13 research outputs found
Phytosomes as a Possible Nano-Delivery System for Enhanced Oral Bioavailability and Hepatoprotective Activity of Indigofera barberi
No full textIndigofera barberi Gamble, a Fabaceae plant, has traditionally been used to treat skin, renal, and liver problems. Documented phytochemicals include glycosides, steroids, tannins, phenolic compounds, and flavonoids. Its low bioavailability and solubility hinder GI absorption. This study sought to improve Indigofera barberi extract bioavailability by making the ethanolic extract more soluble and absorbable. We optimized Indigofera barberi-loaded phytosomes utilizing solvent evaporation. This study developed IBPCs-NPs, a novel phytosome-nanosuspensions for IB shielding, to improve IB bioavailability and hepatoprotection. In in vivo pharmacokinetic studies, the IBPCs-NP formulation had higher plasma concentration and in vitro dissolution rate. IBPCs-NPs also demonstrated stronger hepatoprotective effects in pharmacodynamic studies. Crystalline variation and IB-phospholipid interactions are also physicochemical features of optimized IBPCs-NPs. The synthesised IB phytosomes were cylindrical, smooth-surfaced, and distinct, with a diameter of 332.52 ± 1.54 nm. According to dissolving trials, the enhanced IB phytosomal formulation released silymarin faster and in greater proportions than pure silymarin, with better water solubility (~360 µg/mL). The optimized silymarin phytosomal formulation normalized antioxidant enzymes and helped CCl4-intoxicated cells. In in vivo experiments, it protected the liver from CCl4-induced hepatotoxicity in rats. The optimized phytosomal formulation enhanced oral silymarin bioavailability compared to pure silymarin. This was shown by six-fold systemic bioavailability. Whole phytosomes may increase water-insoluble phyto-constituent oral bioavailability as phospholipid-based nanocarriers
Studies on statistically optimized binary ethosomal gel encapsulated with Carvedilol: Ex-vivo permeation and Pharmacodynamic assessment in male Wistar albino rats
No full textPharmacological and Phytochemical Evaluation Of Gastric Anti-Ulcer Activity of Parthenium hysterophorus In Different Models
No full textThe cause of ulceration in patients is mainly due to hyper secretion of gastric juice and also due to hyper secretion of pepsin. In traditional system of medicine a number of herbal preparations have been used for the treatment of peptic ulcers. There are various medicinal plants has been used for the treatment of gastrointestinal disorders. In view of this, in present study we have to evaluate the anti-ulcer activity of parathenium hysterophorus. Study was carried out, by using three methods i.e., alcohol, paracetamol and stress induced ulcers in rats pretreated with the doses of 250 mg/kg AQPH and ALPH, 20mg/kg Omeoprazole and 50 mg/kg Ranitidine. To evaluate the antiulcer activity of aqueous and alcoholic extracts of parathenium hysterophorus leaves (AQPH and ALPH) at 250 doses using different experimentally induced gastric ulcer models in rats. Gastric ulcers were induced in rats by 80% alcohol, paracetamol and forced immersion stress induced methods. In alcohol induced ulcer model, paracetamol induced ulcer model and stress induced model the ulcer index was determined. Where as in stress induced ulcers stress plays an important role in ulcerogenesis. In alcohol-induced ulcers, AQPH and ALPH were effective in reducing lesion index and increasing the gastric mucus content. It was also effective in decreasing ulcer index in paracetamol-induced ulcers. All the results obtained with parathenium hysterophorus were dose dependent. The results suggest that AQPH and ALPH possesses significant and dose dependent antiulcer activity. The antiulcer activity of AQPH and ALPH can be attributed to its cytoprotective and antisecretory action.</jats:p
FORMULATION DEVELOPMENT AND EVALUATION OF ALLOPURINOL SOLID DISPERSIONS BY SOLVENT EVAPORATION TECHNIQUE
No full textObjective: The main objective of the research work is to develop and characterize allopurinol (ALPN) solid dispersions with different polymers to enhance solubility, enrich dissolution profile and improve patient compliance.Methods: ALPN solid dispersions were prepared by solvent evaporation technique using various grades of polyethelene glycol (PEG) such as PEG 4000 and PEG 6000 with different ratios like 1:0.5, 1:1, 1:1.5 and 1:2 and after formation of solid dispersions all physicochemical properties were examined.Results: All the formulations were found within the permissible pharmacopoeial limits for various physicochemical parameters. The pre-formulation studies, like Fourier, transform infrared spectroscopy (FTIR) showed the absence of drug-excipient interactions. The solubility and dissolution profiles of the sample were increased with increasing the concentration of ALPN solid dispersions. Solvent evaporation was proved to be a successful technique for the development of stable solid dispersion of ALPN. The dissolution amount percentage of ALPN formulations was found between 39.58±2.5 to 94.95±1.8 % within 60 min.Conclusion: Hence, from the all evaluation studies, it was evident that F1 formulation was the better formulation. F1 formulation (ALPN: PEG 4000 in the ratio of 1:0.5), 94.95±1.8 % drug released within 50 min. Â
Development and evaluation of empagliflozin-loaded solid lipid nanoparticles: Pharmacokinetics and pharmacodynamics for oral delivery
