Formulation and evaluation of biodegradable microspheres of tinidazole

The aim of present study is to develop biodegradable microspheres of Tinidazole. Bovine Serum Albumin was used for the preparation of microspheres. They were made in four batches. The emulsion cross-linking method was used for the preparation. The quantity of BSA varies for each formulation. Formulations were evaluated for particle size, Melting point, TLC, entrapment efficiency and in vitro release studies. Depending upon the drug to polymer ratio, the entrapment, loading were found to range between 48, 55, 75 and 78 (in %) respectively. Particle size of prepared microspheres was measured using a compound microscope. The surface topography and internal textures of the microspheres was observed by scanning electron microscopy. The microspheres were spherical, discrete and compact and size distribution was between 33.28 to 36.25 μm. In vitro studies were carried out at different pH for a period of 18 h and compared with marketed formulation. From all the batches it is concluded that when concentration of polymer increases microspheres shows more controlled and prolonged release. The drug release was between 66, 51, 48, 42 (in %). The drug release from 1:4 is most prolonged and constant. Both the IR spectra of drug and formulation were almost same. Combination multitone recorded due to N=O stretching and S=O in the IR region of 1500-1250 cm−1.Keywords: Biodegradable microspheres, BSA, Tinidazole, In vitro release.IntroductionMicrosphere

Formulation and evaluation of biodegradable microspheres of tinidazole

The aim of present study is to develop biodegradable microspheres of Tinidazole. Bovine Serum Albumin was used for the preparation of microspheres. They were made in four batches. The emulsion cross-linking method was used for the preparation. The quantity of BSA varies for each formulation. Formulations were evaluated for particle size, Melting point, TLC, entrapment efficiency and in vitro release studies. Depending upon the drug to polymer ratio, the entrapment, loading were found to range between 48, 55, 75 and 78 (in %) respectively. Particle size of prepared microspheres was measured using a compound microscope. The surface topography and internal textures of the microspheres was observed by scanning electron microscopy. The microspheres were spherical, discrete and compact and size distribution was between 33.28 to 36.25 μm. In vitro studies were carried out at different pH for a period of 18 h and compared with marketed formulation. From all the batches it is concluded that when concentration of polymer increases microspheres shows more controlled and prolonged release. The drug release was between 66, 51, 48, 42 (in %). The drug release from 1:4 is most prolonged and constant. Both the IR spectra of drug and formulation were almost same. Combination multitone recorded due to N=O stretching and S=O in the IR region of 1500-1250 cm−1.Keywords: Biodegradable microspheres, BSA, Tinidazole, In vitro release.IntroductionMicrosphere

Formulation, Optimization and Evaluation of Eudragit RL 100 nanoparticles loaded with Quercetin for its Hypolipidemic action by using Animal Model

Quercetin, a potent pharmacological active phytocompound, plays a crucial role in drug therapy. However, its essential role is limited due to poor water solubility and low bioavailability. To overcome these limitations and enhance oral bioavailability, Quercetin loaded Eudragit nanoparticles were prepared using a single emulsification solvent evaporation method and optimized by applying Box-Behnken design. This study aimed to investigate the anti-hyperlipidemic potential of Quercetin in Triton WR-1339 induced hyperlipidemic rats. Hyperlipidemia was induced in rats using Triton WR-1339, and the hypolipidemic potential of Quercetin was evaluated at doses of 50 and 100 mg/kg. The results revealed that Quercetin significantly (p ≤ 0.005) altered the serum levels of total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol, and high-density lipoprotein cholesterol, bringing them close to normal levels in Triton WR-1339 induced hyperlipidemic rats. Furthermore, both doses of Quercetin (50 and 100 mg/kg) showed significant reductions in TC and TG levels when compared to the standard atorvastatin treatment. The novel formulation of Quercetin loaded Eudragit polymeric nanoparticles displayed remarkable potential as a green antihyperlipidemic agent. These findings suggest that Quercetin loaded Eudragit nanoparticles can effectively mitigate hyperlipidemia and have the potential to be a promising therapeutic option for lipid disorders. The enhanced bioavailability and bioactivity of Quercetin delivered through this novel formulation open new possibilities for its clinical application in managing hyperlipidemia. Further research and clinical studies are warranted to explore its translational potential and wider applications in drug therap

Clinical Importance of FNDC-5 and Selectin-E mRNA Expression Among Type 2 Diabetics with and without Obesity

Background: Type 2 diabetes mellitus (T2DM) is growing illnesses associated with metabolic dysregulation such as obesity affecting a large population become leading causes of death worldwide. Fibronectin type III domain-containing protein 5 (FNDC-5) and selectin-E were suggested to have effects on metabolism and diabetes, therefore present study aimed to evaluate the clinical importance of FNDC-5 and selectin-E among the T2DM patients with and without obesity. Methods: Study included cohort of 200 T2DM patients with and without obesity. We evaluated FNDC-5, selectin-E mRNA expression as well as vitamin-D, and vitamin-B12 levels in among the T2DM patients with and without obesity. Results: Study observed significant difference in biochemical parameters included in study. T2DM patients with obesity had significantly higher fasting blood glucose levels (p\u3c0.0001) and HbA1c (glycated hemoglobin) (p\u3c0.0001) compared to those T2DM patients without obesity. T2DM patients with obesity also had higher systolic blood pressure (p=0.001), LDL (low density lipoprotein) (p=0.02), TG (triglycerides) (p=0.02) and cholesterol (p=0.01) compared to T2DM patients without obesity. The mRNA expression of FNDC-5 (p\u3c0.0001) was lower in T2DM patients with obesity compared to T2DM patients without obesity. It was observed that the T2DM patients with vitamin-D deficiency had significantly lower FNDC-5 mRNA expression (p=0.03) when compared with those with sufficient vitamin-D level. T2DM patients with clinically normal vitamin-B12 level expressed 0.60 fold FNDC-5 mRNA expression while B12 deficient T2DM patients had 0.28 fold FNDC-5 mRNA expression (p=0.005). No as such significant association was was observed with selectin-E. A negative correlation of FNDC-5 mRNA expression with Post prandial glucose (mg/dl) (p=0.04) and TG (mg/dl) (p=0.02) was observed. Conclusion: FNDC-5 down regulation was observed with T2DM with obesity, vitamin-D and vitamin-B12 deficiency suggesting obesity, vitamin-D and vitamin-B12 deficiency could be the factor for FNDC-5 down-regulation leading to worseness or progression of disease. We suggest that FNDC-5 down-regulation could be used as an indicator for T2DM worseness and development of other associated complications

