Siddhartha Maity

Phytochemistry, Pharmacology and Toxicology of Spilanthes acmella: A Review

Spilanthes acmella is an important medicinal plant, found in tropical and subtropical countries mainly India and South America. Popularly, it is known as toothache plant which reduces the pain associated with toothaches and can induce saliva secretion. Various extracts and active metabolites from various parts of this plant possess useful pharmacological activities. Literature survey proposed that it has multiple pharmacological actions, which include antifungal, antipyretic, local anaesthetic, bioinsecticide, anticonvulsant, antioxidant, aphrodisiac, analgesic, pancreatic lipase inhibitor, antimicrobial, antinociception, diuretic, vasorelaxant, anti-human immunodeficiency virus, toothache relieve and anti-inflammatory effects. This review is elaborately describing the traditional uses, phytochemistry, pharmacology, and toxicology of this plant. This review would assist researchers to search scientific information in the future.

Ca-carboxymethyl xanthan gum mini-matrices: Swelling, erosion and their impact on drug release mechanism

The effect of Ca(2+) ion concentration on swelling, erosion, and drug release mechanism of Ca(2+) ion cross-linked carboxymethyl xanthan gum (Ca-CMXG) matrices was investigated. By adding CaCl2 solution, carboxymethyl xanthan gum (CMXG) was converted into Ca-CMXG matrix, which was evaluated for swelling, erosion and drug release in different dissolution media. The amount of Ca(2+) ion alters the viscosity of gel layer formed around the matrices resulting in decreased water penetration into swollen layer. The changes in amount of Ca(2+) ion considerably influenced the swelling and erosion of the matrix leading to different drug release profiles. The simultaneous swelling and erosion of matrices that were controlled by the degree of cross-linking prejudiced the drug release mechanism. The release data fitted well into the Korsmeyer-Peppas equation and the combined effect of diffusion and erosion described the overall drug transport mechanism.

Effect of ionic crosslink on the release of metronidazole from partially carboxymethylated guar gum tablet.

Partially carboxymethylated guar gum (PCMGG) was crosslinked in situ by Ca(2+) ions during wet massing step of tablet preparation. The resulting tablets were evaluated for the effect of the extent of crosslinking on drug release and matrix swelling. Increase in the concentration of Ca(2+) ions increased the viscosity of gel layer and reduced the water penetration velocity into the matrix with subsequent decrease in swelling of the tablets and drug release. Beyond a certain concentration of Ca(2+) ions, the viscosity of the gel layer decreased and the drug release rate increased primarily due to erosion of the matrix. The mechanism of drug release appeared to be non-Fickian or anomalous transport. The release data also best fitted in zero order equation. The model drug, metronidazole, was compatible with the matrix materials as evident from instrumental analyses. Such formulation may provide flexibility in achieving the desired drug release rate from crosslinked matrix tablets.

Antiproliferative effect of isolated isoquinoline alkaloid from Mucuna pruriens seeds in hepatic carcinoma cells

The present study was undertaken to investigate the antiproliferative action of isolated M1 (6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) from Mucuna pruriens seeds using human hepatic carcinoma cell line (Huh-7 cells). Initially, docking studies was performed to find out the binding affinities of M1 to caspase-3 and 8 enzymes. Later, cytotoxic action of M1 was measured by cell growth inhibition (MTT), followed by caspase-3 and 8 enzymes assay colorimetrically. Our results collectively suggested that M1 had strong binding affinity to caspase-8 in molecular modelling. M1 possessed antiproliferative activity on Huh-7 cells (EC50 = 13.97 μM) and also inhibited the action of caspase-8 enzyme, signified process of apoptosis. M1 was active against Huh-7 cells that may be useful for future hepatic cancer treatment.

Phytochemistry, pharmacology, toxicology, and clinical trial of Ficus racemosa

Ficus racemosa is an important medicinal plant, found in India, Australia, and Southeast Asia. It is popularly known as ′gular.′ It reduces blood glucose concentration due to the presence of β-sitosterol. Many active constituents that have been isolated from various parts of this plant possess useful pharmacological activities. The literature survey proposed that it has multiple pharmacological actions that include antidiabetic, antioxidant, antidiarrhoeal, anti-inflammatory, antipyretic, antifungal, antibacterial, hypolipidemic, antifilarial, and hepatoprotection. This review article elaborately describes the traditional uses, phytochemistry, pharmacology, and toxicology of this plant. We also provide useful structures of the secondary metabolites along with their nuclear magnetic resonance (NMR) data. Some clinical trial data have also been provided in this review. This review would assist researchers to gather scientific information in future.