No full textType 2 diabetes mellitus is frequently treated with empagliflozin (EZN), a sodium-glucose cotransporter 2 inhibitor. Solid lipid nanoparticles (SLNs) shield the drug from gastrointestinal breakdown and improve the bioavailability of lipophilic drugs. The aim of the study is to use SLNs to enhance EZN's pharmacokinetics and pharmacodynamics in the treatment of diabetes mellitus. To prepare EZN-loaded SLNs, central composite design (CCD) was employed. The optimized batch (optimized EZN-loaded SLNs) had the desired values of dependent variables Vesicle size (R1), Entrapment Efficiency (R2), and Cumulative Drug Release (CDR) (R3). This was achieved by using analysis of variance (ANOVA) to analyse independent variables such as lipid concentration (X1), surfactant concentration (X2), sonication time (X3), and homogenization speed (X4). F8 exhibited the highest drug entrapment (90.6% ± 2.8%), CDR (89.2 ± 3.6), and average particle size (98.6 ± 2.1 nm) among the 30 distinct formulated formulae (F1–F30). Based on the F-value and p-value, the model was determined to be significant for particle size, entrapment efficiency, and CDR. The actual values of particle size entrapment efficiency and CDR closely matched the projected values of the optimized batch. The in vitro release trials produced a burst release followed by a continuous release. When compared to the EZN solution, the relative bioavailability of EZN-loaded SLNs was 1.2 times higher, indicating superior protection against the gastrointestinal environment. In rats with streptozotocin-induced diabetes mellitus, the optimized EZN-loaded SLNs outperformed the basic drug suspension in terms of antidiabetic efficacy. One promising method for administering EZN in the treatment of diabetes mellitus is by SLNs
Post-operative infection treatment in cardiac surgery: current practices and future directions
No full textAbstract Surgical site infections (SSIs) are a major complication in surgical patients, particularly after cardiac surgeries, where the risk of postoperative infection ranges from 3.5% to 26.8%. Mediastinitis, severe concerns associated with open cardiac surgery, is linked to extreme deaths, increased medical expenses during hospitalization. We investigated the incidence and features of mediastinitis over a twenty-nine-year period as patient demographics and surgical indications evolved. Escherichia coli bloodstream infections (BSIs) contribute to significant mortality (5%–30%), with factors contributing to death remaining unclear, particularly with the rise of ESBL-producing organisms. Infective endocarditis (IE) is an infection that affects the cardiac endocardial layer, may cause valve vegetation, abscesses, and myopericarditis. Postoperative management requires a clinician with a deep understanding of cardiopulmonary function to address complications promptly. Infections of cardiac implanted electronic devices (CIEDs) are catastrophic, causing significant morbidity and mortality. Among CIED complications, infections drastically affect survival rates, require re-intervention, and lengthen hospital stays. Research shows a 1% infection rate within 12 months after CIED surgery. Acute Kidney Injury (AKI) is a common complication following major cardiac surgery, particularly in procedures involving cardiopulmonary bypass (on-pump). AKI significantly increases the risk of chronic kidney disease, cardiovascular complications, and mortality. Advanced age and pre-existing chronic kidney disease are recognized as key risk factors. Sepsis-induced cardiomyopathy (SICM), though primarily a general complication of severe sepsis, can also occur in post-cardiac surgery patients who develop sepsis as a secondary complication. The absence of standardized diagnostic criteria highlights an important knowledge gap and underscores the need for further research to improve recognition and management in this high-risk group. Graphical Abstrac
Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement
No full textAbstract Background Ritonavir is an anti-retroviral protease inhibitor to treat HIV, AIDS infections. Methods The RN-SLNs were prepared by using hot homogenization followed ultrasonication method and optimized by using a two-factor, three-level central composte design (CCD). The independent variables were selected as phospholipids (X1) and type of surfactants (X2), whereas the dependent variables were chosen as percent entrapment efficiency (%EE) (Y1), size of the particle (Y2), and percent cumulative drug release (Y3). Further, the formulated R-SLNs were characterized and in vitro drug release studies were performed. The optimized R-SLNs were subjected to in vivo pharmacokinetic studies. Results The solid lipid soya leccithin showed the maximum solubility of RN (103.34 mg/g) compared to stearic acid (81.44 mg/g), glyceryl monostearate (67.21 mg/g), Gelucire 39/1 (44.22 mg/g), and Compritol 888 ATO (31.23 mg/g). Further, the surfactant blend (Tween 80: Poloxamer 188 (8:2)) showed the maximum entrapment efficiency and was the most suitable surfactant. The optimized RN-SLN formulation showed a particle size of 265.06 ± 5.12 nm, % EE of 86.2 ± 3.16 and cumulative drug release of 94.8 ± 0.16%. In addition, in-vitro drug release studies confirmed a biphasic release pattern, and followed Higuchi’s model. The in vivo pharmacokinetic studies showed an increase in bioavailability by 4.3 folds as compared to marketed formulation. Conclusions The optimized RN-SLNs significantly enhanced the solubility and bioavailability of RN. The results of the present study can become a promising platform for the enhancement of oral bioavailability by novel nano carriers. Graphical abstrac
Retraction: Investigating new bilosomes for ex vivo skin deposition, in vitro characterization, and transdermal delivery of nimodipine
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