Phytochemistry, Pharmacology and Molecular Mechanisms of Herbal Bioactive Compounds for Sickness Behaviour

The host’s response to acute infections or tissue injury is a sophisticated and coordinated adaptive modification called sickness behaviour. Many herbs have been studied for their ability to protect animals against experimentally induced sickness behaviour. However, there is a lack of knowledge and experimental evidence on the use of herbal bioactive compounds (HBACs) in the management of sick behaviour. The goal of this review is to provide a concise summary of the protective benefits and putative mechanisms of action of phytochemicals on the reduction of lipopolysaccharide (LPS)-induced sickness behaviour. Relevant studies were gathered from the search engines Scopus, ScienceDirect, PubMed, Google Scholar, and other scientific databases (between 2000 and to date). The keywords used for the search included “Lipopolysaccharide” OR “LPS” OR “Sickness behaviour” OR “Sickness” AND “Bioactive compounds” OR “Herbal medicine” OR “Herbal drug” OR “Natural products” OR “Isolated compounds”. A total of 41 published articles that represented data on the effect of HBACs in LPS-induced sickness behaviour were reviewed and summarised systemically. There were 33 studies that were conducted in mice and 8 studies in rats. A total of 34 HBACs have had their effects against LPS-induced changes in behaviour and biochemistry investigated. In this review, we examined 34 herbal bioactive components that have been tested in animal models to see if they can fight LPS-induced sickness behaviour. Future research should concentrate on the efficacy, safety, and dosage needed to protect against illness behaviour in humans, because there is a critical shortage of data in this area

Hepatitis B Virus-Encoded HBsAg Contributes to Hepatocarcinogenesis by Inducing the Oncogenic Long Noncoding RNA LINC00665 through the NF-κB Pathway

Clinical and in vivo studies have demonstrated a role for hepatitis B virus (HBV)-encoded HBsAg (hepatitis B surface antigen) in HBV-related hepatocellular carcinoma (HCC); however, the underlying mechanisms remain largely unknown. Here, we investigated the role of HBsAg in regulating long noncoding RNAs (lncRNAs) involved in HCC progression. Our analysis of microarray data sets identified LINC00665 as an HBsAg-regulated lncRNA. Furthermore, LINC00665 is upregulated in liver samples from HBV-infected patients as well as in HCC, specifically in HBV-related HCC liver samples. These findings were supported by our in vitro data demonstrating that HBsAg, as well as HBV, positively regulates LINC00665 in multiple HBV cell culture models. Next, we evaluated the oncogenic potential of LINC00665 by its overexpression and CRISPR interference (CRISPRi)-based knockdown in various cell-based assays. LINC00665 promoted cell proliferation, migration, and colony formation but inhibited cell apoptosis in vitro. We then identified the underlying mechanism of HBsAg-mediated regulation of LINC00665. We used immunofluorescence assays to show that HBsAg enhanced the nuclear translocation of NF-κB factors in HepG2 cells, confirming that HBsAg activates NF-κB. Inhibition of NF-κB signaling nullified HBsAg-mediated LINC00665 upregulation, suggesting that HBsAg acts through NF-κB to regulate LINC00665. Furthermore, the LINC00665 promoter contains NF-κB binding sites, and their disruption abrogated HBsAg-induced LINC00665 upregulation. Finally, HBsAg facilitated the enrichment of the NF-κB factors NF-κB1, RelA, and c-Rel in the LINC00665 promoter. Taken together, this work shows that HBsAg can drive hepatocarcinogenesis by upregulating oncogenic LINC000665 through the NF-κB pathway, thereby identifying a novel mechanism in HBV-related HCC. IMPORTANCE Hepatitis B virus (HBV) is a major risk factor for hepatocellular carcinoma (HCC). Numerous reports indicate an oncogenic role for HBV-encoded HBsAg; however, the underlying mechanisms are not well understood. Here, we studied the role of HBsAg in regulating lncRNAs involved in hepatocarcinogenesis. We demonstrate that HBsAg, as well as HBV, positively regulates oncogenic lncRNA LINC00665. The clinical significance of this lncRNA is highlighted by our observation that LINC00665 is upregulated in liver samples during HBV infection and HBV-related HCC. Furthermore, we show LINC00665 can drive hepatocarcinogenesis by promoting cell proliferation, colony formation, and cell migration and inhibiting apoptosis. Taken together, this work identified LINC00665 as a novel gene through which HBsAg can drive hepatocarcinogenesis. Finally, we show that HBsAg enhances LINC00665 levels in hepatocytes by activating the NF-κB pathway, thereby identifying a novel mechanism by which HBV may contribute to HCC.ISSN:2165-049