Effect of different cross-linking methods and processing parameters on drug release from hydrogel beads

The purpose of this work was to evaluate different methods of cross-linking for developing diltiazem-resin complex loaded carboxymethyl xanthan gum (CMXG) hydrogel beads to achieve highest possible drug entrapment and extended release for effective cardio-protection. The hydrogel beads were prepared by ionic cross-linking and dual cross-linking using simultaneous (SIM) and sequential (SEQ) methods. Among the three methods, SEQ method produced smaller sized beads having higher drug entrapment efficacy and prolonged release characteristics as evidenced from mean dissolution time and diffusion coefficient of drug. Keeping the concentration of ionic cross-linker constant, increase in the amount of covalent cross-linker and cross-linking time decreased the drug release. Higher release of the drug in acid solution was attributed to the higher solubility of the basic drug and higher swelling of the matrices in acid solution. Comparison of FTIR spectra, drug content and dissolution profiles indicated that the drug was stable in the beads when kept under stress condition up to 3 months. In conclusion, the sequential method was found superior for producing CMXG hydrogel beads as a prolonged release delivery device in cardiovascular diseases.

Development and evaluation of Ca(+ 2) ion cross-linked carboxymethyl xanthan gum tablet prepared by wet granulation technique.

The objective of this work was to study the release behavior of prednisolone from calcium-cross-linked carboxymethyl xanthan gum (CMXG) tablets in dissolution medium having different pH values prevailing in the gastrointestinal lumen. Xanthan gum (XG) was derivatized to CMXG which was then cross-linked in situ with Ca+2 ion during wet massing step of tablet preparation. Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry studies did not show any drug-polymer interaction although the drug underwent solid-state transformation during compression as evident from X-ray diffraction analysis. In vitro release study demonstrated that increase in the amount of Ca+2 ion decreased the drug release, and beyond a certain amount, the drug release increased. While increase in both drug load and tablet crushing strength decreased the drug release, increase in exposure time in acid solution of pH 1.2 increased the overall release of the drug. The mechanism of drug release was non-Fickian/anomalous. The results indicated that variation in the amount of Ca+2 ion can modulate the drug release from CMXG matrix tablets as needed.

An updated review on the phytochemistry, pharmacology, and clinical trials of Salacia oblonga

Salacia oblonga (S. oblonga), a perennial herb, has been used for thousands of years in ayurvedic medicine and is closely associated with prevention, treatment, and cure of various human ailments such as obesity and diabetes. A vast and wide range of chemical compounds such as polyphenols, friedelane-type triterpenes, norfriedelane-type triterpenes, eudesmane-type sesquiterpenes including various glycosides had been isolated from this plant. This review is aimed to survey the literature covering the phytochemistry and pharmacology of S. oblonga and to review the scientific data including active components and their multi-targeted mechanisms of action against various metabolic syndromes. We also included clinical trials related to this plant in this review. The overview would assist researchers to gather scientific information related to S. oblonga in future.

Modern Extraction Techniques for Drugs and Medicinal Agents

Abstract In this chapter, we have tried to include various physicochemical methods of extraction that comprise microwave-assisted extraction, pressurized liquid extraction, supercritical fluid extraction, liquid phase microextraction, solid phase extraction, ultrasound-assisted extraction, cloud-point extraction, enzyme-assisted extraction, membrane-based microextraction, and cooling-assisted microextraction. These are the commonly used techniques nowadays in terms of isolation and separation of ingredients from both chemical and biological mixtures. The description is based on principle, method, and comparison of various techniques. Their commercial applications both in analytical and industrial point of view are also included in this chapter. We also include few special biological extraction techniques at the end of this chapter. Finally, the conclusion is drawn based on the application of different techniques, target molecules, and sample types. This chapter will serve as a valuable tool and key milestone to researchers in a future application.

In Vitro and In Vivo Correlation of Colon-Targeted Compression-Coated Tablets

This study was performed to assess and correlate in vitro drug release with in vivo absorption of prednisolone (PDL) from a colon-targeted tablet prepared by compression coating of core tablet. In vivo drug absorption study was conducted using a high performance liquid chromatographic (HPLC) method, which was developed and validated for the estimation of PDL in rabbit plasma. The calibration curve showed linearity in the concentration range of 0.05 to 50 μg/mL with the correlation coefficient (r) of 0.999. The method was specific and sensitive with the limit of detection (LOD) and lower limit of quantification (LLOQ) of 31.89 ± 1.10 ng/mL and 96.63 ± 3.32 ng/mL, respectively. The extraction recovery (ER) of PDL from three different levels of quality control (QC) samples ranged from 98.18% to 103.54%. In vitro drug release study revealed that less than 10% drug was released in 6.34 h and almost complete (98.64%) drug release was achieved in the following 6 h. In vivo drug absorption study demonstrated lower values of C max, AUCtotal, and protracted T max from compression-coated tablet. The results confirmed the maximum release of drug in the colon while minimizing release in the upper gastrointestinal tract (GIT). An excellent in vitro and in vivo correlation (IVIVC) was also achieved after considering the lag time.