat absorption. Before carrying in vivo activity detail pharmacognostic and phytochemical analysis of the extracts was carried out. The plant has shown the presence of saponin, flavonoids, steroids and triterpenoids, glycosides, and anthocynidine. By this study, it can be concluded that, MESM is beneficial in suppression of obesity induced by progesterone.