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Self microemulsifying formulation is an approach used for enhancing the bioavailability of poorly soluble molecules due to their lipidic nature and small particle size. The objective of the present study was to evaluate the hepatoprotective activity of poorly soluble hydroxy- and polyhydroxy-organic phytomolecules rich Lagerstroemia speciosa leaves extract in modern formulation i.e. “Self microemulsifying System”. Different doses of SME (Self microemulsifying) formulation of L. speciosa leaves extract were evaluated for the hepatoprotective activity against carbon tetrachloride induced liver toxicity in rats. The parameters evaluated were (a) biochemical parameters like serum enzymes: aspartate aminotransferase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (ALP) and total bilirubin (b) liver antioxidant parameters as estimation of Lipid peroxidation (LPO), catalase (CAT), Superoxide dismutase (SOD) activity and concentration of reduced glutathione (GSH). Oral administration of SME formulation provided the significant protection in marker enzyme of treated group at 100 mg/kg, p.o. as AST (P

Background: Lagerstroemia speciosa (SEL) leaves are a popular folk medicine for diabetes treatment due to presence of corosolic acid. It has low water solubility resulting poor absorption after oral administration. Self micro-emulsified drug delivery system is the way by which we can improve the oral absorption of drug. Objective: The objective of this study was to develop the self micro-emulsifying formulation of standardized extract of SEL leaves and evaluate its pharmacodynamic performance for antidiabetic activity. Materials and methods: The SME formulation was prepared by using sefsol-218 as oil, cremophor-EL as surfactant and transcutol-P as co-surfactant. The ratio of surfactant and co-surfactant was determined by pseudoternary phase diagram. SME formulations were characterized for dilution at different pH, self emulsification, optical clarity, globule size and thermodynamic stability. Pharmacodynamic evaluation of formulations was assessed in Wistar rats by using parameters viz. blood glucose level and serum lipid profile. Results: SEL loaded SME formulation was successfully developed by using sefsol-218, cremophor-EL and transcutol-P with a droplet size 23.53 nm. Pharmacodynamic results showed a higher reduction in blood glucose by SME formulation than SEL without SMES respectively at 50 mg/kg dose while reduction produced at dose of 100 mg/kg was found significant and better on 15th day of study. The percentage reduction produced by SME formulation on serum lipid profile was also significant and was more prominent than SEL. Conclusion: This study confirms that the formulation elevates the pharmacodynamic performance of SEL approximately two fold. Keywords: Self micro-emulsifying formulation, Lagerstroemia speciosa, antidiabetic activity

This research is dedicated to the creation and analysis of Chitosan Nanoparticles loaded with Busulfan for potential medical applications. The main goal was to produce nanoparticles with specific physical and chemical properties and a sustained release of the drug. Nine different formulations (CNB-1 to CNB-9) were developed using varying concentrations of chitosan and tripolyphosphate (TPP) via a method called ionic gelation. The nanoparticles underwent extensive testing for their size distribution, electrical charge, drug entrapment efficiency, drug content, and how the drug was released over time in vitro. The results showed that CNB-4 had the most desirable characteristics, with an average size of 172 ± 2 nanometers, a slight positive charge (4 ± 1 millivolts), high drug entrapment, and a slow release of the drug over 24 hours. Further examination using techniques like Differential Scanning Calorimetry (DSC) and Atomic Force Microscopy (AFM) confirmed that CNB4 was successfully formed and had a solid structure. DSC analysis showed no interactions between the drug and the polymer, while AFM images displayed dense, spherical nanoparticles. Over the course of 24 hours, CNB-4 released almost 90% of the therapeutic payload, according to in vitro release assays, demonstrating a continuous release of the medication. Statistical analysis revealed a strong correlation between the physical and chemical properties of the formulations and their release rates. In conclusion, CNB-4's favourable features made it an attractive prospect for controlled drug delivery in treatment for cancer. The findings of this study can be used to enhance drug delivery systems that rely on nanoparticles and to better understand how to optimise formulation parameters to achieve desired therapeutic effects. [ABSTRACT FROM AUTHOR]

Background: Breast cancer is one of the leading causes of cancer-related death among females in the world. Sesamol, which is an herbal phenolic compound, is investigated for its powerful antioxidant and anticancer motility. Sesamol induces growth arrest and apoptosis in malignant cells. However, its pharmaceutical significance is limited due to poor bioavailability. The self nanoemulsifying drug delivery system (SNEDDS) is a type of lipid nanocarrier system that is suitable for the encapsulation of lipophilic drug molecules. Objectives: In the present study, Sesamol-loaded SNEDDS were developed, identified, and assessed for the enhancement of its in vitro dissolution rate and anticancer efficacy. Materials and Methods: Based on the solubilization potential of sesamol, the oil (Isopropyl myristate, Isopropyl palmitate, Caprylic capric triglycerides, Sesame oil) surfactant (Span 80, and Tween 80), and cosurfactant (Poly Ethylene Glycol 400) were chosen for the formulation of Sesamol-loaded SNEDDS. SNEDDS were prepared by an aqueous titration technique. Developed formulations were characterized and assessed for thermodynamic stability, self nanoemulsification efficiency, droplet size, polydispersity index, zeta potential, surface morphology, refractive index, the percent of transmittance, and drug release profile. Results: In vitro dissolution rate of Sesamol was significantly enhanced from the optimized formulation in comparison with pure drug. The finalized formulation was selected for in vitro anticancer effects in human breast cancer cells (MCF-7) by 3-(4,5-dimethylthiazol-2-yl)-2,5-Diphenyl Tetrazolium Bromide (MTT) assay. MTT assay suggested remarkable anticancer efficacy of finalized Sesamol-loaded SNEDDS against MCF-7 cells compared with standard (Marketed preparation). Conclusion: The outcome of this study revealed the incredible potential of SNEDDS in the enhancement of in vitro dissolution rate and anticancer efficacy of the poorly soluble drug. [ABSTRACT FROM AUTHOR]

Ziziphus mauritiana (Rhamnaceae), commonly known as Indian jujube, is a pharmacologically diverse medicinal plant. A plethora of active phytochemical constituents of this plant has been revealed so far, namely, berberine, quercetin, kaempferol, sitosterol, stigmasterol, lanosterol, diosgenin, and so forth. Several studies demonstrated the exploration of pharmacological potential of various parts such as fruits, leaves, and stems of the plant as antioxidant, cytotoxic, antimicrobial, anti‐diarrhoeal, antidepressant, immunomodulator, and hepatoprotective. This review gives a unique summary including phytochemistry, nutritional value, and significant pharmacological importance of Z. mauritiana. The literature search was carried out via search engine PubMed, Science Direct, and so on. The data were heterogeneous in terms of leaves, stem, roots, and fruits which were used for different experimental findings, which made the comparison a lengthy task. Study findings suggested that the extracts from this plant may possess numerous types of pharmacological activities. As the search for novel drugs from botanical sources continues, there is need for future investigations to isolate and characterize pharmacologically active agents that confer medicinal properties on Z. mauritiana, as well as to elucidate the structures of these agents by which they exert their healing properties and to scientifically validate the existing traditional practices concerning its health benefits. [ABSTRACT FROM AUTHOR]

Objective:To evaluate hepatoprotective activity along with hematological and defensive recital of Trichosanthes dioica Roxb against simvastatin induced hepatotoxicity in experimental rodents. Methods: In the present study, in- vivo hepatoprotective effect of 50% methanolic fruit extract of Trichosanthes dioica Roxb (TME 200 and 400 mg/kg body weight) was evaluated using experimental model, simvastatin (20 mg/kg, p.o.), induced hepatotoxicity in experimental animals. The hepatoprotective activity was estimatedby interpreting using various biochemical parameters like SGOT, SGPT, ALP, total bilirubin, total protein and albumin along with the haematological and histopathological studies. Results: The treatment with TME significantly (P<0.05-P<0.001) and dose-dependently reversed simvastatin induced elevation in serum level ofSGOT, SGPT, ALP, total bilirubin and restored the total protein and albumin level. Furthermore, TME also signify the blood parameters at dose of 1000 and 2000 mg/kg and restored the body defense mechanism. The histological examination revealed that TME at dose of 200 mg/kg showed regeneration of hepatocytes around central vein with near normal liver architecture. Conclusion: The results of this study exhibited liver protective effect of Trichosanthes dioica Roxb against simvastatin induced liver injury and there by scientifically support its traditional use. [ABSTRACT FROM AUTHOR]

Piper sylvaticum Roxb. is an important folk medicine in Indian Traditional System of Medicine widely used by different tribes in many countries. In the present study, the Antioxidant, Cytotoxic and Hepatoprotective activities of extract/fractions of Piper sylvaticum roots were investigated. 70% ethanolic extract of Piper sylvaticum roots were successively extracted using hexane and ethyl acetate to prepare various fractions. Total phenol content was found maximum 324.65 mg/GAE/g in ethyl acetate fraction (PRF). The antioxidant properties of the ethyl acetate fraction of roots of Piper sylvaticum were examined by DPPH radical scavenging activity and Fe2+ chelating ability. Significant scavenging activity were found for ethyl acetate fraction as compared to standard BHT, while ethyl acetate fraction showed good Fe2+ chelating ability as compared to standard EDTA. It was found that ethyl acetate fraction shows more potent hepatoprotective activity at different dose level against acetaminophen induced hepatic damage in Wistar albino rats. It was found that there was a remarkable decrease in serum Aspartate aminotransferase, serum Alanine aminotransferase, Total bilirubin, direct bilirubin and alkaline phosphatase level in treatment group as compared to the hepatotoxic group. From the observation, it can be concluded that the ethyl acetate fraction at dose level of 200 mg/kg body weight orally, gives the similar hepatoprotective effect as standard drug Silymarin at a dose level of 100 mg/kg body weight orally. It was concluded that phenolrich fraction of roots of Piper sylvaticum is found to be potent antioxidant and hepatoprotective without any cytotoxicity. [ABSTRACT FROM AUTHOR]

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